G1 to S phase transition 1 (GSPT1) is a protein involved in cell cycle progression, translation termination, and protein homeostasis, and its overexpression has been implicated in various cancers. Although GSPT1 is considered a promising therapeutic target, the lack of conventional ligand-binding pockets has historically rendered it undruggable.
Raqualia Pharma Inc.’s Fimecs Inc. subsidiary has agreed with Astellas Pharma Inc. to add two new targets under their ongoing joint research. They entered into an agreement in 2022 to conduct joint research on targeted protein degradation.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has synthesized molecular glue degraders comprising cereblon (CRBN) binding agents and protein degradation moieties reported to be useful for the treatment of cancer, infections, autoimmune diseases, anemia, transplant rejection, diabetes, cardiovascular disorders and inflammatory disorders, among others.
Blueprint Medicines Corp. has disclosed PROTAC compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a cyclin-dependent kinase 4 (CDK4)-targeting moiety potentially useful for the treatment of cancer.
In an effort to develop more effective estrogen receptor α (ERα) inhibitors, researchers at Nanjing University of Chinese Medicine and collaborators aimed to develop a proteolysis targeting chimera (PROTAC) against the receptor.
Nikang Therapeutics Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to a cyclin-dependent kinase 2 (CDK2)- and/or CDK4-targeting moiety through a linker reported to be useful for the treatment of cancer.
Captor Therapeutics Inc. has disclosed molecular glue degraders comprising a cereblon (CRBN) binding moiety acting as serine/threonine-protein kinase Nek7 degradation inducers reported to be useful for the treatment of amyotrophic lateral sclerosis, Still’s disease, Behçet’s disease, familial Mediterranean fever, Alzheimer’s disease, pulmonary arterial hypertension and more.
Vaxcellbio Co. Ltd. has signed a research agreement with the Korea Drug Development Fund (KDDF) to pursue the discovery of next-generation targeted anticancer lead compounds based on degradation of the molecular motor protein MYO1D (myosin 1D).
Crossfire Oncology BV has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a serine/threonine-protein kinase PLK1 (STPK13) targeting moiety through a linker reported to be useful for the treatment of cancer, autoimmune diseases, transplant rejection, neurological disorders and inflammatory disorders.
Mindrank Therapeutics (Suzhou) New Drug Research & Development Co. Ltd. has divulged molecular glue degraders comprising cereblon (CRBN) ligands acting as dual eukaryotic peptide chain release factor GTP-binding subunit ERF3A (GSPT1) and casein kinase 1 isoform α (CSNK1A1) degradation inducers. They are reported to be potentially useful for the treatment of cancer, Alzheimer’s disease, inflammatory disorders, autoimmune diseases and metabolic diseases.
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