Identification

Name
Cholesterol
Accession Number
DB04540  (EXPT00945)
Type
Small Molecule
Groups
Experimental, Investigational
Description

The principal sterol of all higher animals, distributed in body tissues, especially the brain and spinal cord, and in animal fats and oils. [PubChem]

Structure
Thumb
Synonyms
Not Available
External IDs
NSC-8798
Product Ingredients
IngredientUNIICASInChI Key
Cholesteryl chloride39EHZ05V39910-31-6OTVRYZXVVMZHHW-DPAQBDIFSA-N
Cholesteryl sulfateNot Available1256-86-6BHYOQNUELFTYRT-DPAQBDIFSA-N
Categories
UNII
97C5T2UQ7J
CAS number
57-88-5
Weight
Average: 386.6535
Monoisotopic: 386.354866094
Chemical Formula
C27H46O
InChI Key
HVYWMOMLDIMFJA-DPAQBDIFSA-N
InChI
InChI=1S/C27H46O/c1-18(2)7-6-8-19(3)23-11-12-24-22-10-9-20-17-21(28)13-15-26(20,4)25(22)14-16-27(23,24)5/h9,18-19,21-25,28H,6-8,10-17H2,1-5H3/t19-,21+,22+,23-,24+,25+,26+,27-/m1/s1
IUPAC Name
(1S,2R,5S,10S,11S,14R,15R)-2,15-dimethyl-14-[(2R)-6-methylheptan-2-yl]tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-7-en-5-ol
SMILES

Pharmacology

Indication
Not Available
Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action
TargetActionsOrganism
UNuclear receptor ROR-alphaNot AvailableHuman
UNuclear receptor subfamily 1 group I member 3Not AvailableHuman
UVitamin D3 receptorNot AvailableHuman
UC-type lectin domain family 4 member E
ligand
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
PathwayCategory
Rosuvastatin Action PathwayDrug action
Fluvastatin Action PathwayDrug action
CHILD SyndromeDisease
Hyper-IgD syndromeDisease
Corticosterone methyl oxidase I deficiency (CMO I)Disease
27-Hydroxylase DeficiencyDisease
Cerivastatin Action PathwayDrug action
Pamidronate Action PathwayDrug action
SteroidogenesisMetabolic
Atorvastatin Action PathwayDrug action
Adrenal Hyperplasia Type 3 or Congenital Adrenal Hyperplasia due to 21-hydroxylase DeficiencyDisease
Cholesteryl ester storage diseaseDisease
Mevalonic aciduriaDisease
Alendronate Action PathwayDrug action
Zoledronate Action PathwayDrug action
Cerebrotendinous Xanthomatosis (CTX)Disease
Congenital Lipoid Adrenal Hyperplasia (CLAH) or Lipoid CAHDisease
Adrenal Hyperplasia Type 5 or Congenital Adrenal Hyperplasia due to 17 Alpha-hydroxylase DeficiencyDisease
Wolman diseaseDisease
11-beta-hydroxylase deficiency (CYP11B1)Disease
Corticosterone methyl oxidase II deficiency - CMO IIDisease
Pravastatin Action PathwayDrug action
Risedronate Action PathwayDrug action
HypercholesterolemiaDisease
Congenital Bile Acid Synthesis Defect Type IIDisease
Zellweger SyndromeDisease
Congenital Bile Acid Synthesis Defect Type IIIDisease
21-hydroxylase deficiency (CYP21)Disease
Apparent mineralocorticoid excess syndromeDisease
3-Beta-Hydroxysteroid Dehydrogenase DeficiencyDisease
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Cholesterol.Approved, Investigational
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Cholesterol.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Cholesterol.Experimental
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Cholesterol.Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Cholesterol.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Cholesterol.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Cholesterol.Experimental, Investigational
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Cholesterol.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Cholesterol.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Cholesterol.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Cholesterol.Approved, Investigational
BoceprevirThe serum concentration of Cholesterol can be decreased when it is combined with Boceprevir.Approved, Withdrawn
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Cholesterol.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Cholesterol.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Cholesterol.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Cholesterol.Approved
CarbamazepineThe metabolism of Cholesterol can be increased when combined with Carbamazepine.Approved, Investigational
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Cholesterol.Investigational, Withdrawn
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Cholesterol.Approved, Investigational, Withdrawn
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Cholesterol.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Cholesterol.Approved, Vet Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Cholesterol.Approved
Conjugated estrogensThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cholesterol.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Cholesterol.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Cholesterol.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Cholesterol.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Cholesterol.Experimental
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Cholesterol.Approved
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Cholesterol.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Cholesterol.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Cholesterol.Approved
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Cholesterol.Experimental
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Cholesterol.Approved, Investigational
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Cholesterol.Approved, Investigational
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Cholesterol.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Cholesterol.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Cholesterol.Approved, Investigational
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Cholesterol.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Cholesterol.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Cholesterol.Approved, Investigational
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Cholesterol.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Cholesterol.Approved
EltrombopagThe serum concentration of Cholesterol can be increased when it is combined with Eltrombopag.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Cholesterol.Approved, Investigational
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Cholesterol.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Cholesterol.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Cholesterol.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Cholesterol.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Cholesterol.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Cholesterol.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Cholesterol.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Cholesterol.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Cholesterol.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Cholesterol.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Cholesterol.Approved
GarlicThe serum concentration of Cholesterol can be decreased when it is combined with Garlic.Approved
GitoformateGitoformate may decrease the cardiotoxic activities of Cholesterol.Experimental
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Cholesterol.Withdrawn
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Cholesterol.Experimental
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Cholesterol.Experimental
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Cholesterol.Approved
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Cholesterol.Experimental
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Cholesterol.Approved, Investigational
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Cholesterol.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Cholesterol.Experimental
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Cholesterol.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Cholesterol.Experimental
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Cholesterol.Approved, Illicit
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Cholesterol.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Cholesterol.Approved
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Cholesterol.Approved, Withdrawn
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Cholesterol.Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Cholesterol.Experimental, Investigational
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Cholesterol.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Cholesterol.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Cholesterol.Approved, Vet Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Cholesterol.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Cholesterol.Experimental
PethidineThe risk or severity of adverse effects can be increased when Cholesterol is combined with Pethidine.Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Cholesterol.Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Cholesterol.Experimental
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Cholesterol.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Cholesterol.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Cholesterol.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Cholesterol.Approved, Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Cholesterol.Approved
RolapitantThe serum concentration of Cholesterol can be increased when it is combined with Rolapitant.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Cholesterol.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Cholesterol.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Cholesterol.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Cholesterol.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Cholesterol.Approved
St. John's WortThe metabolism of Cholesterol can be increased when combined with St. John's Wort.Investigational, Nutraceutical
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Cholesterol.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Cholesterol.Approved, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Cholesterol is combined with Temsirolimus.Approved
TeriflunomideThe serum concentration of Cholesterol can be increased when it is combined with Teriflunomide.Approved
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Cholesterol.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Cholesterol.Approved, Investigational
TipranavirThe serum concentration of Cholesterol can be decreased when it is combined with Tipranavir.Approved, Investigational
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Cholesterol.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Cholesterol.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Cholesterol.Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Cholesterol.Approved
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Cholesterol.Approved, Investigational
VerapamilThe metabolism of Verapamil can be decreased when combined with Cholesterol.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Cholesterol.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Cholesterol.Approved
Food Interactions
Not Available

References

Synthesis Reference

Tatu Miettenen, Ingmar Wester, Hannu Vanhanen, "Substance for lowering high cholesterol level in serum and methods for preparing and using the same." U.S. Patent US6174560, issued February, 1944.

US6174560
General References
Not Available
External Links
Human Metabolome Database
HMDB62453
KEGG Drug
D00040
KEGG Compound
C00187
PubChem Compound
5997
PubChem Substance
46508234
ChemSpider
5775
BindingDB
20192
ChEBI
16113
ChEMBL
CHEMBL112570
HET
CLR
PDB Entries
1lri / 1n83 / 1zhy / 2rh1 / 2zxe / 3a3y / 3am6 / 3d4s / 3gki / 3jd8
show 100 more

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionCardiovascular Disease (CVD) / Carotid Atherosclerosis / Diabetes / Hyperlipidemias / Hypertensive1
Not AvailableRecruitingTreatmentCone-Rod Dystrophy / Hard of Hearing / Smith-Lemli-Opitz Syndrome1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)148.5 °CPhysProp
boiling point (°C)360 °CPhysProp
water solubility0.095 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
Predicted Properties
PropertyValueSource
Water Solubility2.79e-05 mg/mLALOGPS
logP7.02ALOGPS
logP7.11ChemAxon
logS-7.1ALOGPS
pKa (Strongest Acidic)18.2ChemAxon
pKa (Strongest Basic)-1.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area20.23 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity120.62 m3·mol-1ChemAxon
Polarizability50.6 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9749
Caco-2 permeable+0.8184
P-glycoprotein substrateSubstrate0.6477
P-glycoprotein inhibitor IInhibitor0.6404
P-glycoprotein inhibitor IINon-inhibitor0.529
Renal organic cation transporterNon-inhibitor0.7691
CYP450 2C9 substrateNon-substrate0.8257
CYP450 2D6 substrateNon-substrate0.8794
CYP450 3A4 substrateSubstrate0.7439
CYP450 1A2 substrateNon-inhibitor0.9355
CYP450 2C9 inhibitorNon-inhibitor0.9194
CYP450 2D6 inhibitorNon-inhibitor0.9519
CYP450 2C19 inhibitorNon-inhibitor0.9177
CYP450 3A4 inhibitorNon-inhibitor0.8638
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6721
Ames testNon AMES toxic0.8888
CarcinogenicityNon-carcinogens0.932
BiodegradationNot ready biodegradable0.9825
Rat acute toxicity2.8078 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.773
hERG inhibition (predictor II)Non-inhibitor0.7552
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-MS (1 TMS)GC-MSsplash10-004i-3911000000-52f5261007adc218f8f8
GC-MS Spectrum - EI-BGC-MSsplash10-052b-2932000000-1667c83d002043a59fff
GC-MS Spectrum - EI-BGC-MSsplash10-000l-9527000000-5529a262047f5369c9c1
GC-MS Spectrum - EI-BGC-MSsplash10-0mkr-2954000000-60e7d1f5973e4de33dec
GC-MS Spectrum - CI-BGC-MSsplash10-014i-1009000000-e82b8e23dedb45ce70e6
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-056v-2900000000-04687c9f19ff52ba4654
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0a4l-7922000000-36e8a5e1a77d2e71d1d1
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as cholesterols and derivatives. These are compounds containing a 3-hydroxylated cholestane core.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Cholestane steroids
Direct Parent
Cholesterols and derivatives
Alternative Parents
3-beta-hydroxysteroids / 3-beta-hydroxy delta-5-steroids / Delta-5-steroids / Secondary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
Substituents
Cholesterol-skeleton / Cholesterol / 3-beta-hydroxysteroid / 3-beta-hydroxy-delta-5-steroid / Hydroxysteroid / 3-hydroxysteroid / 3-hydroxy-delta-5-steroid / Delta-5-steroid / Cyclic alcohol / Secondary alcohol
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
cholestanoid, 3beta-sterol (CHEBI:16113) / cholestane, Cholesterol and derivatives, Cholestane and derivatives (C00187) / Cholesterol and derivatives (LMST01010001)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds DNA as a monomer to ROR response elements (RORE) containing a single core motif half-site 5'-AGGTCA-3' preceded by a short A-T-rich sequence. Key regulator of embryonic ...
Gene Name
RORA
Uniprot ID
P35398
Uniprot Name
Nuclear receptor ROR-alpha
Molecular Weight
58974.35 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. 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
Zinc ion binding
Specific Function
Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes. Transactivates both the phenobarbital re...
Gene Name
NR1I3
Uniprot ID
Q14994
Uniprot Name
Nuclear receptor subfamily 1 group I member 3
Molecular Weight
39942.145 Da
References
  1. Mooijaart SP, Brandt BW, Baldal EA, Pijpe J, Kuningas M, Beekman M, Zwaan BJ, Slagboom PE, Westendorp RG, van Heemst D: C. elegans DAF-12, Nuclear Hormone Receptors and human longevity and disease at old age. Ageing Res Rev. 2005 Aug;4(3):351-71. [PubMed:16051528]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Recruited to promoters via its interaction with BAZ1B...
Gene Name
VDR
Uniprot ID
P11473
Uniprot Name
Vitamin D3 receptor
Molecular Weight
48288.64 Da
References
  1. Mooijaart SP, Brandt BW, Baldal EA, Pijpe J, Kuningas M, Beekman M, Zwaan BJ, Slagboom PE, Westendorp RG, van Heemst D: C. elegans DAF-12, Nuclear Hormone Receptors and human longevity and disease at old age. Ageing Res Rev. 2005 Aug;4(3):351-71. [PubMed:16051528]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Ligand
General Function
C-type lectin that functions as cell-surface receptor for a wide variety of ligands such as damaged cells, fungi and mycobacteria. Plays a role in the recognition of pathogenic fungi, such as Candida albicans. The detection of mycobacteria is via trehalose 6,6'-dimycolate (TDM), a cell wall glycolipid. Specifically recognizes alpha-mannose residues on pathogenic fungi of the genus Malassezia. Recognizes also SAP130, a nuclear protein, that is released by dead or dying cells. Transduces signals through an ITAM-containing adapter protein, Fc receptor gamma chain /FCER1G. Induces secretion of inflammatory cytokines through a pathway that depends on SYK, CARD9 and NF-kappa-B.
Specific Function
Carbohydrate binding
Gene Name
CLEC4E
Uniprot ID
Q9ULY5
Uniprot Name
C-type lectin domain family 4 member E
Molecular Weight
25072.31 Da
References
  1. Kiyotake R, Oh-Hora M, Ishikawa E, Miyamoto T, Ishibashi T, Yamasaki S: Human Mincle Binds to Cholesterol Crystals and Triggers Innate Immune Responses. J Biol Chem. 2015 Oct 16;290(42):25322-32. doi: 10.1074/jbc.M115.645234. Epub 2015 Aug 20. [PubMed:26296894]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Wang E, Casciano CN, Clement RP, Johnson WW: Cholesterol interaction with the daunorubicin binding site of P-glycoprotein. Biochem Biophys Res Commun. 2000 Oct 5;276(3):909-16. [PubMed:11027568]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Janvilisri T, Venter H, Shahi S, Reuter G, Balakrishnan L, van Veen HW: Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51. Epub 2003 Mar 28. [PubMed:12668685]

Drug created on June 13, 2005 07:24 / Updated on November 09, 2017 03:43