[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] Chronic and cycling hypoxia: drivers of cancer chronic inflammation through HIF-1 and NF-κB activation: a review of the molecular mechanisms

J Korbecki, D Simińska… - International journal of …, 2021 - mdpi.com
Chronic (continuous, non-interrupted) hypoxia and cycling (intermittent, transient) hypoxia
are two types of hypoxia occurring in malignant tumors. They are both associated with the …

[HTML][HTML] Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

[PDF][PDF] 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 …

E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

Development of targeted protein degradation therapeutics

PP Chamberlain, LG Hamann - Nature chemical biology, 2019 - nature.com
Targeted protein degradation as a therapeutic modality has seen dramatic progress and
massive investment in recent years because of the convergence of two key scientific …

[HTML][HTML] Discovery of CRBN as a target of thalidomide: a breakthrough for progress in the development of protein degraders

J Yamamoto, T Ito, Y Yamaguchi… - Chemical Society Reviews, 2022 - pubs.rsc.org
Progress in strategies aimed at breaking down therapeutic target proteins has led to a
paradigm shift in drug discovery. Thalidomide and its derivatives are the only protein …

[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review

RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …

[PDF][PDF] Lessons in PROTAC design from selective degradation with a promiscuous warhead

DP Bondeson, BE Smith, GM Burslem… - Cell chemical …, 2018 - cell.com
Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we
report a previously understudied benefit of small molecule proteolysis-targeting chimeras …