Anti-cancer drug discovery and development: Bcl-2 family small molecule inhibitors
Deregulated apoptosis is a hallmark of cancer, and the B-cell lymphoma-2 (Bcl-2) family of
proteins is pivotal to mediating the intrinsic pathway of this process. Recent advances have …
proteins is pivotal to mediating the intrinsic pathway of this process. Recent advances have …
Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins
Introduction The anti-apoptotic BCL-2 family proteins, such as BCL-2, BCL-XL, and MCL-1,
are excellent cancer therapeutic targets. The FDA approval of BCL-2 selective inhibitor …
are excellent cancer therapeutic targets. The FDA approval of BCL-2 selective inhibitor …
BM-1197: A Novel and Specific Bcl-2/Bcl-xL Inhibitor Inducing Complete and Long-Lasting Tumor Regression In Vivo
L Bai, J Chen, D McEachern, L Liu, H Zhou, A Aguilar… - PloS one, 2014 - journals.plos.org
Bcl-2 and Bcl-xL are critical regulators of apoptosis that are overexpressed in a variety of
human cancers and pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising …
human cancers and pharmacological inhibition of Bcl-2 and Bcl-xL represents a promising …
[PDF][PDF] Rational design and real time, in-cell detection of the proapoptotic activity of a novel compound targeting Bcl-XL
B Becattini, S Kitada, M Leone, E Monosov… - Chemistry & biology, 2004 - cell.com
Abstract Antiapoptotic Bcl-2-family proteins Bcl-2 and Bcl-X L have been recently validated
as drug discovery targets for cancer. Here, by using a combination of molecular modeling …
as drug discovery targets for cancer. Here, by using a combination of molecular modeling …
Bcl-2 inhibitors: small molecules with a big impact on cancer therapy
M Vogler, D Dinsdale, MJS Dyer… - Cell Death & …, 2009 - nature.com
Despite tremendous advances over the last 15 years in understanding fundamental
mechanisms of apoptosis, this has failed to translate into improved cancer therapy for …
mechanisms of apoptosis, this has failed to translate into improved cancer therapy for …
Structure-based discovery of a new class of Bcl-xL antagonists
MF Rega, M Leone, D Jung, NJH Cotton… - Bioorganic …, 2007 - Elsevier
Apoptosis, or programmed cell death, plays a key role in normal tissue homeostasis
ensuring a proper balance between cell production and cell loss. Anti-apoptotic Bcl-2-family …
ensuring a proper balance between cell production and cell loss. Anti-apoptotic Bcl-2-family …
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 …
process. This family comprises proapoptotic and prosurvival proteins, and shifting the …
Chemical, physical and biological triggers of evolutionary conserved Bcl-xL-mediated apoptosis
Background: The evidence that pan-Bcl-2 or Bcl-xL-specific inhibitors prematurely kill virus-
infected or RNA/DNA-transfected cells provides rationale for investigating these apoptotic …
infected or RNA/DNA-transfected cells provides rationale for investigating these apoptotic …
Targeting BCL2‐proteins for the treatment of solid tumours
M Vogler - Advances in medicine, 2014 - Wiley Online Library
Due to their central role in the regulation of apoptosis, the antiapoptotic BCL2‐proteins are
highly promising targets for the development of novel anticancer treatments. To this end …
highly promising targets for the development of novel anticancer treatments. To this end …
Bcl-2 inhibitors: emerging drugs in cancer therapy
C Bodur, H Basaga - Current medicinal chemistry, 2012 - ingentaconnect.com
Dose-limiting toxicity to healthy tissues is among the major hurdles in anticancer treatment
along with intrinsic or acquired multi-drug resistance. Development of small molecule …
along with intrinsic or acquired multi-drug resistance. Development of small molecule …