[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology

CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …

Scaffold diversity synthesis and its application in probe and drug discovery

M Garcia‐Castro, S Zimmermann… - Angewandte Chemie …, 2016 - Wiley Online Library
Scaffold diversity is a crucial feature of compound collections that has a huge impact on their
success in biological screenings. The synthesis of highly complex and diverse scaffolds …

The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models

A Kotschy, Z Szlavik, J Murray, J Davidson… - Nature, 2016 - nature.com
Avoidance of apoptosis is critical for the development and sustained growth of tumours. The
pro-survival protein myeloid cell leukemia 1 (MCL1) is overexpressed in many cancers, but …

[HTML][HTML] Development of Mcl-1 inhibitors for cancer therapy

A Negi, PV Murphy - European journal of medicinal chemistry, 2021 - Elsevier
The myeloid leukemia cell differentiation protein (Mcl-1) is an anti-apoptotic protein of the B-
cell lymphoma 2 (Bcl-2) family, which regulates cellular apoptosis. Mcl-1 expression plays a …

Targeting BCL-2 to enhance vulnerability to therapy in estrogen receptor-positive breast cancer

D Merino, SW Lok, JE Visvader, GJ Lindeman - Oncogene, 2016 - nature.com
The last three decades have seen significant progress in our understanding of the role of the
pro-survival protein BCL-2 and its family members in apoptosis and cancer. BCL-2 and other …

Clinical implications of molecular heterogeneity in triple negative breast cancer

BD Lehmann, JA Pietenpol - The Breast, 2015 - Elsevier
Triple negative breast cancer (TNBC) is a molecularly heterogeneous disease lacking
recurrent targetable alterations and thus therapeutic advances have been challenging. The …

Hot-spots of Mcl-1 protein: miniperspective

C Denis, J Sopková-de Oliveira Santos… - Journal of medicinal …, 2019 - ACS Publications
Protein–protein interactions (PPIs) control many important physiological processes within
human cells. Apoptosis or programmed cell death is closely regulated by pro-and …

[HTML][HTML] New dimension in therapeutic targeting of BCL-2 family proteins

S Besbes, M Mirshahi, M Pocard, C Billard - Oncotarget, 2015 - ncbi.nlm.nih.gov
Proteins of the BCL-2 family control the mitochondrial pathway of apoptosis. Targeting these
proteins proves to be an attractive strategy for anticancer therapy. The biological context is …

BH3-only protein BIM: an emerging target in chemotherapy

S Shukla, S Saxena, BK Singh, P Kakkar - European journal of cell biology, 2017 - Elsevier
BH3-only proteins constitute major proportion of pro-apoptotic members of B-cell lymphoma
2 (Bcl-2) family of apoptotic regulatory proteins and participate in embryonic development …

Crystal structures of MBP fusion proteins

DS Waugh - Protein Science, 2016 - Wiley Online Library
Although chaperone‐assisted protein crystallization remains a comparatively rare
undertaking, the number of crystal structures of polypeptides fused to maltose‐binding …