BCL2A1: the underdog in the BCL2 family

M Vogler - Cell Death & Differentiation, 2012 - nature.com
Abstract B-cell lymphoma 2 (BCL2) proteins are important cell death regulators, whose main
function is to control the release of cytochrome c from mitochondria in the intrinsic apoptotic …

Perturbing mitosis for anti‐cancer therapy: is cell death the only answer?

M Haschka, G Karbon, LL Fava, A Villunger - EMBO reports, 2018 - embopress.org
Interfering with mitosis for cancer treatment is an old concept that has proven highly
successful in the clinics. Microtubule poisons are used to treat patients with different types of …

The BET bromodomain inhibitor CPI203 overcomes resistance to ABT-199 (venetoclax) by downregulation of BFL-1/A1 in in vitro and in vivo models of MYC+/BCL2+ …

A Esteve-Arenys, JG Valero, A Chamorro-Jorganes… - Oncogene, 2018 - nature.com
High-grade B-cell lymphoma with MYC and BCL2 and/or BCL6 rearrangements, mostly
known as double-hit lymphoma (DHL), is a rare entity characterized by morphologic and …

Antiapoptotic potency of Bcl-2 proteins primarily relies on their stability, not binding selectivity

RW Rooswinkel, B Van De Kooij… - Blood, The Journal …, 2014 - ashpublications.org
All 6 human prosurvival Bcl-2 proteins can drive cancer development and contribute to
therapy resistance. However, their relative abilities to protect cells against cancer therapy …

Inhibitors of BCL2A1/Bfl-1 protein: potential stock in cancer therapy

X Li, J Dou, Q You, Z Jiang - European Journal of Medicinal Chemistry, 2021 - Elsevier
The Bcl-2 family members rigorously regulate cell endogenous apoptosis, and targeting anti-
apoptotic members is a hot topic in design of anti-cancer drugs. At present, FDA and EMA …

TRIM17 and TRIM28 antagonistically regulate the ubiquitination and anti-apoptotic activity of BCL2A1

L Lionnard, P Duc, MS Brennan, AJ Kueh… - Cell Death & …, 2019 - nature.com
BCL2A1 is an anti-apoptotic member of the BCL-2 family that contributes to
chemoresistance in a subset of tumors. BCL2A1 has a short half-life due to its constitutive …

Ubiquitination by the Membrane-associated RING-CH-8 (MARCH-8) Ligase Controls Steady-state Cell Surface Expression of Tumor Necrosis Factor-related …

B van de Kooij, I Verbrugge, E de Vries… - Journal of Biological …, 2013 - ASBMB
The eleven members of the membrane-associated RING-CH (MARCH) ubiquitin ligase
family are relatively unexplored. Upon exogenous (over) expression, a number of these …

Bcl-2 is a better ABT-737 target than Bcl-xL or Bcl-w and only Noxa overcomes resistance mediated by Mcl-1, Bfl-1, or Bcl-B

RW Rooswinkel, B Van De Kooij, M Verheij… - Cell death & …, 2012 - nature.com
The novel anticancer drug ABT-737 is a Bcl-2 Homology 3 (BH3)-mimetic that induces
apoptosis by inhibiting pro-survival Bcl-2 proteins. ABT-737 binds with equal affinity to Bcl-2 …

Selective covalent targeting of anti-apoptotic BFL-1 by cysteine-reactive stapled peptide inhibitors

AJ Huhn, RM Guerra, EP Harvey, GH Bird… - Cell chemical …, 2016 - cell.com
Anti-apoptotic BCL-2 family proteins block cell death by trapping the critical α-helical BH3
domains of pro-apoptotic members in a surface groove. Cancer cells hijack this survival …

[HTML][HTML] Identification of a covalent molecular inhibitor of anti-apoptotic BFL-1 by disulfide tethering

EP Harvey, ZJ Hauseman, DT Cohen… - Cell chemical …, 2020 - cell.com
The BCL-2 family is composed of anti-and pro-apoptotic members that respectively protect
or disrupt mitochondrial integrity. Anti-apoptotic overexpression can promote oncogenesis …