145 articles for thisTarget
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Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors.
Shandong University
Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
Shandong University
Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.
China Pharmaceutical University
Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity.
Second Military Medical University
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
Astrazeneca
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Vanderbilt University School of Medicine
Peptide-based inhibitors of protein-protein interactions.
Wroclaw University of Technology
Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors.
Shandong University
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.
Shandong University
Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Abbvie
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.
University of Naples Federico II
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.
Shandong University
A combination of in silico and SAR studies to identify binding hot spots of Bcl-xL inhibitors.
Bioprojet-Biotech
A simple and widely applicable hit validation strategy for protein-protein interaction inhibitors based on a quantitative ligand displacement assay.
Takeda Pharmaceutical
Endiandric acid analogues from Beilschmiedia ferruginea as dual inhibitors of Bcl-xL/Bak and Mcl-1/Bid interactions.
Institut De Chimie Des Substances Naturelles (Icsn)
3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.
University of Michigan Medical School
Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker.
Eutropics Pharmaceuticals
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
The Walter and Eliza Hall Institute of Medical Research
Novel soluble myeloid cell leukemia sequence 1 (Mcl-1) inhibitor (E,E)-2-(benzylaminocarbonyl)-3-styrylacrylonitrile (4g) developed using a fragment-based approach.
Dalian University of Technology
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Novartis Institutes For Biomedical Research
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.
Dalian University of Technology
3D-QSAR pharmacophore modeling and in silico screening of new Bcl-xl inhibitors.
University of Palermo
Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.
Clermont Universit£
Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity.
University of Michigan
Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold.
University of Michigan
Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.
Bristol-Myers Squibb Research
Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.
Bristol-Myers Squibb Research
Unbiased binding assays for discovering small-molecule probes and drugs.
Broad Institute of Harvard and Mit
BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Sanford-Burnham Medical Research Institute
Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues.
University of Minnesota
Discovery, characterization, and structure-activity relationships studies of proapoptotic polyphenols targeting B-cell lymphocyte/leukemia-2 proteins.
Institute
Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity.
Second Military Medical University
Biochemical and pharmacological profiling of the pro-survival protein Bcl-xL.
University of Washington
SAR by interligand nuclear overhauser effects (ILOEs) based discovery of acylsulfonamide compounds active against Bcl-x(L) and Mcl-1.
Sanford-Burnham Medical Research Institute
Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
The Walter and Eliza Hall Institute of Medical Research
Anti-tumor pyrimidinylpiperazines bind to the prosurvival Bcl-2 protein family member Bcl-XL.
University of The Pacific
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Sanford-Burnham Medical Research Institute
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University of Thessaloniki
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Abbott Laboratories
Rearranged diterpenoids from the biotransformation of ent-trachyloban-18-oic acid by Rhizopus arrhizus.
Centre De Recherche De Gif
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Chinese Academy of Sciences
Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention.
Institute For Medical Research
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.
Institute of Chemical and Engineering Sciences
Cytotoxic pentacyclic triterpenoids from Combretum sundaicum and Lantana camara as inhibitors of Bcl-xL/BakBH3 domain peptide interaction.
Cnrs
A Dimeric sesquiterpenoid from a Malaysian Meiogyne as a new inhibitor of Bcl-xL/BakBH3 domain peptide interaction.
Cnrs
Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl.
Merlion Pharmaceuticals
Diversity-oriented synthesis of a cytisine-inspired pyridone library leading to the discovery of novel inhibitors of Bcl-2.
Infinity Pharmaceuticals
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement.
University of Montpellier
Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy.
AbbVie Inc.
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
AstraZeneca
Discovery of Novel Mcl-1 Inhibitors with a 3-Substituted-1H-indole-1-yl Moiety Binding to the P1-P3 Pockets to Induce Apoptosis in Acute Myeloid Leukemia Cells.
Shenyang Pharmaceutical University
Rational design of small-sized peptidomimetic inhibitors disrupting protein-protein interaction.
Ningxia Medical University
Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors.
Vanderbilt University School of Medicine
Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen.
AstraZeneca
Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.
Symeres
Discovery of the Clinical Candidate Sonrotoclax (BGB-11417), a Highly Potent and Selective Inhibitor for Both WT and G101V Mutant Bcl-2.
BeiGene(Beiing) Co., Ltd.
Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.
Shenyang Pharmaceutical University
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
University of Chinese Academy of Sciences
Targeting the Inhibition of B-Cell Lymphoma 2 Protein for the Treatment of Cancer.
Therachem Research Medilab
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor.
Tianjin University
Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.
University of Minnesota
Inhibitors of BCL2A1/Bfl-1 protein: Potential stock in cancer therapy.
China Pharmaceutical University
Single and dual target inhibitors based on Bcl-2: Promising anti-tumor agents for cancer therapy.
Shandong First Medical University & Shandong Academy of Medical Sciences
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University of Michigan
Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells.
Yancheng Teachers University
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Abbott Laboratories
Development of Mcl-1 inhibitors for cancer therapy.
National University of Ireland Galway
Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.
Shenyang Pharmaceutical University
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.
University of Maryland
Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein.
Yale University
Discovery of potent and selective Bcl-2 inhibitors with acyl sulfonamide skeleton.
Shanghai Institute of Pharmaceutical Industry
Design, synthesis and biological evaluation of dual Bcl-2/Mcl-1 inhibitors bearing 2-(1H-indol-4-yl)benzoic acid scaffold.
Shenyang Pharmaceutical University
Targeting the Allosteric Pathway That Interconnects the Core-Functional Scaffold and the Distal Phosphorylation Sites for Specific Dephosphorylation of Bcl-2.
Dalian University of Technology
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Xihua University
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
Shandong University
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.
Paris-Saclay University
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
University of Naples "Federico Ii
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Vanderbilt University School of Medicine
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Servier Research Institute of Medicinal Chemistry
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
TBA
Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.
National Institute of Chemistry
Clinical candidates modulating protein-protein interactions: The fragment-based experience.
Taros Chemicals
Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors.
Shandong University
Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors.
Shandong University
Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein.
Soochow University
Identification of lead compounds as antagonists of protein Bcl-xL with a diversity-oriented multidisciplinary approach.
Universita Degli Studi Di Salerno
Development of high potent and selective Bcl-2 inhibitors bearing the structural elements of natural product artemisinin.
Shanghai Institute of Materia Medica (Simm)
Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection.
Abbvie
Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors.
Shanghai Institute of Materia Medica (Simm)
Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A.
Paris-Saclay University
Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.
University of Maryland
1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation.
Shandong University
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.
Vanderbilt University School of Medicine
THERAPY BASED ON SYNTHETIC LETHALITY IN SWI/SNF COMPLEX-DYSFUNCTION CANCER
National Cancer Center
Isoindoline compositions and methods for treating neurodegenerative disease
Cognition Therapeutics
Heteroaryl[4,3-C]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
Jiangsu Hengrui Medicine
3-aminocycloalkyl compounds as RORgammaT inhibitors and uses thereof
Merck Sharp & Dohme
Inhibition of guinea pig aldehyde oxidase activity by different flavonoid compounds: An in vitro study.
Kermanshah University of Medical Sciences
Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
Boehringer Ingelheim International
L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.
Case Western Reserve University
5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
University of Oslo
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Merck Frosst Centre For Therapeutic Research
Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors.
Merck Sharp & Dohme Research Laboratories
7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist.
Tokushima Research Institute
SDZ 205-557, a selective, surmountable antagonist for 5-HT4 receptors in the isolated guinea pig ileum.
Sandoz Pharma
Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1).
Pfizer