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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… - Signal transduction and …, 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 …
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 …
Cancer epigenetics in clinical practice
Cancer development is driven by the accumulation of alterations affecting the structure and
function of the genome. Whereas genetic changes disrupt the DNA sequence, epigenetic …
function of the genome. Whereas genetic changes disrupt the DNA sequence, epigenetic …
Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
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 …
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
Bivalent proteolysis-targeting chimeras (PROTACs) drive protein degradation by
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …
PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
durability of their effectiveness can be limited. Resistance to these therapies is often related …
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an
approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera …
approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera …
Current strategies for the design of PROTAC linkers: a critical review
RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti …, 2020 - pmc.ncbi.nlm.nih.gov
PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules consisting of
two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to bind to a …
two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to bind to a …
E3 ligase ligands for PROTACs: how they were found and how to discover new ones
T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …
a new modality of chemical tools and potential therapeutics to understand and treat human …