Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials

X Xie, T Yu, X Li, N Zhang, LJ Foster, C Peng… - Signal transduction and …, 2023 - nature.com
Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

S Pan, A Ding, Y Li, Y Sun, Y Zhan, Z Ye… - Chemical Society …, 2023 - pubs.rsc.org
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …

Current advances and development strategies of orally bioavailable PROTACs

S Zeng, Y Ye, H Xia, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …

DNA damage and its role in cancer therapeutics

J Moon, I Kitty, K Renata, S Qin, F Zhao… - International Journal of …, 2023 - mdpi.com
DNA damage is a double-edged sword in cancer cells. On the one hand, DNA damage
exacerbates gene mutation frequency and cancer risk. Mutations in key DNA repair genes …

[HTML][HTML] Targeting androgen receptor degradation with PROTACs from bench to bedside

X Jia, X Han - Biomedicine & Pharmacotherapy, 2023 - Elsevier
Highlights•AR is a clinically fully validated target for treatment of human prostate
cancer.•PROTAC AR degraders overcome common resistance mechanisms developed …

Blocking non-enzymatic functions by PROTAC-mediated targeted protein degradation

D Sun, J Zhang, G Dong, S He… - Journal of Medicinal …, 2022 - ACS Publications
The non-enzymatic functions of target proteins play key roles in the regulation of various cell
signaling pathways and are closely related to numerous human diseases. However …

FGFR-targeted therapeutics: Clinical activity, mechanisms of resistance and new directions

M Katoh, Y Loriot, G Brandi, S Tavolari… - Nature Reviews …, 2024 - nature.com
Fibroblast growth factor (FGF) signalling via FGF receptors (FGFR1–4) orchestrates fetal
development and contributes to tissue and whole-body homeostasis, but can also promote …

Target protein degradation by protacs: A budding cancer treatment strategy

D Choudhary, A Kaur, P Singh, G Chaudhary… - Pharmacology & …, 2023 - Elsevier
Cancer is one of the most common causes of death. So, its lethal effect increases with time.
Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or …

Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design

D Mi, Y Li, H Gu, Y Li, Y Chen - European Journal of Medicinal Chemistry, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) as an emerging drug discovery modality has
been extensively concerned in recent years. Over 20 years development, accumulated …