Targeted protein degradation has gained attention in recent years due to its potential to hit proteins that are difficult to engage with conventional small molecules. Pin1 is an enzyme associated with tumor formation overexpressed in pancreatic cancer cells or cancer-associated fibroblasts in particular.

Additional early-stage research and drug discovery news in brief, from: Abelzeta Pharma, Carisma Therapeutics, Innate Pharma, Neurizon Therapeutics, Precision Biosciences, Silo Pharma, Ziccum.

F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have patented oxazolo[4,5-B]pyrazine and oxazolo[4,5-B]pyridine derivatives acting as NLRP3 inflammasome inhibitors and reported to be useful for the treatment of asthma, chronic obstructive pulmonary disease and cardiovascular disorders.

Kallyope Inc. has identified new tachykinin NK3 receptor antagonists reported to be useful for the treatment of migraine.

Work at Foghorn Therapeutics Inc. has led to the design of proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding agent coupled to CREB-binding protein (CREBBP; CBP)-targeting moiety through a linker acting as CBP degradation inducers.

Novel macrocyclic heteroaryl derivatives acting as non-receptor tyrosine-protein kinase TYK2 and/or JAK1 and/or JAK2 inhibitors have been reported in a Hangzhou Highlightll Pharmaceutical Co. Ltd. patent.

Hainan Simcere Pharmaceutical Co. Ltd. has patented new membrane-associated tyrosine- and threonine-specific Cdc2-inhibitory kinase (PKMYT1) inhibitors reported to be useful for the treatment of breast cancer.