The interplay between apoptosis and cellular senescence: Bcl-2 family proteins as targets for cancer therapy
A Basu - Pharmacology & therapeutics, 2022 - Elsevier
Cell death by apoptosis and permanent cell cycle arrest by senescence serve as barriers to
the development of cancer. Chemotherapeutic agents not only induce apoptosis, they can …
the development of cancer. Chemotherapeutic agents not only induce apoptosis, they can …
The multiple mechanisms of MCL1 in the regulation of cell fate
Abstract MCL1 (myeloid cell leukemia-1) is a widely recognized pro-survival member of the
Bcl-2 (B-cell lymphoma protein 2) family and a promising target for cancer therapy. While the …
Bcl-2 (B-cell lymphoma protein 2) family and a promising target for cancer therapy. While the …
BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models
U Rauh, G Wei, M Serrano-Wu, G Kosmidis… - Nature Cancer, 2024 - nature.com
The MCL1 gene is frequently amplified in cancer and codes for the antiapoptotic protein
myeloid cell leukemia 1 (MCL1), which confers resistance to the current standard of care …
myeloid cell leukemia 1 (MCL1), which confers resistance to the current standard of care …
[HTML][HTML] Venetoclax resistance: mechanistic insights and future strategies
F Ong, K Kim, MY Konopleva - Cancer Drug Resistance, 2022 - ncbi.nlm.nih.gov
Acute myeloid leukemia (AML) is historically associated with poor prognosis, especially in
older AML patients unfit for intensive chemotherapy. The development of Venetoclax, a …
older AML patients unfit for intensive chemotherapy. The development of Venetoclax, a …
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
J Cantley, X Ye, E Rousseau, T Januario… - Nature …, 2022 - nature.com
Abstract The mammalian SWItch/Sucrose Non-Fermentable (SWI/SNF) helicase SMARCA4
is frequently mutated in cancer and inactivation results in a cellular dependence on its …
is frequently mutated in cancer and inactivation results in a cellular dependence on its …
Targeting CDK9 for anti-cancer therapeutics
R Mandal, S Becker, K Strebhardt - Cancers, 2021 - mdpi.com
Simple Summary CDK9, in combination with Cyclin T1, is one of the major regulators of RNA
Polymerase II mediated productive transcription of critical genes in any cell. The activity of …
Polymerase II mediated productive transcription of critical genes in any cell. The activity of …
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 …
A phase 1 first-in-human study of the MCL-1 inhibitor AZD5991 in patients with relapsed/refractory hematologic malignancies
P Desai, S Lonial, A Cashen, M Kamdar… - Clinical Cancer …, 2024 - aacrjournals.org
Purpose: AZD5991, a human MCL-1 inhibitor, was assessed for safety, tolerability,
pharmacokinetics, and antitumor activity as monotherapy and in combination with …
pharmacokinetics, and antitumor activity as monotherapy and in combination with …
[HTML][HTML] Inhibition of the CDK9–cyclin T1 protein–protein interaction as a new approach against triple-negative breast cancer
Abstract Cyclin-dependent kinase 9 (CDK9) activity is correlated with worse outcomes of
triple-negative breast cancer (TNBC) patients. The heterodimer between CDK9 with cyclin …
triple-negative breast cancer (TNBC) patients. The heterodimer between CDK9 with cyclin …
The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico …
Abstract Treatment options for the management of breast cancer are still inadequate. This
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …