Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation
RP Wurz, H Rui, K Dellamaggiore… - Nature …, 2023 - nature.com
Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
Recent developments in PROTAC‐mediated protein degradation: from bench to clinic
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
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 …
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
Assessing different E3 ligases for small molecule induced protein ubiquitination and degradation
P Ottis, M Toure, PM Cromm, E Ko… - ACS chemical …, 2017 - ACS Publications
Proteolysis targeting chimera (PROTAC) technology, the recruitment of E3 ubiquitin ligases
to induce the degradation of a protein target, is rapidly impacting chemical biology, as well …
to induce the degradation of a protein target, is rapidly impacting chemical biology, as well …
The advantages of targeted protein degradation over inhibition: an RTK case study
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 …
as a powerful tool for targeted degradation of endogenous proteins. Herein we describe the …
Targeted protein degradation by PROTACs
TK Neklesa, JD Winkler, CM Crews - Pharmacology & therapeutics, 2017 - Elsevier
Targeted protein degradation using the PROTAC technology is emerging as a novel
therapeutic method to address diseases driven by the aberrant expression of a disease …
therapeutic method to address diseases driven by the aberrant expression of a disease …
Chemical-mediated targeted protein degradation in neurodegenerative diseases
S Hyun, D Shin - Life, 2021 - mdpi.com
Neurodegenerative diseases, including Alzheimer's disease, Huntington's disease, and
Parkinson's disease, are a class of diseases that lead to dysfunction of cognition and …
Parkinson's disease, are a class of diseases that lead to dysfunction of cognition and …
The rise of covalent proteolysis targeting chimeras
R Gabizon, N London - Current opinion in chemical biology, 2021 - Elsevier
Targeted protein degradation offers several advantages over direct inhibition of protein
activity and is gaining increasing interest in chemical biology and drug discovery …
activity and is gaining increasing interest in chemical biology and drug discovery …
Harnessing the power of proteolysis for targeted protein inactivation
R Verma, D Mohl, RJ Deshaies - Molecular cell, 2020 - cell.com
Two decades into the twenty-first century, a confluence of breakthrough technologies
wielded at the molecular level is presenting biologists with unique opportunities to unravel …
wielded at the molecular level is presenting biologists with unique opportunities to unravel …
Fundamental aspects of DMPK optimization of targeted protein degraders
C Cantrill, P Chaturvedi, C Rynn, JP Schaffland… - Drug discovery today, 2020 - Elsevier
Highlights•Degraders are an emerging modality which fall into the 'beyond rule of
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …