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Identification
NameInsulin Pork
Accession NumberDB00071  (BTD00031, BIOD00031)
TypeBiotech
GroupsApproved
DescriptionInsulin isolated from pig pancreas. Composed of alpha and beta chains, processed from pro-insulin. Forms a hexameric structure.
Protein structureDb00071
Related Articles
Protein chemical formulaC257H387N65O76S6
Protein average weight5795.6 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
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Iletin IILilly
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Insulin suspension isophane purified pork
ThumbNot applicableDBSALT001735
Insulin suspension protamine zinc purified pork
ThumbNot applicableDBSALT001736
Insulin zinc suspension prompt purified pork
ThumbNot applicableDBSALT001737
Insulin zinc suspension purified pork
ThumbNot applicableDBSALT001738
Categories
UNIIAVT680JB39
CAS number12584-58-6
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of type I and II diabetes mellitus.
PharmacodynamicsInsulin 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 actionInsulin 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.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

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

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
Manufacturers
  • Eli lilly and co
  • Novo nordisk inc
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
water solubilitySlightly solubleNot Available
hydrophobicity0.218Not Available
isoelectric point5.39Not Available
References
Synthesis Reference

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

US4430266
General ReferencesNot Available
External Links
ATC CodesA10AC03A10AB03A10AE03A10AD03
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololAcebutolol may increase the hypoglycemic activities of Insulin Pork.
AlbiglutideAlbiglutide may increase the hypoglycemic activities of Insulin Pork.
AlogliptinAlogliptin may increase the hypoglycemic activities of Insulin Pork.
AlprenololAlprenolol may increase the hypoglycemic activities of Insulin Pork.
AripiprazoleThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Aripiprazole.
ArotinololArotinolol may increase the hypoglycemic activities of Insulin Pork.
Arsenic trioxideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Arsenic trioxide.
ArticaineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Asenapine.
AtazanavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Atazanavir.
AtenololAtenolol may increase the hypoglycemic activities of Insulin Pork.
AtorvastatinAtorvastatin may increase the hypoglycemic activities of Insulin Pork.
BefunololBefunolol may increase the hypoglycemic activities of Insulin Pork.
BendroflumethiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Bendroflumethiazide.
BetamethasoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Betamethasone.
BetaxololBetaxolol may increase the hypoglycemic activities of Insulin Pork.
BevantololBevantolol may increase the hypoglycemic activities of Insulin Pork.
BisoprololBisoprolol may increase the hypoglycemic activities of Insulin Pork.
BopindololBopindolol may increase the hypoglycemic activities of Insulin Pork.
BrexpiprazoleThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Brexpiprazole.
BufuralolBufuralol may increase the hypoglycemic activities of Insulin Pork.
BumetanideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Bumetanide.
BupranololBupranolol may increase the hypoglycemic activities of Insulin Pork.
BuserelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Buserelin.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Insulin Pork.
CarteololCarteolol may increase the hypoglycemic activities of Insulin Pork.
CarvedilolCarvedilol may increase the hypoglycemic activities of Insulin Pork.
CeliprololCeliprolol may increase the hypoglycemic activities of Insulin Pork.
CeritinibThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ceritinib.
ChlorothiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Chlorothiazide.
ChlorpropamideInsulin Pork may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Chlorthalidone.
ClozapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Clozapine.
CorticotropinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Cortisone acetate.
Cyproterone acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Dabrafenib.
DanazolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Danazol.
DarunavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Darunavir.
DesogestrelThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Dexamethasone.
DiazoxideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Diazoxide.
DienogestThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Dienogest.
DisopyramideInsulin Pork may increase the hypoglycemic activities of Disopyramide.
DrospirenoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Drospirenone.
DulaglutideDulaglutide may increase the hypoglycemic activities of Insulin Pork.
Edetic AcidEdetic Acid may increase the hypoglycemic activities of Insulin Pork.
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Insulin Pork.
EpinephrineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Epinephrine.
EsmololEsmolol may increase the hypoglycemic activities of Insulin Pork.
EstradiolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Estrone sulfate.
Etacrynic acidThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Etacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ethynodiol diacetate.
EtonogestrelThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Etonogestrel.
EverolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Everolimus.
ExenatideExenatide may increase the hypoglycemic activities of Insulin Pork.
FludrocortisoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Fludrocortisone.
FosamprenavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Fosamprenavir.
FurosemideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Furosemide.
GliclazideInsulin Pork may increase the hypoglycemic activities of Gliclazide.
GlimepirideInsulin Pork may increase the hypoglycemic activities of Glimepiride.
GlipizideInsulin Pork may increase the hypoglycemic activities of Glipizide.
GlyburideInsulin Pork may increase the hypoglycemic activities of Glyburide.
GoserelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Goserelin.
HistrelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Histrelin.
HydrochlorothiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydrocortisone.
HydroflumethiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydroflumethiazide.
Hydroxyprogesterone caproateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Hydroxyprogesterone caproate.
IloperidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Iloperidone.
IndapamideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Indapamide.
IndenololIndenolol may increase the hypoglycemic activities of Insulin Pork.
IndinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Indinavir.
Insulin AspartInsulin Pork may increase the hypoglycemic activities of Insulin Aspart.
Insulin DetemirInsulin Pork may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineInsulin Pork may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineInsulin Pork may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanInsulin Pork may increase the hypoglycemic activities of Insulin Human.
Insulin LisproInsulin Pork may increase the hypoglycemic activities of Insulin Lispro.
LabetalolLabetalol may increase the hypoglycemic activities of Insulin Pork.
LanreotideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Lanreotide.
LanreotideInsulin Pork may increase the hypoglycemic activities of Lanreotide.
LeuprolideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Leuprolide.
LevonorgestrelThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Levonorgestrel.
LinagliptinLinagliptin may increase the hypoglycemic activities of Insulin Pork.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Insulin Pork.
LiraglutideLiraglutide may increase the hypoglycemic activities of Insulin Pork.
LopinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Lopinavir.
LurasidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Lurasidone.
MecaserminInsulin Pork may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Medroxyprogesterone acetate.
Megestrol acetateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Megestrol acetate.
MestranolThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Mestranol.
MethotrimeprazineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Methyclothiazide.
MethylprednisoloneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Methylprednisolone.
MetolazoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Metolazone.
MetoprololMetoprolol may increase the hypoglycemic activities of Insulin Pork.
MetreleptinMetreleptin may increase the hypoglycemic activities of Insulin Pork.
MifepristoneInsulin Pork may increase the hypoglycemic activities of Mifepristone.
NadololNadolol may increase the hypoglycemic activities of Insulin Pork.
NateglinideInsulin Pork may increase the hypoglycemic activities of Nateglinide.
NelfinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Nelfinavir.
NiacinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Niacin.
NilotinibThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Nilotinib.
NorethisteroneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Norethisterone.
NorgestimateThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Norgestimate.
OctreotideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Octreotide.
OctreotideInsulin Pork may increase the hypoglycemic activities of Octreotide.
OlanzapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Olanzapine.
OxprenololOxprenolol may increase the hypoglycemic activities of Insulin Pork.
PaliperidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Paliperidone.
PasireotideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pasireotide.
PasireotideInsulin Pork may increase the hypoglycemic activities of Pasireotide.
PenbutololPenbutolol may increase the hypoglycemic activities of Insulin Pork.
PentamidineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pentamidine.
PentamidineInsulin Pork may increase the hypoglycemic activities of Pentamidine.
PindololPindolol may increase the hypoglycemic activities of Insulin Pork.
PioglitazoneThe risk or severity of adverse effects can be increased when Pioglitazone is combined with Insulin Pork.
PiperazineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Piperazine.
PipotiazineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Pipotiazine.
PolythiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Polythiazide.
PractololPractolol may increase the hypoglycemic activities of Insulin Pork.
PramlintidePramlintide may increase the hypoglycemic activities of Insulin Pork.
PrednisoloneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Prednisone.
ProgesteroneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Progesterone.
PropranololPropranolol may increase the hypoglycemic activities of Insulin Pork.
QuetiapineThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Quetiapine.
QuinethazoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Quinethazone.
QuinineInsulin Pork may increase the hypoglycemic activities of Quinine.
RepaglinideInsulin Pork may increase the hypoglycemic activities of Repaglinide.
RisperidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ritonavir.
RosiglitazoneThe risk or severity of adverse effects can be increased when Insulin Pork is combined with Rosiglitazone.
SaquinavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Saquinavir.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Insulin Pork.
SirolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Sirolimus.
SitagliptinSitagliptin may increase the hypoglycemic activities of Insulin Pork.
SotalolSotalol may increase the hypoglycemic activities of Insulin Pork.
SulfadiazineInsulin Pork may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleInsulin Pork may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleInsulin Pork may increase the hypoglycemic activities of Sulfisoxazole.
SunitinibInsulin Pork may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tacrolimus.
TemsirolimusThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Temsirolimus.
TimololTimolol may increase the hypoglycemic activities of Insulin Pork.
TipranavirThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Tipranavir.
TolazamideInsulin Pork may increase the hypoglycemic activities of Tolazamide.
TolbutamideInsulin Pork may increase the hypoglycemic activities of Tolbutamide.
TorasemideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Torasemide.
TriamcinoloneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Triamcinolone.
TrichlormethiazideThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Trichlormethiazide.
TriptorelinThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Triptorelin.
VildagliptinVildagliptin may increase the hypoglycemic activities of Insulin Pork.
VorinostatThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Vorinostat.
ZiprasidoneThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Ziprasidone.
Food InteractionsNot 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 (IRS1, 2, 3, 4), SHC, GAB1, CBL and other signaling intermediates. Each of these phosphorylated proteins serve as docking proteins for other signaling proteins that contain Src-homology-2 domains (SH2 ...
Gene Name:
INSR
Uniprot ID:
P06213
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 involved in cell growth and survival control. IGF1R is crucial for tumor transformation and survival of malignant cell. Ligand binding activates the receptor kinase, leading to receptor autophosphorylation,...
Gene Name:
IGF1R
Uniprot ID:
P08069
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 APP and IAPP. May play a role in the degradation and clearance of naturally secreted amyloid beta-protein by neurons and microglia.(Microbial infection) The membrane-associated isoform acts as an entry...
Gene Name:
IDE
Uniprot ID:
P14735
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 cleft accommodates peptides of 10-30 residues. The peptides presented by MHC class II molecules are generated mostly by degradation of proteins that access the endocytic route, where they are processe...
Gene Name:
HLA-DQA2
Uniprot ID:
P01906
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 cleft accommodates peptides of 10-30 residues. The peptides presented by MHC class II molecules are generated mostly by degradation of proteins that access the endocytic route, where they are processe...
Gene Name:
HLA-DQB1
Uniprot ID:
P01920
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. The underphosphorylated, active form of RB1 interacts with E2F1 and represses its transcription activity, leading to cell cycle arrest. Directly involved in heterochromatin formation by maintaining over...
Gene Name:
RB1
Uniprot ID:
P06400
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
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
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 cells.
Gene Name:
PCSK2
Uniprot ID:
P16519
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, insulin and AGRP.
Gene Name:
PCSK1
Uniprot ID:
P29120
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, PubMed:21344378, PubMed:12050162). Acts by binding to integrins or membrane receptors such as NOTCH1 (PubMed:12695522, PubMed:21344378, PubMed:15611078). Essential regulator of hematopoietic stem and p...
Gene Name:
NOV
Uniprot ID:
P48745
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
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
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 manner (By similarity).
Gene Name:
SYTL4
Uniprot ID:
Q96C24
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23