ArticleACS omega2019
Establishing Drug Discovery and Identification of Hit Series for the Anti-apoptotic Proteins, Bcl-2 and Mcl-1.
Article in ACS omega, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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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.
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Who cites it
25 citing papers in PubMed, 68 citations in OpenAlex.
- Structure-Based Discovery of Potent BCL-XL Inhibitors through Rescaffolding.Journal of medicinal chemistry · 2026Article
- What does BCL-2 do? From new molecular insights to the clinical implications.Cell death and differentiation · 2026Review
- Revealing the Binding Mechanism of Gossypol on Bcl‑2 via Funnel Metadynamics Simulations.ACS omega · 2026Article
- Quinoline and coumarin isoxazole derivatives: synthesis, antitumor evaluation and molecular docking studies with Bcl-2.RSC advances · 2025Article
- Identification of chrysin derivatives anticancer potential in MCF7 cells: biological insights and in silico evaluation.Future medicinal chemistry · 2025Article
- Deciphering molecular specificity in MCL-1/BAK interaction and its implications for designing potent MCL-1 inhibitors.Cell death and differentiation · 2025Article
- Structural basis of BAK sequestration by MCL-1 in apoptosis.Molecular cell · 2025Article
- Examination of Triazolinedione-Derived Dihydropyrrole Hybrid Compounds: ER Stress-Related Apoptosis in Breast Cancer Cells, Molecular Docking, and ADMET Analysis.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Article
- The landscape of programmed cell death-related lncRNAs in Alzheimer's disease and Parkinson's disease.Apoptosis : an international journal on programmed cell death · 2024Article
- Development and crystal structures of a potent second-generation dual degrader of BCL-2 and BCL-xL.Nature communications · 2024Article
- In silico design of potential Mcl-1 peptide-based inhibitors.Journal of molecular modeling · 2024Article
- Cyclic peptides discriminate BCL-2 and its clinical mutants from BCL-XNature communications · 2024Article
- Structural insights for selective disruption of Beclin 1 binding to Bcl-2.Communications biology · 2023Article
- In silico design and cell-based evaluation of two dual anti breast cancer compounds targeting Bcl-2 and GPER.Scientific reports · 2023Article
- Structures of p53/BCL-2 complex suggest a mechanism for p53 to antagonize BCL-2 activity.Nature communications · 2023Article
- Discovering small-molecule senolytics with deep neural networks.Nature aging · 2023Article
- Structural basis of the specificity and interaction mechanism of Bmf binding to pro-survival Bcl-2 family proteins.Computational and structural biotechnology journal · 2023Article
- New pyrimidine-N-β-D-glucosides: synthesis, biological evaluation, and molecular docking investigations.Turkish journal of chemistry · 2023Article
- Understanding MCL1: from cellular function and regulation to pharmacological inhibition.The FEBS journal · 2022Review
- Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins.Expert opinion on therapeutic patents · 2022Review
Corrections and comments
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Authors and funding
24 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We describe our work to establish structure- and fragment-based drug discovery to identify small molecules that inhibit the anti-apoptotic activity of the proteins Mcl-1 and Bcl-2. This identified hit series of compounds, some of which were subsequently optimized to clinical candidates in trials for treating various cancers. Many protein constructs were designed to identify protein with suitable properties for different biophysical assays and structural methods. Fragment screening using ligand-observed NMR experiments identified several series of compounds for each protein. The series were assessed for their potential for subsequent optimization using
Identifiers
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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.