[HTML][HTML] PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature Reviews Drug Discovery, 2022 - nature.com
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 …

[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 …

[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 …

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 …

Discovery of a first-in-class degrader for nuclear receptor binding SET domain protein 2 (NSD2) and Ikaros/Aiolos

F Meng, C Xu, KS Park, HU Kaniskan… - Journal of medicinal …, 2022 - ACS Publications
Overexpression of nuclear receptor binding SET domain protein 2 (NSD2) is frequent in
multiple myeloma (MM). However, existing NSD2 inhibitors are largely ineffective in …

[HTML][HTML] Recent advances in PROTACs for drug targeted protein research

T Yao, H Xiao, H Wang, X Xu - International Journal of Molecular …, 2022 - mdpi.com
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 …

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 …

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 …

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 …

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 …