Targeting tyrosine-protein kinase Lck (LCK) with dasatinib has demonstrated activity against T-cell acute lymphoblastic leukemia (T-ALL). To make the effects more lasting, researchers from St. Jude Children's Research Hospital and the University of Pennsylvania designed proteolysis targeting chimeras (PROTACs) using dasatinib as an LCK ligand and phenyl-glutarimide as a cereblon-directing moiety.
Araris Biotech AG has raised $24 million in a second round of funding, as it completes preparations to take its lead antibody-drug conjugate (ADC) into the clinic. The company continues to accumulate preclinical data indicating its novel linker technology makes for an improved therapeutic index compared to approved ADCs, and the lead product is expected to begin clinical development next year.
Failure of integrin inhibitors in clinical trials can be avoided by redesigning the chemical conformation of these proteins, as shown by a study led by Timothy Springer, a professor in the Department of Biological Chemistry and Molecular Pharmacology at Boston Children's Hospital, and one of the winners of the 2022 Albert Lasker Basic Medical Research Award.
Lyell Immunopharma Inc. has received FDA clearance for its IND application to initiate a phase I trial for LYL-845, an investigational tumor-infiltrating lymphocyte (TIL) therapy enhanced with Lyell's Epi-R technology for patients with relapsed and/or refractory metastatic or locally advanced melanoma and other select solid tumors.
Vincere Biosciences Inc. has presented new ubiquitin carboxyl-terminal hydrolase 30 (USP30) inhibitors reported to be useful for the treatment of cancer, cardiovascular disorders, eye disorders, renal disorders, peroxisomal disorders, ataxia, pulmonary fibrosis and neurodegeneration.
Mirati Therapeutics Inc. has identified new protein arginine N-methyltransferase 5 (PRMT5) inhibitors reported to be useful for the treatment of methylthioadenosine phosphorylase (MTAP)-associated cancer.
Proteolysis targeting chimeras (PROTACs) are drugs that use cancer cells’ own proteasome to selectively degrade essential tumor-driver molecules through E3 ubiquitin ligase binding. Resistance to PROTAC therapy in cultured cells has been shown to involve genomic alterations in their E3 ligase targets.
A research team at Deciphera Pharmaceuticals LLC has discovered novel small-molecule colony-stimulating factor 1 receptor (CSF-1R) inhibitors for the treatment of cancer.
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