From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors
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 …
programmed cell death by controlling pro-apoptotic and anti-apoptotic intracellular signals …
Pathways and mechanisms of venetoclax resistance
P Bose, V Gandhi, M Konopleva - Leukemia & lymphoma, 2017 - Taylor & Francis
The approval of venetoclax, a 'BH3-mimetic'antagonist of the BCL-2 anti-apoptotic protein,
for chronic lymphocytic leukemia represents a major milestone in translational apoptosis …
for chronic lymphocytic leukemia represents a major milestone in translational apoptosis …
Selective MCL-1 inhibitor ABBV-467 is efficacious in tumor models but is associated with cardiac troponin increases in patients
J Yuda, C Will, DC Phillips, L Abraham… - Communications …, 2023 - nature.com
Background MCL-1 is a prosurvival B-cell lymphoma 2 family protein that plays a critical role
in tumor maintenance and survival and can act as a resistance factor to multiple anticancer …
in tumor maintenance and survival and can act as a resistance factor to multiple anticancer …
BCL2 inhibitors as anticancer drugs: a plethora of misleading BH3 mimetics
R S. Soderquist, A Eastman - Molecular cancer therapeutics, 2016 - AACR
Antiapoptotic BCL2 proteins play a major role in tumor cell survival. Hence, BCL2 inhibitors
have been developed as direct inducers of apoptosis. ABT-199 (venetoclax) received …
have been developed as direct inducers of apoptosis. ABT-199 (venetoclax) received …
MCL-1 is a master regulator of cancer dependency on fatty acid oxidation
MS Prew, U Adhikary, DW Choi, EP Portero, JA Paulo… - Cell reports, 2022 - cell.com
MCL-1 is an anti-apoptotic BCL-2 family protein essential for survival of diverse cell types
and is a major driver of cancer and chemoresistance. The mechanistic basis for the …
and is a major driver of cancer and chemoresistance. The mechanistic basis for the …
BH3 profiling discriminates on-target small molecule BH3 mimetics from putative mimetics
M Villalobos-Ortiz, J Ryan, TN Mashaka… - Cell Death & …, 2020 - nature.com
Inhibition of the anti-apoptotic machinery of cancer cells is a promising therapeutic approach
that has driven the development of an important class of compounds termed “BH3 mimetics” …
that has driven the development of an important class of compounds termed “BH3 mimetics” …
Lisaftoclax (APG-2575) is a novel BCL-2 inhibitor with robust antitumor activity in preclinical models of hematologic malignancy
Purpose: Development of B-cell lymphoma 2 (BCL-2)–specific inhibitors poses unique
challenges in drug design because of BCL-2 homology domain 3 (BH3) shared homology …
challenges in drug design because of BCL-2 homology domain 3 (BH3) shared homology …
Iterative optimization yields Mcl-1–targeting stapled peptides with selective cytotoxicity to Mcl-1–dependent cancer cells
R Rezaei Araghi, GH Bird, JA Ryan… - Proceedings of the …, 2018 - National Acad Sciences
Bcl-2 family proteins regulate apoptosis, and aberrant interactions of overexpressed
antiapoptotic family members such as Mcl-1 promote cell transformation, cancer survival …
antiapoptotic family members such as Mcl-1 promote cell transformation, cancer survival …
Novel BCL-2 inhibitor lisaftoclax in relapsed or refractory chronic lymphocytic leukemia and other hematologic malignancies: first-in-human open-label trial
Purpose: This global phase I trial investigated the safety, efficacy, pharmacokinetics, and
pharmacodynamics of lisaftoclax (APG-2575), a novel, orally active, potent selective B-cell …
pharmacodynamics of lisaftoclax (APG-2575), a novel, orally active, potent selective B-cell …
Peptide design by optimization on a data-parameterized protein interaction landscape
Many applications in protein engineering require optimizing multiple protein properties
simultaneously, such as binding one target but not others or binding a target while …
simultaneously, such as binding one target but not others or binding a target while …