ArticleThe Journal of biological chemistry2019
Structure of human cortisol-producing cytochrome P450 11B1 bound to the breast cancer drug fadrozole provides insights for drug design.
Article in The Journal of biological chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
26 citing papers in PubMed, 42 citations in OpenAlex.
- Visualization of relative 11β-hydroxylase (CYP11B1) activity in human cortisol-producing adrenocortical adenoma (CPA) using mass spectrometry imaging-based enzyme histochemistry.Analytical and bioanalytical chemistry · 2026Article
- Aldosterone Synthase Inhibitors: Emerging Therapeutic Strategies in Resistant Hypertension.Life (Basel, Switzerland) · 2026Review
- Evaluation of AlphaFold3 for Predicting Human Heme-Binding Protein Structures.International journal of molecular sciences · 2026Article
- The regulatory potential of cytochrome P450-adrenodoxin interactions: Insights toward understanding redox partner regulation in drug metabolizing enzymes.Drug metabolism and disposition: the biological fate of chemicals · 2026Review
- From target specificity to metabolic efficiency: Design and optimization of etomidate analogues for potential improvement in postoperative outcomes.Acta pharmaceutica Sinica. B · 2026Article
- Mycobacteriumabscessus CYP123 is a steroid hydroxylase with an implication in host infection.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Development of Highly Selective Aldosterone Synthase Inhibitors.ACS medicinal chemistry letters · 2025Article
- Cytochrome P450 Enzymes as Drug Targets in Human Disease.Drug metabolism and disposition: the biological fate of chemicals · 2024Review
- Kinetics of Intermediate Release Enhances P450 11B2-Catalyzed Aldosterone Synthesis.Biochemistry · 2024Article
- Exploring the anticancer and antibacterial potential of naphthoquinone derivatives: a comprehensive computational investigation.Frontiers in chemistry · 2024Article
- Discovery of a Potent Dual Inhibitor of Aromatase and Aldosterone Synthase.ACS pharmacology & translational science · 2023Article
- Selectivity of osilodrostat as an inhibitor of human steroidogenic cytochromes P450.The Journal of steroid biochemistry and molecular biology · 2023Article
- Recombinant Technologies Facilitate Drug Metabolism, Pharmacokinetics, and General Biomedical Research.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- Generation of human steroidogenic cytochrome P450 enzymes for structural and functional characterization.Methods in enzymology · 2023Article
- Four Decades of Cytochrome P450 2B Research: From Protein Adducts to Protein Structures and Beyond.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- Redox partner adrenodoxin alters cytochrome P450 11B1 ligand binding and inhibition.Journal of inorganic biochemistry · 2022Article
- Hexaconazole exposure ravages biosynthesis pathway of steroid hormones: revealed by molecular dynamics and interaction.Toxicology research · 2022Article
- Characterization of a Cleavable Fusion of Human CYP24A1 with Adrenodoxin Reveals the Variable Role of Hydrophobics in Redox Partner Binding.Biochemistry · 2022Article
- Diverse reactions catalyzed by cytochrome P450 and biosynthesis of steroid hormone.Biophysics and physicobiology · 2022Article
- Atractylenolide-I covalently binds to CYP11B2, selectively inhibits aldosterone synthesis, and improves hyperaldosteronism.Acta pharmaceutica Sinica. B · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 2 countries.
Funding
Abstract
Human cytochrome P450 11B1 (CYP11B1) is responsible for the final step generating the steroid hormone cortisol, which controls stress and immune responses and glucose homeostasis. CYP11B1 is a promising drug target to manage Cushing's disease, a disorder arising from excessive cortisol production. However, the design of selective inhibitors has been hampered because structural information for CYP11B1 is unavailable and the enzyme has high amino acid sequence identity (93%) to a closely related enzyme, the aldosterone-producing CYP11B2. Here we report the X-ray crystal structure of human CYP11B1 (at 2.1 Å resolution) in complex with fadrozole, a racemic compound normally used to treat breast cancer by inhibiting estrogen-producing CYP19A1. Comparison of fadrozole-bound CYP11B1 with fadrozole-bound CYP11B2 revealed that despite conservation of the active-site residues, the overall structures and active sites had structural rearrangements consistent with distinct protein functions and inhibition. Whereas fadrozole binds to both CYP11B enzymes by coordinating the heme iron, CYP11B2 binds to the
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.