Beyond proteolysis-targeting chimeric molecules: designing heterobifunctional molecules based on functional effectors
L Hua, Q Zhang, X Zhu, R Wang, Q You… - Journal of Medicinal …, 2022 - ACS Publications
In recent years, with the successful development of proteolysis-targeting chimeric molecules
(PROTACs), the potential of heterobifunctional molecules to contribute to reenvisioning drug …
(PROTACs), the potential of heterobifunctional molecules to contribute to reenvisioning drug …
Stimuli‐Responsive PROTACs for Controlled Protein Degradation
K An, X Deng, H Chi, Y Zhang, Y Li… - Angewandte Chemie …, 2023 - Wiley Online Library
Abstract Proteolysis Targeting Chimeras (PROTACs) represent a promising therapeutic
modality to address undruggable and resistant issues in drug discovery. However, potential …
modality to address undruggable and resistant issues in drug discovery. However, potential …
Strategies for designing proteolysis targeting chimaeras (PROTACs)
S He, G Dong, J Cheng, Y Wu… - Medicinal Research …, 2022 - Wiley Online Library
Proteolysis targeting chimaeras (PROTACs) is a cutting edge and rapidly growing technique
for new drug discovery and development. Currently, the largest challenge in the molecular …
for new drug discovery and development. Currently, the largest challenge in the molecular …
From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation
C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs
The vast majority of currently marketed drugs rely on small molecules with an 'occupancy-
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five'chemical space: Recent progress and future challenges
SD Edmondson, B Yang, C Fallan - Bioorganic & Medicinal Chemistry …, 2019 - Elsevier
Proteolysis targeting chimeras (PROTACs) are heterobifunctional compounds with
molecular weights and other properties that lie outside the classic 'rule-of-five'space …
molecular weights and other properties that lie outside the classic 'rule-of-five'space …
Rapid PROTAC discovery platform: nanomole-scale array synthesis and direct screening of reaction mixtures
MP Plesniak, EK Taylor, F Eisele… - ACS Medicinal …, 2023 - ACS Publications
Precise length, shape, and linker attachment points are all integral components to designing
efficacious proteolysis targeting chimeras (PROTACs). Due to the synthetic complexity of …
efficacious proteolysis targeting chimeras (PROTACs). Due to the synthetic complexity of …
Enriching proteolysis targeting chimeras with a second modality: When two are better than one
A Salerno, F Seghetti, J Caciolla, E Uliassi… - Journal of Medicinal …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC)-mediated protein degradation has prompted a
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
Covalent PROTACs: the best of both worlds?
NP Grimster - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Covalent PROTACs combine the cutting edge research areas of targeted covalent inhibitors
(TCIs) and proteolysis targeting chimeras (PROTACs). This nascent field of research has …
(TCIs) and proteolysis targeting chimeras (PROTACs). This nascent field of research has …