The manipulation of apoptosis for cancer therapy using BH3-mimetic drugs

ST Diepstraten, MA Anderson, PE Czabotar… - Nature Reviews …, 2022 - nature.com
Apoptosis is a form of programmed cell death that is regulated by the balance between
prosurvival and proapoptotic BCL-2 protein family members. Evasion of apoptosis is a …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

Targeting MCL-1 in cancer: current status and perspectives

H Wang, M Guo, H Wei, Y Chen - Journal of hematology & oncology, 2021 - Springer
Abstract Myeloid leukemia 1 (MCL-1) is an antiapoptotic protein of the BCL-2 family that
prevents apoptosis by binding to the pro-apoptotic BCL-2 proteins. Overexpression of MCL …

PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

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 …

Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation

Y Wan, G Fang, H Chen, X Deng, Z Tang - European Journal of Medicinal …, 2021 - Elsevier
Currently, the arise of drug resistance and undesirable off-target effects of anti-cancer
agents are major challenges for cancer treatment, which energizes medicinal chemists to …

E3 ligase ligands in successful PROTACs: an overview of syntheses and linker attachment points

A Bricelj, C Steinebach, R Kuchta, M Gütschow… - Frontiers in …, 2021 - frontiersin.org
Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new
and exciting class of therapeutic agents that promise to significantly impact drug discovery …

MCL-1 inhibitors, fast-lane development of a new class of anti-cancer agents

A Bolomsky, M Vogler, MC Köse, CA Heckman… - Journal of hematology & …, 2020 - Springer
Cell death escape is one of the most prominent features of tumor cells and closely linked to
the dysregulation of members of the Bcl-2 family of proteins. Among those, the anti-apoptotic …

Developments of CRBN-based PROTACs as potential therapeutic agents

C Wang, Y Zhang, Y Wu, D Xing - European journal of medicinal chemistry, 2021 - Elsevier
Protease-targeted chimeras (PROTACs) are a new technology that is receiving much
attention in the treatment of diseases. The mechanism is to inhibit protein function by …

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

X Li, Y Song - Journal of hematology & oncology, 2020 - Springer
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for
targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly …