159 articles for thisTarget
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Article Title
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26
Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors.
Shandong University
41
Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
Shandong University
10
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.
Wuhan University School of Pharmaceutical Sciences
21
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
31
DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.
University of Kansas
67
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.
Vanderbilt University School of Medicine
46
Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.
University of Maryland
6
Inhibitors of the Antiapoptotic Myeloid Cell Leukemia-1 (Mcl-1) May Provide Effective Treatment for Cancer.
Therachem Research Medilab (India)
27
Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors.
Shandong University
34
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.
Shandong University
11
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Novartis Institutes For Biomedical Research
28
Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
18
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Abbvie
36
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.
Shandong University
2
Design, synthesis and evaluation of marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors.
University of Nebraska
16
Biased and unbiased strategies to identify biologically active small molecules.
Institut De Chimie Des Substances Naturelles
13
Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1).
Institute
2
A simple and widely applicable hit validation strategy for protein-protein interaction inhibitors based on a quantitative ligand displacement assay.
Takeda Pharmaceutical
7
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)
48
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
37
Fragment-based discovery of potent inhibitors of the anti-apoptotic MCL-1 protein.
Research & Development, Abbvie
9
Discovery of potent Mcl-1/Bcl-xL dual inhibitors by using a hybridization strategy based on structural analysis of target proteins.
Takeda Pharmaceutical
8
Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker.
Eutropics Pharmaceuticals
9
Design and application of a rigid quinazolone scaffold based on two-face Bima-helix mimicking.
Dalian University of Technology
58
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
The Walter and Eliza Hall Institute of Medical Research
30
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
20
Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors.
Dalian University of Technology
70
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
24
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
9
An anthraquinone scaffold for putative, two-face Bim BH3a-helix mimic.
Dalian University of Technology
6
Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.
Clermont Universit£
15
Structure-based design of potent Bcl-2/Bcl-xL inhibitors with strong in vivo antitumor activity.
University of Michigan
19
Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold.
University of Michigan
1
Structure-activity relationship of selected polyphenol derivatives as inhibitors of Bax/Bcl-xL interaction.
University of Rennes 1
4
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
5
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
1
Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis.
Mcgill University
14
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
37
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
10
Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design.
Dalian University of Technology
11
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
15
3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.
Dalian University of Technology
12
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
8
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University of Thessaloniki
2
Cryptosphaerolide, a cytotoxic Mcl-1 inhibitor from a marine-derived ascomycete related to the genus Cryptosphaeria.
University of California San Diego
2
Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii.
Florida Atlantic University
3
Structural insights into the design of small molecule inhibitors that selectively antagonize Mcl-1.
Institute of Chemical and Engineering Sciences
10
Macrocycles and macrocyclization in anticancer drug discovery: Important pieces of the puzzle.
Dezhou University
32
Autophagy modulation in cancer therapy: Challenges coexist with opportunities.
Sichuan University
15
Innovative design and potential applications of covalent strategy in drug discovery.
Sichuan University
54
Chemical dissection of selective myeloid leukemia-1 inhibitors: How they were found and evolved.
Nanjing University of Chinese Medicine
7
Macrocyclic-based strategy in drug design: From lab to the clinic.
Shengjing Hospital of China Medical University
11
Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors.
AstraZeneca
6
Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy.
Abbvie
22
Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
AstraZeneca
51
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
23
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
13
Histidine-Covalent Stapled Alpha-Helical Peptides Targeting hMcl-1.
University of California Riverside
14
Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen.
AstraZeneca
59
Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen.
Symeres
43
Emerging and Re-emerging Warheads for Targeted Covalent Inhibitors: An Update.
Eberhard Karls University Tubingen
25
Targeting Myeloid Leukemia-1 in Cancer Therapy: Advances and Directions.
Shenyang Pharmaceutical University
4
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
University of Chinese Academy of Sciences
4
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
University of Michigan
15
Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1.
Janssen Research & Development
4
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
University of Michigan
21
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor.
Tianjin University
17
Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.
AstraZeneca
22
Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation.
Hunan University of Science and Technology
12
Inhibitors of BCL2A1/Bfl-1 protein: Potential stock in cancer therapy.
China Pharmaceutical University
15
Evolution in non-peptide α-helix mimetics on the road to effective protein-protein interaction modulators.
IQM-CSIC
12
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
8
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University of Michigan
30
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.
Sichuan University
11
Recent applications of covalent chemistries in protein-protein interaction inhibitors.
University of Maryland
23
Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells.
Yancheng Teachers University
31
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Abbott Laboratories
32
Development of Mcl-1 inhibitors for cancer therapy.
National University of Ireland Galway
8
Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.
Shenyang Pharmaceutical University
27
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.
University of Maryland
17
Design, Synthesis, and Structural Characterization of Lysine Covalent BH3 Peptides Targeting Mcl-1.
University of California Riverside
24
Design, synthesis and biological evaluation of dual Bcl-2/Mcl-1 inhibitors bearing 2-(1H-indol-4-yl)benzoic acid scaffold.
Shenyang Pharmaceutical University
12
Discovery of a Copper-Based Mcl-1 Inhibitor as an Effective Antitumor Agent.
Guangxi Normal University
7
Bicyclic Helical Peptides as Dual Inhibitors Selective for Bcl2A1 and Mcl-1 Proteins.
The University of Queensland
37
Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment.
Dalian University of Technology
14
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
10
Myeloid Cell Leukemia-1 Inhibitors as Emerging Cancer Treatment.
Therachem Research Medilab
4
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Xihua University
2
Synthesis and evaluation of a UMI-77-based fluorescent probe for selective detecting Mcl-1 protein and imaging in living cancer cells.
Shandong University
17
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
Shandong University
31
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.
Paris-Saclay University
2
From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1).
University of Calgary
42
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
47
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Servier Research Institute of Medicinal Chemistry
30
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
TBA
20
Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology.
Eberhard Karls University T£Bingen
27
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
17
Indole: A privileged scaffold for the design of anti-cancer agents.
Hunan University of Science and Technology
26
Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors.
Shandong University
16
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles.
AstraZeneca
15
Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands.
TBA
22
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
Dalian University of Technology
27
Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors.
Shandong University
10
NMR strategy for unraveling structures of bioactive sponge-derived oxy-polyhalogenated diphenyl ethers.
University of California
16
Discovery and development of substituted tyrosine derivatives as Bcl-2/Mcl-1 inhibitors.
Shandong University
20
Kröhnke pyridines: Rapid and facile access to Mcl-1 inhibitors.
University of Maryland
11
Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.
University of Maryland
27
1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation.
Shandong University
4
Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.
Vanderbilt University
7
X-ray Structures of Target-Ligand Complexes Containing Compounds with Assay Interference Potential.
Rheinische Friedrich-Wilhelms-Universit£T
40
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.
Vanderbilt University School of Medicine
42
Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors.
Shenyang Pharmaceutical University
85
PHENYLPIPERIDINE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN
Boehringer Ingelheim International
454
ALPHA PROTEIN KINASE 1 INHIBITORS FOR USE IN TREATING KAWASAKI DISEASE
Shanghai Yao Yuan Biotechnology Co.
91
BORON CONTAINING PYRIMIDINE COMPOUNDS, COMPOSITIONS COMPRISING THEM, METHODS AND USES THEREOF
Boehringer Ingelheim Animal Health Usa
186
ASGPR-BINDING COMPOUNDS FOR THE DEGRADATION OF EXTRACELLULAR PROTEINS
Avilar Therapeutics
93
Isoindoline compositions and methods for treating neurodegenerative disease
Cognition Therapeutics
3
Methods of treating neurological, metabolic, and other disorders using enantiopure deuterium-enriched pioglitazone
Poxel
58
Fluorinated cyclopropylamine compound, preparation method therefor, pharmaceutical composition thereof, and uses thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
1
Salts and pharmaceutical compositions thereof for the treatment of inflammatory disorders
Galapagos
489
Methods of modulating the activity of the MC5 receptor and treatment of conditions related to this receptor
Mimetica
5
Structure-Activity Relationships of Benzenesulfonamide-Based Inhibitors towards Carbonic Anhydrase Isoform Specificity.
University of Florida
11
Inhibition of guinea pig aldehyde oxidase activity by different flavonoid compounds: An in vitro study.
Kermanshah University of Medical Sciences
3
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
53
Synthesis and target identification of hymenialdisine analogs.
Genomics Institute of The Novartis Research Foundation
109
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Abbott Laboratories