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 …
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 …
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 …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
Cell cycle on the crossroad of tumorigenesis and cancer therapy
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
[PDF][PDF] Targeting cell-cycle machinery in cancer
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 …
represents a driving force of tumorigenesis. Recent studies revealed that cell-cycle proteins …
Protein degradation technology: a strategic paradigm shift in drug discovery
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely
used strategy for treating malignant tumors. However, most intracellular proteins have been …
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 …
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 …
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
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 …
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 …
nervous system but also in the periphery, including immune response, regulation of insulin …