Identification

Name
Insulin Pork
Accession Number
DB00071  (BTD00031, BIOD00031)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Hormones / Insulins
Description

Insulin isolated from pig pancreas. Composed of alpha and beta chains, processed from pro-insulin. Forms a hexameric structure.

Protein structure
Db00071
Protein chemical formula
C257H387N65O76S6
Protein average weight
5795.6 Da
Sequences
>A chain
GIVEQCCTSICSLYQLENYCN
>B chain
FVNQHLCGSHLVEALYLVCGERGFFYTPKT
Download FASTA Format
Synonyms
  • Insulin (pork)
  • Insulin porcine
  • Insulin purified porcine
  • Insulin purified pork
  • Insulin, porcine
  • Insulin, regular, pork
  • Porcine insulin
Product Ingredients
IngredientUNIICASInChI Key
Insulin suspension isophane purified porkNot AvailableNot AvailableNot applicable
Insulin suspension protamine zinc purified porkNot AvailableNot AvailableNot applicable
Insulin zinc suspension prompt purified porkNot AvailableNot AvailableNot applicable
Insulin zinc suspension purified porkNot AvailableNot AvailableNot applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Hypurin Regular Insulin PorkSolution100 unitIntramuscular; Intravenous; SubcutaneousWockhardt Uk Ltd2006-04-01Not applicableCanada
International/Other Brands
Iletin II (Lilly)
Categories
UNII
AVT680JB39
CAS number
12584-58-6

Pharmacology

Indication

For the treatment of type I and II diabetes mellitus.

Structured Indications
Not Available
Pharmacodynamics

Insulin is used in the treatment of type I and type II diabetes. The primary activity of insulin is the regulation of glucose metabolism. In muscle and other tissues (except the brain), insulin causes rapid transport of glucose and amino acids intracellularly. It also promotes anabolism, and inhibits protein catabolism. In the liver, insulin promotes the uptake and storage of glucose in the form of glycogen, inhibits gluconeogenesis, and promotes the conversion of excess glucose into fat.

Mechanism of action

Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism.

TargetActionsOrganism
AInsulin receptor
binder
Human
UInsulin-like growth factor 1 receptorNot AvailableHuman
UInsulin-degrading enzymeNot AvailableHuman
UHLA class II histocompatibility antigen, DQ alpha 2 chainNot AvailableHuman
UHLA class II histocompatibility antigen, DQ beta 1 chainNot AvailableHuman
URetinoblastoma-associated proteinNot AvailableHuman
UCathepsin DNot AvailableHuman
UCarboxypeptidase ENot AvailableHuman
UNeuroendocrine convertase 2Not AvailableHuman
UNeuroendocrine convertase 1Not AvailableHuman
UProtein NOV homologNot AvailableHuman
ULow-density lipoprotein receptor-related protein 2Not AvailableHuman
UInsulin-like growth factor-binding protein 7Not AvailableHuman
USynaptotagmin-like protein 4Not AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process.

Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcebutololAcebutolol may increase the hypoglycemic activities of Insulin Pork.Approved
AlbiglutideAlbiglutide may increase the hypoglycemic activities of Insulin Pork.Approved
AlogliptinAlogliptin may increase the hypoglycemic activities of Insulin Pork.Approved
AlprenololAlprenolol may increase the hypoglycemic activities of Insulin Pork.Approved, Withdrawn
AripiprazoleThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Aripiprazole.Approved, Investigational
ArotinololArotinolol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
Arsenic trioxideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Arsenic trioxide.Approved, Investigational
ArticaineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Articaine.Approved
AsenapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Asenapine.Approved
AtazanavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the hypoglycemic activities of Insulin Pork.Approved
AtorvastatinAtorvastatin may increase the hypoglycemic activities of Insulin Pork.Approved
BefunololBefunolol may increase the hypoglycemic activities of Insulin Pork.Experimental
BendroflumethiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Bendroflumethiazide.Approved
BetamethasoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Betamethasone.Approved, Vet Approved
BetaxololBetaxolol may increase the hypoglycemic activities of Insulin Pork.Approved
BevantololBevantolol may increase the hypoglycemic activities of Insulin Pork.Approved
BisoprololBisoprolol may increase the hypoglycemic activities of Insulin Pork.Approved
BopindololBopindolol may increase the hypoglycemic activities of Insulin Pork.Approved
BrexpiprazoleThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Brexpiprazole.Approved
BucindololBucindolol may increase the hypoglycemic activities of Insulin Pork.Investigational
BufuralolBufuralol may increase the hypoglycemic activities of Insulin Pork.Experimental, Investigational
BumetanideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Bumetanide.Approved
BupranololBupranolol may increase the hypoglycemic activities of Insulin Pork.Approved
BuserelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Buserelin.Approved
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Insulin Pork.Approved
CarteololCarteolol may increase the hypoglycemic activities of Insulin Pork.Approved
CarvedilolCarvedilol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
CeliprololCeliprolol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
CeritinibThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ceritinib.Approved
ChlorothiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Chlorothiazide.Approved, Vet Approved
ChlorpropamideInsulin Pork may increase the hypoglycemic activities of Chlorpropamide.Approved
ChlorthalidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Chlorthalidone.Approved
CloranololCloranolol may increase the hypoglycemic activities of Insulin Pork.Experimental
ClozapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Clozapine.Approved
CorticotropinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Corticotropin.Approved, Vet Approved
Cortisone acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Cortisone acetate.Approved
CyclopenthiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Cyclopenthiazide.Experimental
Cyproterone acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Cyproterone acetate.Approved, Investigational
DabrafenibThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Dabrafenib.Approved
DanazolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Danazol.Approved
DarunavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Darunavir.Approved
DesogestrelThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Desogestrel.Approved
DexamethasoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Dexamethasone.Approved, Investigational, Vet Approved
DiazoxideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Diazoxide.Approved
DienogestThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Dienogest.Approved
DisopyramideInsulin Pork may increase the hypoglycemic activities of Disopyramide.Approved
DrospirenoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Drospirenone.Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Insulin Pork.Approved
Edetic AcidEdetic Acid may increase the hypoglycemic activities of Insulin Pork.Approved, Vet Approved
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Insulin Pork.Approved
EpanololEpanolol may increase the hypoglycemic activities of Insulin Pork.Experimental
EpinephrineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Epinephrine.Approved, Vet Approved
EsmololEsmolol may increase the hypoglycemic activities of Insulin Pork.Approved
EstradiolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Estradiol.Approved, Investigational, Vet Approved
Estrone sulfateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Estrone sulfate.Approved
Etacrynic acidThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Etacrynic acid.Approved
Ethinyl EstradiolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ethinyl Estradiol.Approved
Ethynodiol diacetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ethynodiol diacetate.Approved
EtonogestrelThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Etonogestrel.Approved, Investigational
EverolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Everolimus.Approved
ExenatideExenatide may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
FludrocortisoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Fludrocortisone.Approved
FosamprenavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Fosamprenavir.Approved
FurosemideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Furosemide.Approved, Vet Approved
GliclazideInsulin Pork may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideInsulin Pork may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideInsulin Pork may increase the hypoglycemic activities of Glipizide.Approved
GlyburideInsulin Pork may increase the hypoglycemic activities of Glyburide.Approved
GoserelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Goserelin.Approved
HistrelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Histrelin.Approved
HydrochlorothiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydrochlorothiazide.Approved, Vet Approved
HydrocortisoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydroflumethiazide.Approved, Investigational
Hydroxyprogesterone caproateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydroxyprogesterone caproate.Approved
IloperidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Iloperidone.Approved
IndapamideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Indapamide.Approved
IndenololIndenolol may increase the hypoglycemic activities of Insulin Pork.Withdrawn
IndinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Indinavir.Approved
Insulin AspartInsulin Pork may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirInsulin Pork may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineInsulin Pork may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineInsulin Pork may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Pork may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproInsulin Pork may increase the hypoglycemic activities of Insulin Lispro.Approved
LabetalolLabetalol may increase the hypoglycemic activities of Insulin Pork.Approved
LandiololLandiolol may increase the hypoglycemic activities of Insulin Pork.Investigational
LanreotideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Lanreotide.Approved
LeuprolideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Leuprolide.Approved, Investigational
LevonorgestrelThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Levonorgestrel.Approved, Investigational
LinagliptinLinagliptin may increase the hypoglycemic activities of Insulin Pork.Approved
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Insulin Pork.Approved, Nutraceutical
LiraglutideLiraglutide may increase the hypoglycemic activities of Insulin Pork.Approved
LopinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Lopinavir.Approved
LurasidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Lurasidone.Approved
MecaserminInsulin Pork may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Medroxyprogesterone acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Medroxyprogesterone acetate.Approved, Investigational
Megestrol acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
MepindololMepindolol may increase the hypoglycemic activities of Insulin Pork.Experimental
MestranolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Mestranol.Approved
MethotrimeprazineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Methotrimeprazine.Approved
MethyclothiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Methyclothiazide.Approved
MethylprednisoloneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Methylprednisolone.Approved, Vet Approved
MetolazoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Metolazone.Approved
MetoprololMetoprolol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
MetreleptinMetreleptin may increase the hypoglycemic activities of Insulin Pork.Approved
MifepristoneInsulin Pork may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
NadololNadolol may increase the hypoglycemic activities of Insulin Pork.Approved
NateglinideInsulin Pork may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NebivololNebivolol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
NelfinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Nelfinavir.Approved
NiacinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Niacin.Approved, Investigational, Nutraceutical
NilotinibThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Nilotinib.Approved, Investigational
NorethisteroneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Norethisterone.Approved
NorgestimateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Norgestimate.Approved
OctreotideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Octreotide.Approved, Investigational
OlanzapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Olanzapine.Approved, Investigational
OxprenololOxprenolol may increase the hypoglycemic activities of Insulin Pork.Approved
PaliperidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Paliperidone.Approved
PasireotideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pasireotide.Approved
PenbutololPenbutolol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
PentamidineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pentamidine.Approved
PindololPindolol may increase the hypoglycemic activities of Insulin Pork.Approved
PioglitazoneThe risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin Pork.Approved, Investigational
PiperazineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Piperazine.Approved, Vet Approved
PipotiazineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pipotiazine.Approved, Investigational
Platelet Activating FactorPlatelet Activating Factor may increase the hypoglycemic activities of Insulin Pork.Experimental
PolythiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Polythiazide.Approved
PractololPractolol may increase the hypoglycemic activities of Insulin Pork.Approved
PramlintidePramlintide may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
PrednisoloneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Prednisolone.Approved, Vet Approved
PrednisoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Prednisone.Approved, Vet Approved
ProgesteroneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Progesterone.Approved, Vet Approved
PropranololPropranolol may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
QuetiapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Quetiapine.Approved
QuinethazoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Quinethazone.Approved
QuinineInsulin Pork may increase the hypoglycemic activities of Quinine.Approved
RepaglinideInsulin Pork may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
RisperidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Risperidone.Approved, Investigational
RitonavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ritonavir.Approved, Investigational
RosiglitazoneThe risk or severity of myocardial ischemia can be increased when Insulin Pork is combined with Rosiglitazone.Approved, Investigational
SaquinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Insulin Pork.Approved
SirolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Sirolimus.Approved, Investigational
SitagliptinSitagliptin may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
SotalolSotalol may increase the hypoglycemic activities of Insulin Pork.Approved
SulfadiazineInsulin Pork may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleInsulin Pork may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfisoxazoleInsulin Pork may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SunitinibInsulin Pork may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tacrolimus.Approved, Investigational
TalinololTalinolol may increase the hypoglycemic activities of Insulin Pork.Investigational
TemsirolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Temsirolimus.Approved
TertatololTertatolol may increase the hypoglycemic activities of Insulin Pork.Experimental
TimololTimolol may increase the hypoglycemic activities of Insulin Pork.Approved
TipranavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tipranavir.Approved, Investigational
TolazamideInsulin Pork may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideInsulin Pork may increase the hypoglycemic activities of Tolbutamide.Approved
TorasemideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Torasemide.Approved
TriamcinoloneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Triamcinolone.Approved, Vet Approved
TrichlormethiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Trichlormethiazide.Approved, Vet Approved
TriptorelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Triptorelin.Approved, Vet Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Insulin Pork.Approved, Investigational
VorinostatThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Vorinostat.Approved, Investigational
ZiprasidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ziprasidone.Approved
Food Interactions
Not Available

References

Synthesis Reference

Bruce H. Frank, "Process for producing an insulin precursor." U.S. Patent US4430266, issued November, 1974.

US4430266
General References
Not Available
External Links
UniProt
Q8HXV2
Genbank
AY137503
PubChem Substance
46508925
Therapeutic Targets Database
DAP001089
PharmGKB
PA164781053
ATC Codes
A10AC03 — Insulin (pork)A10AB03 — Insulin (pork)A10AE03 — Insulin (pork)A10AD03 — Insulin (pork)
AHFS Codes
  • 68:20.08 — Insulins

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
  • Novo nordisk inc
Packagers
Not Available
Dosage forms
FormRouteStrength
SolutionIntramuscular; Intravenous; Subcutaneous100 unit
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
water solubilitySlightly solubleNot Available
hydrophobicity0.218Not Available
isoelectric point5.39Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Binder
General Function
Receptor signaling protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase which mediates the pleiotropic actions of insulin. Binding of insulin leads to phosphorylation of several intracellular substrates, including, insulin receptor substrates (...
Gene Name
INSR
Uniprot ID
P06213
Uniprot Name
Insulin receptor
Molecular Weight
156331.465 Da
References
  1. Chen LM, Yang XW, Tang JG: Acidic residues on the N-terminus of proinsulin C-Peptide are important for the folding of insulin precursor. J Biochem. 2002 Jun;131(6):855-9. [PubMed:12038982]
  2. Desbuquois B, Chauvet G, Kouach M, Authier F: Cell itinerary and metabolic fate of proinsulin in rat liver: in vivo and in vitro studies. Endocrinology. 2003 Dec;144(12):5308-21. Epub 2003 Sep 11. [PubMed:12970169]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase which mediates actions of insulin-like growth factor 1 (IGF1). Binds IGF1 with high affinity and IGF2 and insulin (INS) with a lower affinity. The activated IGF1R is involv...
Gene Name
IGF1R
Uniprot ID
P08069
Uniprot Name
Insulin-like growth factor 1 receptor
Molecular Weight
154791.73 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Fottner C, Engelhardt D, Weber MM: Regulation of steroidogenesis by insulin-like growth factors (IGFs) in adult human adrenocortical cells: IGF-I and, more potently, IGF-II preferentially enhance androgen biosynthesis through interaction with the IGF-I receptor and IGF-binding proteins. J Endocrinol. 1998 Sep;158(3):409-17. [PubMed:9846170]
  4. Zhang Q, Berggren PO, Hansson A, Tally M: Insulin-like growth factor-I-induced DNA synthesis in insulin-secreting cell line RINm5F is associated with phosphorylation of the insulin-like growth factor-I receptor and the insulin receptor substrate-2. J Endocrinol. 1998 Mar;156(3):573-81. [PubMed:9582514]
  5. Sowers JR, Jacobs DB, Simpson L, al-Homsi B, Grunberger G, Sokol R: Erythrocyte insulin and insulin-like growth factor-I receptor tyrosine kinase activity in hypertension in pregnancy. Metabolism. 1995 Oct;44(10):1308-13. [PubMed:7476290]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Plays a role in the cellular breakdown of insulin, IAPP, glucagon, bradykinin, kallidin and other peptides, and thereby plays a role in intercellular peptide signaling. Degrades amyloid formed by A...
Gene Name
IDE
Uniprot ID
P14735
Uniprot Name
Insulin-degrading enzyme
Molecular Weight
117967.49 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Harada S, Smith RM, Smith JA, Jarett L: Inhibition of insulin-degrading enzyme increases translocation of insulin to the nucleus in H35 rat hepatoma cells: evidence of a cytosolic pathway. Endocrinology. 1993 Jun;132(6):2293-8. [PubMed:8504733]
  4. Hsu MC, Bai JP: Investigation into the presence of insulin-degrading enzyme in cultured type II alveolar cells and the effects of enzyme inhibitors on pulmonary bioavailability of insulin in rats. J Pharm Pharmacol. 1998 May;50(5):507-14. [PubMed:9643444]
  5. MARIGO S, PANELLI G: [Insulinase and its inhibition by hypoglycemic sulfonamides; data on insulin sensitivity during tolbutamide therapy]. Arch Sci Med (Torino). 1958 Jun;105(6):587-609. [PubMed:13560210]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Mhc class ii receptor activity
Specific Function
Binds peptides derived from antigens that access the endocytic route of antigen presenting cells (APC) and presents them on the cell surface for recognition by the CD4 T-cells. The peptide binding ...
Gene Name
HLA-DQA2
Uniprot ID
P01906
Uniprot Name
HLA class II histocompatibility antigen, DQ alpha 2 chain
Molecular Weight
28032.82 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Pugliese A, Bugawan T, Moromisato R, Awdeh ZL, Alper CA, Jackson RA, Erlich HA, Eisenbarth GS: Two subsets of HLA-DQA1 alleles mark phenotypic variation in levels of insulin autoantibodies in first degree relatives at risk for insulin-dependent diabetes. J Clin Invest. 1994 Jun;93(6):2447-52. [PubMed:8200980]
  4. Hermann R, Soltesz G: [Pathogenesis and types of neonatal diabetes]. Orv Hetil. 2000 Aug 20;141(34):1855-8. [PubMed:11006709]
  5. Donner H, Rau H, Braun J, Herwig J, Usadel KH, Badenhoop K: Highly polymorphic promoter regions of HLA DQA1 and DQB1 genes do not help to further define disease susceptibility in insulin-dependent diabetes mellitus. Tissue Antigens. 1997 Dec;50(6):642-5. [PubMed:9458118]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Peptide antigen binding
Specific Function
Binds peptides derived from antigens that access the endocytic route of antigen presenting cells (APC) and presents them on the cell surface for recognition by the CD4 T-cells. The peptide binding ...
Gene Name
HLA-DQB1
Uniprot ID
P01920
Uniprot Name
HLA class II histocompatibility antigen, DQ beta 1 chain
Molecular Weight
29991.02 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Mahran MZ, Ross DG, Sadeghi-Nejad A, Rabson AR: Use of the polymerase chain reaction mismatch technique to identify the HLA-DQw8 allele in patients with insulin-dependent diabetes mellitus. Am J Clin Pathol. 1992 Jan;97(1):29-33. [PubMed:1728861]
  4. Levy-Marchal C, Tichet J, Fajardy I, Gu XF, Dubois F, Czernichow P: Islet cell antibodies in normal French schoolchildren. Diabetologia. 1992 Jun;35(6):577-82. [PubMed:1612232]
  5. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Ubiquitin protein ligase binding
Specific Function
Key regulator of entry into cell division that acts as a tumor suppressor. Promotes G0-G1 transition when phosphorylated by CDK3/cyclin-C. Acts as a transcription repressor of E2F1 target genes. Th...
Gene Name
RB1
Uniprot ID
P06400
Uniprot Name
Retinoblastoma-associated protein
Molecular Weight
106158.335 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Biener Y, Zick Y: Basic polycations activate the insulin receptor kinase and a tightly associated serine kinase. Eur J Biochem. 1990 Nov 26;194(1):243-50. [PubMed:1701386]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Aspartic-type endopeptidase activity
Specific Function
Acid protease active in intracellular protein breakdown. Involved in the pathogenesis of several diseases such as breast cancer and possibly Alzheimer disease.
Gene Name
CTSD
Uniprot ID
P07339
Uniprot Name
Cathepsin D
Molecular Weight
44551.845 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Authier F, Metioui M, Fabrega S, Kouach M, Briand G: Endosomal proteolysis of internalized insulin at the C-terminal region of the B chain by cathepsin D. J Biol Chem. 2002 Mar 15;277(11):9437-46. Epub 2002 Jan 4. [PubMed:11779865]
  4. Ogino S, Cohen ML, Abdul-Karim FW: Atypical teratoid/rhabdoid tumor of the CNS: cytopathology and immunohistochemistry of insulin-like growth factor-II, insulin-like growth factor receptor type 1, cathepsin D, and Ki-67. Mod Pathol. 1999 Apr;12(4):379-85. [PubMed:10229502]
  5. Nunn SE, Peehl DM, Cohen P: Acid-activated insulin-like growth factor binding protein protease activity of cathepsin D in normal and malignant prostatic epithelial cells and seminal plasma. J Cell Physiol. 1997 May;171(2):196-204. [PubMed:9130467]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Removes residual C-terminal Arg or Lys remaining after initial endoprotease cleavage during prohormone processing. Processes proinsulin.
Gene Name
CPE
Uniprot ID
P16870
Uniprot Name
Carboxypeptidase E
Molecular Weight
53150.185 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Polastri L, Galbiati F, Folli F, Davalli AM: Effects of carboxypeptidase E overexpression on insulin mRNA levels, regulated insulin secretion, and proinsulin processing of pituitary GH3 cells transfected with a furin-cleavable human proinsulin cDNA. Cell Transplant. 2002;11(8):803-11. [PubMed:12588113]
  4. Guest PC, Pipeleers D, Rossier J, Rhodes CJ, Hutton JC: Co-secretion of carboxypeptidase H and insulin from isolated rat islets of Langerhans. Biochem J. 1989 Dec 1;264(2):503-8. [PubMed:2481446]
  5. Furuta M, Carroll R, Martin S, Swift HH, Ravazzola M, Orci L, Steiner DF: Incomplete processing of proinsulin to insulin accompanied by elevation of Des-31,32 proinsulin intermediates in islets of mice lacking active PC2. J Biol Chem. 1998 Feb 6;273(6):3431-7. [PubMed:9452465]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Responsible for the release of glucagon from proglucagon in pancreatic A...
Gene Name
PCSK2
Uniprot ID
P16519
Uniprot Name
Neuroendocrine convertase 2
Molecular Weight
70564.735 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Zertal-Zidani S, Bounacer A, Scharfmann R: Regulation of pancreatic endocrine cell differentiation by sulphated proteoglycans. Diabetologia. 2007 Mar;50(3):585-95. Epub 2007 Jan 13. [PubMed:17221210]
  4. Utsunomiya N, Ohagi S, Sanke T, Tatsuta H, Hanabusa T, Nanjo K: Organization of the human carboxypeptidase E gene and molecular scanning for mutations in Japanese subjects with NIDDM or obesity. Diabetologia. 1998 Jun;41(6):701-5. [PubMed:9662053]
  5. Ohagi S, Sakaguchi H, Sanke T, Tatsuta H, Hanabusa T, Nanjo K: Human prohormone convertase 3 gene: exon-intron organization and molecular scanning for mutations in Japanese subjects with NIDDM. Diabetes. 1996 Jul;45(7):897-901. [PubMed:8666140]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serine-type endopeptidase activity
Specific Function
Involved in the processing of hormone and other protein precursors at sites comprised of pairs of basic amino acid residues. Substrates include POMC, renin, enkephalin, dynorphin, somatostatin, ins...
Gene Name
PCSK1
Uniprot ID
P29120
Uniprot Name
Neuroendocrine convertase 1
Molecular Weight
84150.92 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Marriott D, Gillece-Castro B, Gorman CM: Prohormone convertase-1 will process prorelaxin, a member of the insulin family of hormones. Mol Endocrinol. 1992 Sep;6(9):1441-50. [PubMed:1435788]
  4. Zhu X, Orci L, Carroll R, Norrbom C, Ravazzola M, Steiner DF: Severe block in processing of proinsulin to insulin accompanied by elevation of des-64,65 proinsulin intermediates in islets of mice lacking prohormone convertase 1/3. Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10299-304. Epub 2002 Jul 22. [PubMed:12136131]
  5. Kuwahata M, Tomoe Y, Harada N, Amano S, Segawa H, Tatsumi S, Ito M, Oka T, Miyamoto K: Characterization of the molecular mechanisms involved in the increased insulin secretion in rats with acute liver failure. Biochim Biophys Acta. 2007 Jan;1772(1):60-5. Epub 2006 Oct 4. [PubMed:17097861]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Notch binding
Specific Function
Immediate-early protein playing a role in various cellular processes including proliferation, adhesion, migration, differentiation and survival (PubMed:15181016, PubMed:15611078, PubMed:12695522, P...
Gene Name
NOV
Uniprot ID
P48745
Uniprot Name
Protein NOV homolog
Molecular Weight
39161.82 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Burren CP, Wilson EM, Hwa V, Oh Y, Rosenfeld RG: Binding properties and distribution of insulin-like growth factor binding protein-related protein 3 (IGFBP-rP3/NovH), an additional member of the IGFBP Superfamily. J Clin Endocrinol Metab. 1999 Mar;84(3):1096-103. [PubMed:10084601]
  4. Lafont J, Laurent M, Thibout H, Lallemand F, Le Bouc Y, Atfi A, Martinerie C: The expression of novH in adrenocortical cells is down-regulated by TGFbeta 1 through c-Jun in a Smad-independent manner. J Biol Chem. 2002 Oct 25;277(43):41220-9. Epub 2002 Jul 30. [PubMed:12149257]
  5. Martinerie C, Chevalier G, Rauscher FJ 3rd, Perbal B: Regulation of nov by WT1: a potential role for nov in nephrogenesis. Oncogene. 1996 Apr 4;12(7):1479-92. [PubMed:8622864]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Calcium ion binding
Specific Function
Acts together with cubilin to mediate HDL endocytosis (By similarity). May participate in regulation of parathyroid-hormone and para-thyroid-hormone-related protein release.
Gene Name
LRP2
Uniprot ID
P98164
Uniprot Name
Low-density lipoprotein receptor-related protein 2
Molecular Weight
521952.77 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Orlando RA, Rader K, Authier F, Yamazaki H, Posner BI, Bergeron JJ, Farquhar MG: Megalin is an endocytic receptor for insulin. J Am Soc Nephrol. 1998 Oct;9(10):1759-66. [PubMed:9773776]
  4. Christensen EI, Birn H: Hormone, growth factor, and vitamin handling by proximal tubule cells. Curr Opin Nephrol Hypertens. 1997 Jan;6(1):20-7. [PubMed:9051350]
  5. Fuster DG, Bobulescu IA, Zhang J, Wade J, Moe OW: Characterization of the regulation of renal Na+/H+ exchanger NHE3 by insulin. Am J Physiol Renal Physiol. 2007 Feb;292(2):F577-85. Epub 2006 Oct 3. [PubMed:17018843]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Not Available
Specific Function
Binds IGF-I and IGF-II with a relatively low affinity. Stimulates prostacyclin (PGI2) production. Stimulates cell adhesion.
Gene Name
IGFBP7
Uniprot ID
Q16270
Uniprot Name
Insulin-like growth factor-binding protein 7
Molecular Weight
29130.055 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Lopez-Bermejo A, Buckway CK, Devi GR, Hwa V, Plymate SR, Oh Y, Rosenfeld RG: Characterization of insulin-like growth factor-binding protein-related proteins (IGFBP-rPs) 1, 2, and 3 in human prostate epithelial cells: potential roles for IGFBP-rP1 and 2 in senescence of the prostatic epithelium. Endocrinology. 2000 Nov;141(11):4072-80. [PubMed:11089538]
  4. Radulescu RT: One for all and all for one: RB defends the cell while IDE, PTEN and IGFBP-7 antagonize insulin and IGFs to protect RB. Med Hypotheses. 2007;69(5):1018-20. Epub 2007 May 1. [PubMed:17475416]
  5. Degeorges A, Wang F, Frierson HF Jr, Seth A, Chung LW, Sikes RA: Human prostate cancer expresses the low affinity insulin-like growth factor binding protein IGFBP-rP1. Cancer Res. 1999 Jun 15;59(12):2787-90. [PubMed:10383131]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Modulates exocytosis of dense-core granules and secretion of hormones in the pancreas and the pituitary. Interacts with vesicles containing negatively charged phospholipids in a Ca(2+)-independent ...
Gene Name
SYTL4
Uniprot ID
Q96C24
Uniprot Name
Synaptotagmin-like protein 4
Molecular Weight
76022.99 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Gomi H, Mizutani S, Kasai K, Itohara S, Izumi T: Granuphilin molecularly docks insulin granules to the fusion machinery. J Cell Biol. 2005 Oct 10;171(1):99-109. [PubMed:16216924]
  4. Plaisance V, Abderrahmani A, Perret-Menoud V, Jacquemin P, Lemaigre F, Regazzi R: MicroRNA-9 controls the expression of Granuphilin/Slp4 and the secretory response of insulin-producing cells. J Biol Chem. 2006 Sep 15;281(37):26932-42. Epub 2006 Jul 10. [PubMed:16831872]
  5. Torii S, Takeuchi T, Nagamatsu S, Izumi T: Rab27 effector granuphilin promotes the plasma membrane targeting of insulin granules via interaction with syntaxin 1a. J Biol Chem. 2004 May 21;279(21):22532-8. Epub 2004 Mar 17. [PubMed:15028737]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34