[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 …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

[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 …

Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …

Advances in targeting 'undruggable'transcription factors with small molecules

MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …

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 …

[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 …

The great escape: tumour cell plasticity in resistance to targeted therapy

S Boumahdi, FJ de Sauvage - Nature reviews Drug discovery, 2020 - nature.com
The success of targeted therapies in cancer treatment has been impeded by various
mechanisms of resistance. Besides the acquisition of resistance-conferring genetic …

The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K

M Słabicki, Z Kozicka, G Petzold, YD Li, M Manojkumar… - Nature, 2020 - nature.com
Molecular glue compounds induce protein–protein interactions that, in the context of a
ubiquitin ligase, lead to protein degradation. Unlike traditional enzyme inhibitors, these …

[HTML][HTML] Epigenetic modifications of histones in cancer

Z Zhao, A Shilatifard - Genome biology, 2019 - Springer
The epigenetic modifications of histones are versatile marks that are intimately connected to
development and disease pathogenesis including human cancers. In this review, we will …