Assays and technologies for developing proteolysis targeting chimera degraders
Targeted protein degradation by small-molecule degraders represents an emerging mode of
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …
action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules …
Targeted protein degradation: elements of PROTAC design
SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …
PROTACs: current trends in protein degradation by proteolysis-targeting chimeras
In the recent past, proteolysis-targeting chimera (PROTAC) technology has received
enormous attention for its ability to overcome the limitations of protein inhibitors and its …
enormous attention for its ability to overcome the limitations of protein inhibitors and its …
[HTML][HTML] PROteolysis TArgeting Chimeras (PROTACs)—past, present and future
M Pettersson, CM Crews - Drug Discovery Today: Technologies, 2019 - Elsevier
The majority of currently used therapeutics are small molecule-based and utilize occupancy-
driven pharmacology as the mode of action (MOA), in which the protein function is …
driven pharmacology as the mode of action (MOA), in which the protein function is …
Small-molecule degraders beyond PROTACs—challenges and opportunities
JM Kastl, G Davies, E Godsman… - … the Science of Drug …, 2021 - journals.sagepub.com
Targeted protein degradation (TPD) is a recent strategy, utilizing the cell's proteostasis
machinery to deplete specific proteins. This represents a paradigm shift in early drug …
machinery to deplete specific proteins. This represents a paradigm shift in early drug …
[引用][C] Proteolysis targeting chimera (PROTAC): a paradigm-shifting approach in small molecule drug discovery
Great success has been achieved in small molecule drug discovery programs, making
extraordinary contributions for human health, especially in targeted therapy. Taking …
extraordinary contributions for human health, especially in targeted therapy. Taking …
Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …
therapeutic resistance, which is partially driven by the undruggable proteome. The …
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 …
PROTACs: an emerging therapeutic modality in precision medicine
DA Nalawansha, CM Crews - Cell chemical biology, 2020 - cell.com
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …