PROTAC targeted protein degraders: the past is prologue
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 …
tackle disease-causing proteins that have historically been highly challenging to target with …
Advancing targeted protein degradation for cancer therapy
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 …
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
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
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 …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
From thalidomide to rational molecular glue design for targeted protein degradation
Thalidomide and its derivatives are powerful cancer therapeutics that are among the best-
understood molecular glue degraders (MGDs). These drugs selectively reprogram the E3 …
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 …
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 …
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 …
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 …
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 …
therapies for the treatment of multiple myeloma and other hematologic malignancies. These …