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Protein / target

Cytochrome P450 7A1

Encoded byCYP7A1P22680Homo sapiensSwiss-Prot
Small-molecule tractable
Druggability
Structure with Ligand
1
Research papers

Protein at a glance

Biological role

24S-hydroxycholesterol 7-alpha-hydroxylase

Strongest disease association

Cholelithiasis

Via encoding gene CYP7A1 · Genetic evidence · score 0.90

Research activity

Emerging research

1 papers · latest 2024

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function overview

A cytochrome P450 monooxygenase involved in the metabolism of endogenous cholesterol and its oxygenated derivatives (oxysterols).

View complete UniProt function annotation

A cytochrome P450 monooxygenase involved in the metabolism of endogenous cholesterol and its oxygenated derivatives (oxysterols) (PubMed:11013305, PubMed:12077124, PubMed:19965590, PubMed:21813643, PubMed:2384150). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed:11013305, PubMed:12077124, PubMed:19965590, PubMed:21813643, PubMed:2384150). Functions as a critical regulatory enzyme of bile acid biosynthesis and cholesterol homeostasis. Catalyzes the hydroxylation of carbon hydrogen bond at 7-alpha position of cholesterol, a rate-limiting step in cholesterol catabolism and bile acid biosynthesis (PubMed:12077124, PubMed:19965590, PubMed:2384150). 7-alpha hydroxylates several oxysterols, including 4beta-hydroxycholesterol and 24-hydroxycholesterol (PubMed:11013305, PubMed:12077124). Catalyzes the oxidation of the 7,8 double bond of 7-dehydrocholesterol and lathosterol with direct and predominant formation of the 7-keto derivatives (PubMed:21813643)

Subcellular location

Endoplasmic reticulum membraneMicrosome membrane
Domains and Gene Ontology detail (17)

Gene Ontology

  • Cendoplasmic reticulum membrane
  • Cintracellular membrane-bounded organelle
  • F24S-hydroxycholesterol 7-alpha-hydroxylase activity
  • Fcholesterol 7-alpha-monooxygenase activity
  • Fheme binding
  • Firon ion binding
  • Pbile acid biosynthetic process
  • Pcellular response to cholesterol
  • Pcellular response to glucose stimulus
  • Pcholesterol catabolic process
  • Pcholesterol homeostasis
  • Pnegative regulation of collagen biosynthetic process

504 aa · 58 kDa

Biological roles

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Lipid & lipoprotein metabolismUniProt · GO
View supporting evidence

Lipid & lipoprotein metabolism

  • ·A cytochrome P450 monooxygenase involved in the metabolism of endogenous cholesterol and…
  • ·24S-hydroxycholesterol 7-alpha-hydroxylase activity
  • ·cholesterol 7-alpha-monooxygenase activity
  • ·cellular response to cholesterol

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene CYP7A1

Gene-level evidence surfaced through the gene CYP7A1 that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Cholelithiasis
0.91Well supported

Genetic evidence dominant · Open Targets 0.55

Metabolic Diseases
0.85Well supported

Genetic evidence dominant · Open Targets 0.52

Hyperlipidemias
0.77Well supported

Genetic evidence dominant · Open Targets 0.47

Gallstones
0.74Moderately supported

Genetic evidence dominant · Open Targets 0.46

View evidence synthesis (4)
CholelithiasisWell supported
0.91
agreement 0.771.00
Genetic98%Literature2%

Open Targets aggregate 0.55 · 2 independent evidence families

Metabolic DiseasesWell supported
0.85
agreement 0.710.99
Genetic99%Literature1%

Open Targets aggregate 0.52 · 2 independent evidence families

HyperlipidemiasWell supported
0.77
agreement 0.630.91
Genetic97%Literature3%

Open Targets aggregate 0.47 · 2 independent evidence families

GallstonesModerately supported
0.74
agreement 0.610.88
Genetic93%Literature7%

Open Targets aggregate 0.46 · 2 independent evidence families

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.

Show all associations
Cholelithiasis0.55
Metabolic Diseases0.52
Hyperlipidemias0.47
Gallstones0.46

Tractability

Small moleculesEmerging

Feasibility evidence (structure with ligand and high-quality pocket) — no clinical-stage drug of this modality recorded.

AntibodiesEmerging

Feasibility evidence (uniprot sigp or tmhmm) — no clinical-stage drug of this modality recorded.

Protein degradersEmerging

Feasibility evidence (small molecule binder) — no clinical-stage drug of this modality recorded.

View underlying tractability evidence (4)
SM · Structure with LigandSM · High-Quality PocketAB · UniProt SigP or TMHMMPR · Small Molecule Binder

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

regulation of transcription factor activityToxCast

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

Research activity

1 papers · to 2024

Papers linked directly to this protein. This is the protein's own literature — descriptor-derived papers are kept separate below.

Most cited

Recent

Europe PMC papers linked directly to this protein.