ReviewJournal of medicinal chemistry2016
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.
Review in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
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
24 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Adjuvant endocrine therapy and risk of contralateral breast cancer: a systematic review and meta-analysis of observational studies.Cancer causes & control : CCC · 2025Pooled it
- Aromatase inhibitors induce pain-like musculoskeletal symptoms in mice: behavioural, pharmacological and pathophysiological characterization.British journal of pharmacology · 2026Article
- Integrated Virtual Screening Approach Identifies New CYP19A1 Inhibitors.Journal of chemical information and modeling · 2025Article
- Roles of Ferric Peroxide Anion Intermediates (FeAngewandte Chemie (International ed. in English) · 2024Article
- Structure-Activity Relationship Study of Tris-Benzamides as Estrogen Receptor Coregulator Binding Modulators.ACS pharmacology & translational science · 2024Article
- New 1,2,3-Triazole/1,2,4-triazole Hybrids as Aromatase Inhibitors: Design, Synthesis, and Apoptotic Antiproliferative Activity.Molecules (Basel, Switzerland) · 2023Article
- A Theoretical Study of Organotin Binding in Aromatase.International journal of molecular sciences · 2023Article
- Pyridine based dual binding site aromatase (CYP19A1) inhibitors.RSC medicinal chemistry · 2023Article
- Adrenal Steroids and Resistance to Hormonal Blockade of Prostate and Breast Cancer.Endocrinology · 2023Review
- Targeting allosteric sites of human aromatase: a comprehensiveJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Coumarins as Tool Compounds to Aid the Discovery of Selective Function Modulators of Steroid Hormone Binding Proteins.Molecules (Basel, Switzerland) · 2021Review
- 19-hydroxy Steroids in the Aromatase Reaction: Review on Expression and Potential Functions.Journal of the Endocrine Society · 2021Review
- Frontiers of metal-coordinating drug design.Expert opinion on drug discovery · 2021Review
- Estrogen disorders: Interpreting the abnormal regulation of aromatase in granulosa cells (Review).International journal of molecular medicine · 2021Review
- Aromatase Inhibitor-Associated Musculoskeletal Syndrome: Understanding Mechanisms and Management.Frontiers in endocrinology · 2021Review
- Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides.ACS medicinal chemistry letters · 2020Article
- Reconsidering Aromatase for Breast Cancer Treatment: New Roles for an Old Target.Molecules (Basel, Switzerland) · 2020Review
- Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors.ACS medicinal chemistry letters · 2020Article
- Review
- Phosphorylation of human placental aromatase CYP19A1.The Biochemical journal · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors.
Funding
Abstract
Human aromatase catalyzes the synthesis of estrogen from androgen with high substrate specificity. For the past 40 years, aromatase has been a target of intense inhibitor discovery research for the prevention and treatment of estrogen-dependent breast cancer. The so-called third generation aromatase inhibitors (AIs) letrozole, anastrozole, and the steroidal exemestane were approved in the U.S. in the late 1990s for estrogen-dependent postmenopausal breast cancer. Efforts to develop better AIs with higher selectivity and lower side effects were handicapped by the lack of an experimental structure of this unique P450. The year 2009 marked the publication of the crystal structure of aromatase purified from human placenta, revealing an androgen-specific active site. The structure has reinvigorated research activities on this fascinating enzyme and served as the catalyst for next generation AI discovery research. Here, we present an account of recent developments in the AI field from the perspective of the enzyme's structure-function relationships.
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.