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 …

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 …

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 …

From thalidomide to rational molecular glue design for targeted protein degradation

V Oleinikovas, P Gainza, T Ryckmans… - Annual Review of …, 2024 - annualreviews.org
Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …

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 …

Kinase inhibitors: the road ahead

FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

Phase 2 trial of iberdomide in systemic lupus erythematosus

JT Merrill, VP Werth, R Furie… - … England Journal of …, 2022 - Mass Medical Soc
Background Iberdomide, a cereblon modulator promoting degradation of the transcription
factors Ikaros and Aiolos, which affect leukocyte development and autoimmunity, is being …

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 …

Defining the human C2H2 zinc finger degrome targeted by thalidomide analogs through CRBN

QL Sievers, G Petzold, RD Bunker, A Renneville… - Science, 2018 - science.org
INTRODUCTION Thalidomide, lenalidomide, and pomalidomide are clinically approved
therapies for the treatment of multiple myeloma and other hematologic malignancies. These …