An inhibitor of Bcl-2 family proteins induces regression of solid tumours

By T. Oltersdorf, S. Elmore, A. Shoemaker, R. Armstrong, D. Augeri, B. Belli, M. Bruncko, T. Deckwerth, J. Dinges, Philip J. Hajduk and 23 more. Nature, 2005

3,422 citations recorded by the source corpus.

Subfields: Molecular Biology, Organic Chemistry

View Paper: https://www.semanticscholar.org/paper/281eefc24cbd799766ef30d61681f4f7745d5cd1

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Citations in the corpus

The BH3 mimetic ABT-737 targets selective Bcl-2 proteins and efficiently induces apoptosis via Bak/Bax if Mcl-1 is neutralized. (2006, background): “In conclusion, the present studies validate the feasibility of targeting Bcl-2-like proteins using BH3 mimetics such as ABT-737 to induce apoptosis (Oltersdorf et al., 2005).”
Small-molecule inhibitors of protein-protein interactions: progressing toward the reality. (2014, background): “The major preclinical breakthrough was the 2005 disclosure of ABT-737, which was discovered through NMRbased fragment discovery, structurebased design, and medicinal chemistry (Oltersdorf et al., 2005).”
Control of mitochondrial apoptosis by the Bcl-2 family (2009, methodology): “A strategy of Bcl-2 antagonism is being employed in clinical trials of agents such as ABT-263, as some cancers are dependent on Bcl-2 for survival (Oltersdorf et al., 2005; Tse et al., 2008).”
Substantial susceptibility of chronic lymphocytic leukemia to BCL2 inhibition: results of a phase I study of navitoclax in patients with relapsed or refractory disease. (2012, background): “In preclinical in vivo models, both ABT-737 and navitoclax display synergy with cytotoxic agents and targeted therapies against other lymphoproliferative diseases(5,14) and malignancies.(3,34) Along with the promising single-agent activity observed in this study of heavily pretreated patients, such ”
Recent advances in the development of protein–protein interactions modulators: mechanisms and clinical trials (2020, methodology): “Abbott researchers studied the Bcl-XL hydrophobic groove and found that the hydrophobic groove consists of two relatively independent small pockets.(82) They used the “SAR by NMR” approach to screen the fragments with BH3 on Bcl-XL, and obtained compound 1 (Kd = 0.”
Selectivity by Small-Molecule Inhibitors of Protein Interactions Can Be Driven by Protein Surface Fluctuations (2015, neutral): “Markings inside the cells denote experimental reports (2, 22, 107, 116, 122-130) for a given protein-ligand pair (Kd or Ki where available,”
How do BCL-2 proteins induce mitochondrial outer membrane permeabilization? (2008, neutral): “ABT-737 (Abbott compound 737)] [19,27,33, 39 ].”