Bruton tyrosine kinase (BTK) inhibition is a provenly effective strategy for the treatment of B-cell malignancies with several compounds approved such as ibrutinib, acalabrutinib or zanubrutinib. BTK also plays a central role in immunity and has thus emerged as a potential therapeutic target in autoimmune and inflammatory disorders.
Tegid Therapeutics Inc. has identified proteolysis targeting chimera (PROTACs) compounds comprising cereblon (CRBN) ligands covalently bonded to a mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1)-targeting moiety.
Cancer Research Technology Ltd. has disclosed proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding moiety covalently bonded to a mitogen-activated protein kinase 7 (MAPK7; ERK5)-targeting moiety through a linker. They are reported to be useful for the treatment of cancer.
“I am not a fortune teller, nor am I a gambler. I will make no bets,” Lorraine Kalia told the audience at the 2023 International Congress of Parkinson’s Disease and Movement Disorders. “But I am optimistic.” At the meeting, which is being held in Copenhagen this week, Kalia, who is a scientist at Toronto Western Hospital’s Krembil Brain Institute and at the University of Toronto’s Tanz Centre for Research in Neurodegenerative Diseases, was giving an overview of “Emerging targets in the clinic” in a plenary session on “Therapeutic strategies for the future.”
Research at Beigene Co. Ltd. has led to the identification of new proteolysis targeting chimera (PROTAC) compounds comprising E3 ubiquitin ligase binding moiety covalently linked to a Bruton tyrosine kinase (BTK) targeting moiety via linker. They are reported to be useful for the treatment of cancer.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has patented new proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a target protein binding moiety through a linker.
Researchers at Boehringer Ingelheim (BI) Pharma GmbH & Co. KG and Vanderbilt University have described proteolysis targeting chimera (PROTAC) compounds comprising E3 ubiquitin ligase binding moieties covalently linked to GTPase KRAS (mutant) binding moieties through a linker.
Arvinas Operations Inc. and Genentech Inc. have described proteolysis targeting chimera (PROTAC) compounds comprising a Von Hippel-Lindau (VHL) E3 ubiquitin ligase binding moiety coupled to a probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) targeting moiety through a linker reported to be useful for the treatment of cancer, including non-small-cell lung cancer.
St. Jude Children’s Research Hospital has divulged proteolysis targeting chimeras (PROTACs) comprising cereblon (CRBN) ligands coupled to a tyrosine-protein kinase Lck targeting moiety via a linker acting as Lck degradation inducers reported to be useful for the treatment of cancer and immunological disorders.
