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 …

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 …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Cell cycle on the crossroad of tumorigenesis and cancer therapy

J Liu, Y Peng, W Wei - Trends in cell biology, 2022 - cell.com
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …

[PDF][PDF] Targeting cell-cycle machinery in cancer

JM Suski, M Braun, V Strmiska, P Sicinski - Cancer cell, 2021 - cell.com
Abnormal activity of the core cell-cycle machinery is seen in essentially all tumor types and
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …

Protein degradation technology: a strategic paradigm shift in drug discovery

H Li, J Dong, M Cai, Z Xu, XD Cheng, JJ Qin - Journal of Hematology & …, 2021 - Springer
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely
used strategy for treating malignant tumors. However, most intracellular proteins have been …

Understanding the metabolism of proteolysis targeting chimeras (PROTACs): the next step toward pharmaceutical applications

L Goracci, J Desantis, A Valeri… - Journal of Medicinal …, 2020 - ACS Publications
Hetero-bifunctional PROteolysis TArgeting Chimeras (PROTACs) represent a new emerging
class of small molecules designed to induce polyubiquitylation and proteasomal-dependent …

A bibliometric analysis of PROTAC from 2001 to 2021

D Li, D Yu, Y Li, R Yang - European Journal of Medicinal Chemistry, 2022 - Elsevier
Proteolysis targeting chimera (PROTAC) technology, one of the targeted protein degradation
technologies, has drawn marked attention from researchers of both academia and industry …

Development of allosteric and selective CDK2 inhibitors for contraception with negative cooperativity to cyclin binding

EB Faber, L Sun, J Tang, E Roberts… - Nature …, 2023 - nature.com
Compared to most ATP-site kinase inhibitors, small molecules that target an allosteric pocket
have the potential for improved selectivity due to the often observed lower structural …

novel medicinal chemistry strategies targeting CDK5 for Drug Discovery

W Tang, C Lin, Q Yu, D Zhang, Y Liu… - Journal of Medicinal …, 2023 - ACS Publications
Cyclin-dependent kinase 5 (CDK5) protein plays an important role not only in the central
nervous system but also in the periphery, including immune response, regulation of insulin …