Direct activation of Bax protein for cancer therapy
Bax, a central cell death regulator, is an indispensable gateway to mitochondrial dysfunction
and a major proapoptotic member of the B‐cell lymphoma 2 (Bcl‐2) family proteins that …
and a major proapoptotic member of the B‐cell lymphoma 2 (Bcl‐2) family proteins that …
Chemical modulation of cytosolic BAX homodimer potentiates BAX activation and apoptosis
N Gitego, B Agianian, OW Mak, V Kumar MV… - Nature …, 2023 - nature.com
The BCL-2 family protein BAX is a major regulator of physiological and pathological cell
death. BAX predominantly resides in the cytosol in a quiescent state and upon stress, it …
death. BAX predominantly resides in the cytosol in a quiescent state and upon stress, it …
Small-molecule Bax agonists for cancer therapy
M Xin, R Li, M Xie, D Park, TK Owonikoko… - Nature …, 2014 - nature.com
Bax, a central death regulator, is required at the decisional stage of apoptosis. We recently
identified serine 184 (S184) of Bax as a critical functional switch controlling its proapoptotic …
identified serine 184 (S184) of Bax as a critical functional switch controlling its proapoptotic …
Activation of the proapoptotic Bcl-2 protein Bax by a small molecule induces tumor cell apoptosis
G Zhao, Y Zhu, CO Eno, Y Liu, L DeLeeuw… - … and Cellular Biology, 2014 - Taylor & Francis
The proapoptotic Bcl-2 protein Bax by itself is sufficient to initiate apoptosis in almost all
apoptotic paradigms. Thus, compounds that can facilitate disruptive Bax insertion into …
apoptotic paradigms. Thus, compounds that can facilitate disruptive Bax insertion into …
Pharmacological inhibition of Bax-induced cell death: Bax-inhibiting peptides and small compounds inhibiting Bax
K Jensen, DJ WuWong, S Wong… - Experimental …, 2019 - journals.sagepub.com
Bax is an essential mediator of mitochondria-dependent programed cell death. Bax belongs
to the Bcl-2 family of proteins and its activities are regulated through interaction with other …
to the Bcl-2 family of proteins and its activities are regulated through interaction with other …
Physiological and pharmacological modulation of BAX
AZ Spitz, E Gavathiotis - Trends in pharmacological sciences, 2022 - cell.com
Bcl-2-associated X protein (BAX) is a critical executioner of mitochondrial regulated cell
death through its lethal activity of permeabilizing the mitochondrial outer membrane (MOM) …
death through its lethal activity of permeabilizing the mitochondrial outer membrane (MOM) …
An autoinhibited dimeric form of BAX regulates the BAX activation pathway
Pro-apoptotic BAX is a cell fate regulator playing an important role in cellular homeostasis
and pathological cell death. BAX is predominantly localized in the cytosol, where it has a …
and pathological cell death. BAX is predominantly localized in the cytosol, where it has a …
Phosphorylation switches Bax from promoting to inhibiting apoptosis thereby increasing drug resistance
Akt is a pro‐survival kinase frequently activated in human cancers and is associated with
more aggressive tumors that resist therapy. Here, we connect Akt pathway activation to …
more aggressive tumors that resist therapy. Here, we connect Akt pathway activation to …
Small-molecule allosteric inhibitors of BAX
BAX is a critical effector of the mitochondrial cell death pathway in response to a diverse
range of stimuli in physiological and disease contexts. Upon binding by BH3-only proteins …
range of stimuli in physiological and disease contexts. Upon binding by BH3-only proteins …
Direct and selective small-molecule activation of proapoptotic BAX
BCL-2 family proteins are key regulators of the apoptotic pathway. Antiapoptotic members
sequester the BCL-2 homology 3 (BH3) death domains of proapoptotic members such as …
sequester the BCL-2 homology 3 (BH3) death domains of proapoptotic members such as …