Halda Therapeutics Opco Inc. has divulged proteolysis-targeting chimeric (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently bonded to a protein targeting moiety via linker; they are reported to be useful for the treatment of cancer.
Research at Boehringer Ingelheim Pharma GmbH & Co. KG has led to the development of proteolysis targeting chimeras (PROTACs) comprising a Von Hippel-Lindau E3 ubiquitin ligase (VHL)-binding moiety covalently linked to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety through a linker.
Researchers from Arvinas Inc. and affiliated organizations presented the discovery and preclinical evaluation of ARV-766, a novel androgen receptor (AR) degrading proteolysis targeting chimera (PROTAC), being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC).
Researchers from the University of Arizona presented the discovery of first-in-class dual-specificity tyrosine phosphorylation-regulated kinase 1A/B (DYRK1A/B) proteolysis targeting chimeras (PROTACs) as potential Alzheimer’s disease (AD) therapeutic candidates.
A recent Nurix Therapeutics Inc. patent describes proteolysis targeting chimeras (PROTACs) comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to interleukin-1 receptor-associated kinase 4 (IRAK-4) targeting moiety via a linker reported to be useful for the treatment of cancer, metabolic diseases and inflammatory disorders.
Research at Abbvie Inc. and Calico Life Sciences LLC has led to the development of proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to tyrosine-protein phosphatase non-receptor type 2 (PTPN2; TCPTP) and/or PTPN1B. They are reported to be useful for the treatment of cancer, type 2 diabetes and nonalcoholic steatohepatitis (NASH).
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.
