Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …

Target protein degradation by protacs: A budding cancer treatment strategy

D Choudhary, A Kaur, P Singh, G Chaudhary… - Pharmacology & …, 2023 - Elsevier
Cancer is one of the most common causes of death. So, its lethal effect increases with time.
Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or …

Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …

Targeted protein degradation by PROTACs

TK Neklesa, JD Winkler, CM Crews - Pharmacology & therapeutics, 2017 - Elsevier
Targeted protein degradation using the PROTAC technology is emerging as a novel
therapeutic method to address diseases driven by the aberrant expression of a disease …

Small molecule PROTACs: an emerging technology for targeted therapy in drug discovery

H Pei, Y Peng, Q Zhao, Y Chen - RSC advances, 2019 - pubs.rsc.org
Curing malignant carcinomas is a grand ambition in the development of human health. Over
the past decades, targeted therapies have become one of the most successful ways of …

Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

The PROTAC gold rush

K Garber - Nat. Biotechnol, 2022 - nature.com
Targeted protein degradation never had it so good. In July, Pfizer paid Arvinas $650 million
up front, plus a $350-million equity investment, to jointly develop a PROTAC degrader, now …

Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

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 …

The state of the art of PROTAC technologies for drug discovery

C Wang, C Zheng, H Wang, L Zhang, Z Liu… - European Journal of …, 2022 - Elsevier
Protein degradation technology has progressed dramatically since 2001 when proteolysis
targeting chimera (PROTAC) was first reported. Various of distinctive degradation …