Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTSYVO6)

• DTT Name: Cholesterol desmolase (CYP11A1)
• Synonyms: P450(scc); Cytochrome P450(scc); Cytochrome P450 11A1; Cholesterol side-chain cleavage enzyme, mitochondrial; CYPXIA1; CYP11A
• Gene Name: CYP11A1
• DTT Type: Successful target; [1]
• BioChemical Class: Paired donor oxygen oxidoreductase
• UniProt ID: CP11A_HUMAN
• TTD ID: T23145
• EC Number: EC 1.14.15.6
• Sequence:
  MLAKGLPPRSVLVKGCQTFLSAPREGLGRLRVPTGEGAGISTRSPRPFNEIPSPGDNGWL
  NLYHFWRETGTHKVHLHHVQNFQKYGPIYREKLGNVESVYVIDPEDVALLFKSEGPNPER
  FLIPPWVAYHQYYQRPIGVLLKKSAAWKKDRVALNQEVMAPEATKNFLPLLDAVSRDFVS
  VLHRRIKKAGSGNYSGDISDDLFRFAFESITNVIFGERQGMLEEVVNPEAQRFIDAIYQM
  FHTSVPMLNLPPDLFRLFRTKTWKDHVAAWDVIFSKADIYTQNFYWELRQKGSVHHDYRG
  ILYRLLGDSKMSFEDIKANVTEMLAGGVDTTSMTLQWHLYEMARNLKVQDMLRAEVLAAR
  HQAQGDMATMLQLVPLLKASIKETLRLHPISVTLQRYLVNDLVLRDYMIPAKTLVQVAIY
  ALGREPTFFFDPENFDPTRWLSKDKNITYFRNLGFGWGVRQCLGRRIAELEMTIFLINML
  ENFRVEIQHLSDVGTTFNLILMPEKPISFTFWPFNQEATQQ
• Function: Catalyzes the side-chain cleavage reaction of cholesterol to pregnenolone, the precursor of most steroid hormones.
• KEGG Pathway:
  Steroid hormone biosynthesis (hsa00140)
  Metabolic pathways (hsa01100)
  Ovarian steroidogenesis (hsa04913)
• Reactome Pathway: Endogenous sterols (R-HSA-211976)
• BioCyc Pathway: MetaCyc:HS06719-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aminoglutethimide	DMWFHMZ	Cushing disease	5A70	Approved	[1]

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MK-5684	DMU93NS	Prostate cancer	2C82.0	Phase 1/2	[2]

2 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3-(4-Amino-phenyl)-3-butyl-piperidine-2,6-dione	DMD5YKO	Discovery agent	N.A.	Investigative	[3]
3-(4-Amino-phenyl)-3-pentyl-piperidine-2,6-dione	DM20DXS	Discovery agent	N.A.	Investigative	[3]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Breast cancer	2C82	Breast tissue	1.09E-47	-0.41	-1.12

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: Cholesterol desmolase (CYP11A1) DME Info
• Gene Name: CYP11A1

2 Approved Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ergocalciferol	DMHO0AR	Hypoparathyroidism	5A50	Approved	[4]
Vitamin D	DMWQUC9	N. A.	N. A.	Approved	[5]

1 Clinical Trial Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ANW-32821	DMMJOZD	N. A.	N. A.	Phase 2	[6]

References

• [1] Breakdown of Th cell immune responses and steroidogenic CYP11A1 expression in CD4+ T cells in a murine model implanted with B16 melanoma. Cell Immunol. 2000 Nov 25;206(1):7-15.
• [2] Clinical pipeline report, company report or official report of Merck
• [3] Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones. J Med Chem. 1986 Aug;29(8):1362-9.
• [4] Vitamin D: mechanisms of action and clinical applications. Endocrinol Metab Clin North Am. 2017 Dec;46(4):xvii-xviii.
• [5] Metabolism of 1alpha-hydroxyvitamin D3 by cytochrome P450scc to biologically active 1alpha,20-dihydroxyvitamin D3. J Steroid Biochem Mol Biol. 2008 Dec;112(4-5):213-9.
• [6] Cholesterol-metabolizing cytochromes P450. Drug Metab Dispos. 2006 Apr;34(4):513-20.