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 …
[HTML][HTML] Degradation of proteins by PROTACs and other strategies
Y Wang, X Jiang, F Feng, W Liu, H Sun - Acta Pharmaceutica Sinica B, 2020 - Elsevier
Blocking the biological functions of scaffold proteins and aggregated proteins is a
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …
Mapping the degradable kinome provides a resource for expedited degrader development
Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-
dependent degradation of proteins. TPD is of interest in drug development, as it can address …
dependent degradation of proteins. TPD is of interest in drug development, as it can address …
PHOTACs enable optical control of protein degradation
M Reynders, BS Matsuura, M Bérouti, D Simoneschi… - Science …, 2020 - science.org
PROTACs (PROteolysis TArgeting Chimeras) are bifunctional molecules that target proteins
for ubiquitylation by an E3 ligase complex and subsequent degradation by the proteasome …
for ubiquitylation by an E3 ligase complex and subsequent degradation by the proteasome …
Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2
A Mares, AH Miah, IED Smith, M Rackham… - Communications …, 2020 - nature.com
Abstract Proteolysis-Targeting Chimeras (PROTACs) are heterobifunctional small-molecules
that can promote the rapid and selective proteasome-mediated degradation of intracellular …
that can promote the rapid and selective proteasome-mediated degradation of intracellular …
Efficient targeted degradation via reversible and irreversible covalent PROTACs
R Gabizon, A Shraga, P Gehrtz, E Livnah… - Journal of the …, 2020 - ACS Publications
Proteolysis targeting chimeras (PROTACs) represent an exciting inhibitory modality with
many advantages, including substoichiometric degradation of targets. Their scope, though …
many advantages, including substoichiometric degradation of targets. Their scope, though …
Targeted protein degradation as a powerful research tool in basic biology and drug target discovery
Controlled perturbation of protein activity is essential to study protein function in cells and
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …
living organisms. Small molecules that hijack the cellular protein ubiquitination machinery to …
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 …
Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
Current efforts in the proteolysis targeting chimera (PROTAC) field mostly focus on choosing
an appropriate E3 ligase for the target protein, improving the binding affinities towards the …
an appropriate E3 ligase for the target protein, improving the binding affinities towards the …