Protein / target
Lanosterol 14-alpha demethylase
Protein at a glance
Biological role
Sterol 14-demethylase
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Sterol 14alpha-demethylase that plays a critical role in the third module of ergosterol biosynthesis pathway, being ergosterol the major sterol component in fungal membranes that participates in a variety of functions.
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Sterol 14alpha-demethylase that plays a critical role in the third module of ergosterol biosynthesis pathway, being ergosterol the major sterol component in fungal membranes that participates in a variety of functions (PubMed:10393548, PubMed:28258218, PubMed:8647850, PubMed:9559662). The third module or late pathway involves the ergosterol synthesis itself through consecutive reactions that mainly occur in the endoplasmic reticulum (ER) membrane (By similarity). In filamentous fungi, during the initial step of this module, lanosterol (lanosta-8,24-dien-3beta-ol) can be metabolized to eburicol (By similarity). Sterol 14alpha-demethylase catalyzes the three-step oxidative removal of the 14alpha-methyl group (C-32) of both these sterols in the form of formate, and converts eburicol and lanosterol to 14-demethyleburicol (4,4,24-trimethylergosta-8,14,24(28)-trienol) and 4,4-dimethyl-5alpha-cholesta-8,14,24-trien-3beta-ol, respectively, which are further metabolized by other enzymes in the pathway to ergosterol (PubMed:10393548, PubMed:28258218, PubMed:8647850, PubMed:9559662). Can also use substrates not intrinsic to fungi, such as 24,25-dihydrolanosterol (DHL), producing 4,4-dimethyl-8,14-cholestadien-3-beta-ol, but at lower rates than the endogenous substrates (By similarity)
Subcellular location
Domains and Gene Ontology detail (14)Hide
Gene Ontology
- Ccortical endoplasmic reticulum
- Cendoplasmic reticulum membrane
- Cmembrane
- Cperinuclear endoplasmic reticulum
- Cplasma membrane
- Fheme binding
- Firon ion binding
- Foxidoreductase activity
- Fsterol 14-demethylase activity
- Pcell growth mode switching, budding to filamentous
- Pcellular response to xenobiotic stimulus
- Pendosome organization
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Lipid & lipoprotein metabolism
- ·Sterol 14alpha-demethylase that plays a critical role in the third module of ergosterol…
- ·sterol 14-demethylase activity
- ·ergosterol biosynthetic process
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Cytochrome P450 51 inhibitor
Indicated for Aspergillosis, Candidemia, Candidiasis, Infections
Cytochrome P450 51 inhibitor
Indicated for Candidiasis, Candidiasis, Vulvovaginal, Urinary Tract Infections
Cytochrome P450 51 inhibitor
Indicated for Aspergillosis, Candidiasis, Lung Diseases, Mycoses
Cytochrome P450 51 inhibitor
Indicated for Infections, Mycoses, Pruritus, Tinea
Cytochrome P450 51 inhibitor
Indicated for Aspergillosis, Candidiasis, Mycoses, Neutropenia
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 5 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Label change
Label change: ITRACONAZOLE (ANDA205080)
- Label change
Label change: ITRACONAZOLE (ANDA206741)
- Label change
Label change: ITRACONAZOLE (ANDA208481)
- Trial status changed
An Open-label, Phase 1 Study to Individually Characterize the Food Effect, the Drug-Drug Interaction Effect of OAT Inhibition, and the Drug-Drug Interaction Effect of P-glycoprotein Inhibition on the Pharmacokinetics of MK-8527 in Healthy Adult Participants
- Trial status changed
A Phase 1 Crossover Design Study to Assess the Effect of CYP3A Moderate and Strong Inhibitors (Fluconazole and Itraconazole) and Strong Inducer (Carbamazepine) on the Single-dose Pharmacokinetics of ASP3082 in Healthy Adults
- Trial status changed
A Phase 1, Open-Label, Fixed-Sequence Study to Investigate the Effect of Itraconazole on the Pharmacokinetics of LY4395089 in Healthy Participants
- Trial status changed
A Two-Part Clinical Study to Evaluate the Effects of Multiple Doses of Itraconazole on the Single-Dose Pharmacokinetics of MK-2828 (Part 1) and Multiple Doses of MK-2828 on the Single-Dose PK of Midazolam (Part 2) in Healthy Participants
- Regulatory approval
Approval: POSACONAZOLE (ANDA213331)
- New publicationDefining and managing COVID-19-associated pulmonary aspergillosis: the 2020 ECMM/ISHAM consensus criteria for research and clinical guidance.
- Safety communication
Drug Safety Update: Miconazole (Daktarin): over-the-counter oral gel contraindicated in patients taking warfarin
- Safety communication
Drug Safety Update: Posaconazole (Noxafil): tablets and oral suspension are not directly interchangeable
- Safety communication
Drug Safety Update: Voriconazole: reminder of risk of liver toxicity, phototoxicity, and squamous cell carcinoma
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.