Discovery of new Lenalidomide derivatives as potent and selective GSPT1 degraders

Advancing Strategies for Proteolysis-Targeting Chimera Design

(2023) Minglei Li et al.   Journal of Medicinal Chemistry

Protein degraders enter the clinic — a new approach to cancer therapy

(2023) Deborah Chirnomas et al.   Nature Reviews Clinical Oncology

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

(2022) Yue Zhong et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic

(2022) Janet M. Sasso et al.   BIOCHEMISTRY

SJPYT-195: A Designed Nuclear Receptor Degrader That Functions as a Molecular Glue Degrader of GSPT1

(2022) Andrew D. Huber et al.   ACS Medicinal Chemistry Letters

Structure-activity relationship analysis of novel GSPT1 degraders based on benzotriazinone scaffold and its antitumor effect on xenograft mouse model

(2022) Akshay D. Takwale et al.   BIOORGANIC CHEMISTRY

C-MYC Targeting By Degradation: Novel Dual c-Myc/GSPT1 Degrader GT19715 Induces TP53-Independent Cell Death in Acute Myeloid Leukemia and Lymphomas

(2022) Yuki Nishida et al.   BLOOD

PROTACS: A technology with a gold rush-like atmosphere

(2022) Yu-Wei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

GSPT1 Functions as a Tumor Promoter in Human Liver Cancer

(2022) Yi-qing Xi et al.   Current Medical Science

CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia

(2021) Joshua D. Hansen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery

(2021) Guoqiang Dong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators

(2021) Gisele Nishiguchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library

(2020) Chelsea E. Powell et al.   ACS Chemical Biology

CC-90009, a novel cereblon E3 ligase modulator targets acute myeloid leukemia blasts and leukemia stem cells

(2020) Christine Surka et al.   BLOOD

Simple Structural Modifications Converting a Bona Fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

(2019) Jiuling Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

(2016) Mary E. Matyskiela et al.   NATURE

Translation termination factor eRF3 is targeted for caspase-mediated proteolytic cleavage and degradation during DNA damage-induced apoptosis

(2012) Yoshifumi Hashimoto et al.   APOPTOSIS

GGCn polymorphism of eRF3a/GSPT1 gene and breast cancer susceptibility

(2011) Mahboobe Miri et al.   MEDICAL ONCOLOGY

Structural insights into eRF3 and stop codon recognition by eRF1

(2009) Z. Cheng et al.   GENES & DEVELOPMENT