[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
[HTML][HTML] 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 …
[HTML][HTML] 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… - … and Targeted Therapy, 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 …
Target and tissue selectivity of PROTAC degraders
RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
Discovery of a first-in-class degrader for nuclear receptor binding SET domain protein 2 (NSD2) and Ikaros/Aiolos
Overexpression of nuclear receptor binding SET domain protein 2 (NSD2) is frequent in
multiple myeloma (MM). However, existing NSD2 inhibitors are largely ineffective in …
multiple myeloma (MM). However, existing NSD2 inhibitors are largely ineffective in …
[HTML][HTML] Recent advances in PROTACs for drug targeted protein research
Proteolysis-targeting chimera (PROTAC) is a heterobifunctional molecule. Typically,
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …
PROTAC consists of two terminals which are the ligand of the protein of interest (POI) and …
Strategies to Reduce the On‐Target Platelet Toxicity of Bcl‐xL Inhibitors: PROTACs, SNIPERs and Prodrug‐Based Approaches
A Negi, AS Voisin‐Chiret - ChemBioChem, 2022 - Wiley Online Library
Apoptosis is a highly regulated cellular process. Aberration in apoptosis is a common
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …
characteristic of various disorders. Therefore, proteins involved in apoptosis are prime …
Discovery of pomalidomide-based PROTACs for selective degradation of histone deacetylase 8
Z Sun, B Deng, Z Yang, R Mai, J Huang, Z Ma… - European Journal of …, 2022 - Elsevier
Overexpression of histone deacetylase 8 (HDAC8) is associated with various diseases such
as cancer. Thus, compounds that can modulate HDAC8 levels have therapeutic potential for …
as cancer. Thus, compounds that can modulate HDAC8 levels have therapeutic potential for …
Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment
Z Zhang, L Bai, L Hou, H Deng, S Luan, D Liu… - European Journal of …, 2022 - Elsevier
Apoptosis is the major mode of programmed cell death, which conduces to maintain tissue
homeostasis, clearance of abnormal cells and development of organisms. Over the past two …
homeostasis, clearance of abnormal cells and development of organisms. Over the past two …
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 …