Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
The concept of intrinsic versus extrinsic apoptosis
L Lossi - Biochemical Journal, 2022 - portlandpress.com
Regulated cell death is a vital and dynamic process in multicellular organisms that maintains
tissue homeostasis and eliminates potentially dangerous cells. Apoptosis, one of the better …
tissue homeostasis and eliminates potentially dangerous cells. Apoptosis, one of the better …
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) …
Co-targeting of BAX and BCL-XL proteins broadly overcomes resistance to apoptosis in cancer
Deregulation of the BCL-2 family interaction network ensures cancer resistance to apoptosis
and is a major challenge to current treatments. Cancer cells commonly evade apoptosis …
and is a major challenge to current treatments. Cancer cells commonly evade apoptosis …
Apoptosis deregulation and the development of cancer multi-drug resistance
Simple Summary Despite recent therapeutic advances against cancer, many patients do not
respond well or respond poorly, to treatment and develop resistance to more than one anti …
respond well or respond poorly, to treatment and develop resistance to more than one anti …
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
B-cell lymphoma extra large (BCL-XL) is a well-validated cancer target. However, the on-
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …
target and dose-limiting thrombocytopenia limits the use of BCL-XL inhibitors, such as …
Molecular mechanisms of cell death: recommendations of the Nomenclature Committee on Cell Death 2018
L Galluzzi, I Vitale, SA Aaronson, JM Abrams… - Cell Death & …, 2018 - nature.com
Over the past decade, the Nomenclature Committee on Cell Death (NCCD) has formulated
guidelines for the definition and interpretation of cell death from morphological, biochemical …
guidelines for the definition and interpretation of cell death from morphological, biochemical …
BCL-2 family proteins: changing partners in the dance towards death
The BCL-2 family of proteins controls cell death primarily by direct binding interactions that
regulate mitochondrial outer membrane permeabilization (MOMP) leading to the irreversible …
regulate mitochondrial outer membrane permeabilization (MOMP) leading to the irreversible …
Mitochondria as playmakers of apoptosis, autophagy and senescence
Mitochondria are the key energy-producing organelles and cellular source of reactive
species. They are responsible for managing cell life and death by a balanced homeostasis …
species. They are responsible for managing cell life and death by a balanced homeostasis …
[HTML][HTML] Targeting apoptotic caspases in cancer
A Boice, L Bouchier-Hayes - … et Biophysica Acta (BBA)-Molecular Cell …, 2020 - Elsevier
Members of the caspase family of proteases play essential roles in the initiation and
execution of apoptosis. These caspases are divided into two groups: the initiator caspases …
execution of apoptosis. These caspases are divided into two groups: the initiator caspases …