From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors
…, WJ Fairbrother, JD Leverson, AJ Souers - Nature reviews drug …, 2017 - nature.com
Members of the B cell lymphoma 2 (BCL-2) gene family have a central role in regulating
programmed cell death by controlling pro-apoptotic and anti-apoptotic intracellular signals. In …
programmed cell death by controlling pro-apoptotic and anti-apoptotic intracellular signals. In …
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets
AJ Souers, JD Leverson, ER Boghaert, SL Ackler… - Nature medicine, 2013 - nature.com
Proteins in the B cell CLL/lymphoma 2 (BCL-2) family are key regulators of the apoptotic
process. This family comprises proapoptotic and prosurvival proteins, and shifting the balance …
process. This family comprises proapoptotic and prosurvival proteins, and shifting the balance …
Found in translation: how preclinical research is guiding the clinical development of the BCL2-selective inhibitor venetoclax
JD Leverson, D Sampath, AJ Souers, SH Rosenberg… - Cancer discovery, 2017 - AACR
Since the discovery of apoptosis as a form of programmed cell death, targeting the apoptosis
pathway to induce cancer cell death has been a high-priority goal for cancer therapy. After …
pathway to induce cancer cell death has been a high-priority goal for cancer therapy. After …
β-Turn mimetic library synthesis: scaffolds and applications
AJ Souers, JA Ellman - Tetrahedron, 2001 - Elsevier
The poor receptor subtype selectivity, poor biostability and unfavorable absorption properties
that often accompany therapeutically relevant peptides has generated a considerable …
that often accompany therapeutically relevant peptides has generated a considerable …
[HTML][HTML] Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 …
…, SH Rosenberg, C Tse, SW Elmore, AJ Souers - Cell death & …, 2015 - nature.com
The anti-apoptotic protein MCL-1 is a key regulator of cancer cell survival and a known
resistance factor for small-molecule BCL-2 family inhibitors such as ABT-263 (navitoclax), making …
resistance factor for small-molecule BCL-2 family inhibitors such as ABT-263 (navitoclax), making …
Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy
…, WJ Fairbrother, SW Elmore, AJ Souers - Science translational …, 2015 - science.org
The BCL-2/BCL-X L /BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical activity
in lymphoid malignancies such as chronic lymphocytic leukemia. However, its efficacy in …
in lymphoid malignancies such as chronic lymphocytic leukemia. However, its efficacy in …
[HTML][HTML] The Bcl-2 specific BH3 mimetic ABT-199: a promising targeted therapy for t (11; 14) multiple myeloma
…, S Le Gouill, D Sampath, JD Leverson, AJ Souers… - Leukemia, 2014 - nature.com
Despite recent advances in the treatment of multiple myeloma (MM), including proteasome
inhibitors and immunomodulatory agents, patients invariably relapse and alternative …
inhibitors and immunomodulatory agents, patients invariably relapse and alternative …
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity
…, JD Leverson, SW Elmore, AJ Souers - ACS medicinal …, 2014 - ACS Publications
A-1155463, a highly potent and selective BCL-X L inhibitor, was discovered through
nuclear magnetic resonance (NMR) fragment screening and structure-based design. This …
nuclear magnetic resonance (NMR) fragment screening and structure-based design. This …
Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models
…, S Maiga, WJ Fairbrother, M Amiot, AJ Souers… - Molecular cancer …, 2016 - AACR
BCL-2 family proteins dictate survival of human multiple myeloma cells, making them attractive
drug targets. Indeed, multiple myeloma cells are sensitive to antagonists that selectively …
drug targets. Indeed, multiple myeloma cells are sensitive to antagonists that selectively …
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity
…, JD Leverson, SW Elmore, AJ Souers - Journal of medicinal …, 2015 - ACS Publications
Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the
progression and survival of multiple tumor types. Herein we report a series of MCL-1 inhibitors …
progression and survival of multiple tumor types. Herein we report a series of MCL-1 inhibitors …