Beigene Co. Ltd. has divulged proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding moiety covalently linked to a mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1; HPK1; MEKKK1)-targeting moiety reported to be useful for the treatment of cancer.
A preclinical data presentation at the American Society of Clinical Oncology Genitourinary Cancers Symposium later this week has prompted Halda Therapeutics Inc. to emerge from stealth and unveil its novel Riptac (Regulated Induced Proximity Targeting Chimera) platform for creating heterobifunctional small molecules designed to kill cancer cells selectively. The New Haven, Conn.-based company has been quietly refining the technology since its formation in 2019 and has already secured $76 million in series A and B rounds.
Prelude Therapeutics Inc. has divulged proteolysis-targeting chimeric (PROTAC) compounds comprising a Von Hippel-Lindau E3 ubiquitin ligase (VHL)-binding moiety covalently linked to a SMARCA2- or SMARCA4-targeting moiety through a linker reported to be useful for the treatment of cancer.
Hinova Pharmaceuticals Inc. has presented proteolysis targeting chimera (PROTAC) compounds comprising E3 ubiquitin ligase-binding moiety covalently linked to tyrosine-protein phosphatase nonreceptor type 11 (PTPN11)-targeting moiety through a linker reported to be useful for the treatment of cancer, Noonan and LEOPARD syndromes.
Medshine Discovery Inc. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moieties covalently linked to bromodomain-containing protein 4 (BRD4; HUNK1) targeting moieties through a linker reported to be useful for the treatment of cancer.
Uppthera Inc. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding agent coupled to serine/threonine-protein kinase PLK1 (STPK13) targeting moiety through a linker, acting as novel PLK1 protein degradation-inducing compounds with use for the treatment of cancer and neurological disorders.
Abbvie Inc. has described new proteolysis targeting chimera (PROTA) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to tyrosine protein phosphatase nonreceptor type 2 (PTPN2)-targeting moiety reported to be useful for the treatment of cancer, diabetes type 2 and nonalcoholic steatohepatitis.
Shaanxi Panlong Pharmaceutical Group Co. Ltd. has disclosed proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to 3C-like proteinase (3CLpro; Mpro; nsp5) (SARS-CoV-2; COVID-19 virus) targeting moiety via linker acting as 3CLpro (SARS-CoV-2) degradation inducers reported to be useful for the treatment of SARS-CoV-2 infection.
University of Maryland has presented proteolysis targeting chimeras (PROTACs) comprised of E3 ubiquitin ligase cereblon (CRBN)-binding moiety covalently linked to induced myeloid leukemia cell differentiation protein Mcl-1-binding moiety through a linker reported to be useful for the treatment of cancer.
