Advancing strategies for proteolysis-targeting chimera design

M Li, Y Zhi, B Liu, Q Yao - Journal of medicinal chemistry, 2023 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by
degrading various disease-causing proteins, particularly those related to tumors. Therefore …

Unlocking the potential of PROTACs: A comprehensive review of protein degradation strategies in disease therapy

RP Bhole, PR Kute, RV Chikhale, CG Bonde, A Pant… - Bioorganic …, 2023 - Elsevier
The technology known asPROTACs (PROteolysisTArgeting Chimeras) is a method of
protein degradation. Utilising bifunctional small molecules, the ubiquitin-proteosome system …

Protein degradation by in-cell self-assembly of proteolysis targeting chimeras

H Lebraud, DJ Wright, CN Johnson… - ACS central …, 2016 - ACS Publications
Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a
promising potential alternative to protein inhibition for therapeutic intervention. Current …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

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 …

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …

The advantages of targeted protein degradation over inhibition: an RTK case study

GM Burslem, BE Smith, AC Lai, S Jaime-Figueroa… - Cell chemical …, 2018 - cell.com
Proteolysis targeting chimera (PROTAC) technology has emerged over the last two decades
as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the …

Reversible assembly of proteolysis targeting chimeras

W Gui, SF Giardina, M Balzarini, F Barany… - ACS Chemical …, 2023 - ACS Publications
PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the
development of probe molecules and drug leads. However, they suffer from certain …

Recent progress in degradation of membrane proteins by PROTACs and alternative targeted protein degradation techniques

S Chen, J Cui, H Chen, B Yu, S Long - European Journal of Medicinal …, 2023 - Elsevier
Targeted protein degradation (TPD) is one of the key strategies of current targeted cancer
therapy, and it can eliminate some of the root causes of cancer, and effectively avoid drug …

Targeted protein degradation by chimeric small molecules, PROTACs and SNIPERs

M Naito, N Ohoka, N Shibata, Y Tsukumo - Frontiers in chemistry, 2019 - frontiersin.org
Technologies that induce targeted protein degradation by small molecules have been
developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras …