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 …

[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 …

Mapping the degradable kinome provides a resource for expedited degrader development

KA Donovan, FM Ferguson, JW Bushman, NA Eleuteri… - Cell, 2020 - cell.com
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 …

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 …

Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

B Nabet, FM Ferguson, BKA Seong, M Kuljanin… - Nature …, 2020 - nature.com
Chemical biology strategies for directly perturbing protein homeostasis including the
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 …

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 …

Targeted protein degradation as a powerful research tool in basic biology and drug target discovery

T Wu, H Yoon, Y Xiong, SE Dixon-Clarke… - Nature Structural & …, 2020 - nature.com
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 …

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 …

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

WH Guo, X Qi, X Yu, Y Liu, CI Chung, F Bai… - Nature …, 2020 - nature.com
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 …