Researchers from Centre National de la Recherche Scientifique and affiliated organizations presented the discovery and preclinical identification of novel inhibitors of metallo-beta-lactamases (MBLs). Synthesis and optimization of novel broad-spectrum inhibitors against most relevant MBLs, such as VIM-type enzymes and NDM-1, led to the identification of JMV-7061 as the lead from the series.
Researchers from Italfarmaco SpA presented a new class of highly selective histone deacetylase 6 (HDAC6) inhibitors as potential candidates for the treatment of several pathologies, such as autoimmune disorders, neurodegenerative diseases, and cancer.
The Massachusetts Institute of Technology (MIT) has developed collagen mimetic peptides for PET imaging to detect idiopathic pulmonary fibrosis (IPF), with [68Ga]DOTA-CMP showing selective identification of fibrotic collagen in vivo.
Mas-related G-protein coupled receptor X2 (MRGPRX2) is expressed particularly on mast cells and its activation leads to the mast cell degranulation with release of inflammatory mediators.
Researchers from Baylor College of Medicine and Texas Children's Hospital detailed the discovery of CPK-03-37, a novel fluorescent organic molecule for tumor imaging.
Genentech Inc. presented data on structure-based lead optimization of orally bioavailable hematopoietic progenitor kinase 1 (HPK1) inhibitors. HPK1 is a negative regulator of T-cell receptor signaling in human T cells and target inhibition significantly increases cytokine production, such as IFN-gamma, TNF-alpha and IL-2, and T-cell proliferation, suggesting HPK1 inhibition as an intracellular T-cell target for cancer immunotherapy.
Identification of selective, ligand-efficient ATP-competitive inhibitors of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) for the potential treatment of cancer was discussed by Bristol Myers Squibb Co. (BMS).
Data on the development of novel noncationic macrocyclic peptides for inhibiting GTPase KRAS signaling for the potential treatment of cancer were presented by investigators from Merck & Co. Inc.
Researchers from BeiGene presented data on the discovery of highly selective covalent tyrosine-protein kinase BTK inhibitors for the potential treatment of B-cell malignancies and autoimmune disorders.
In cancer, aberrant signaling pathways can evade therapy; activation of oncogenic PI3K and MAPK signaling has inspired researchers to develop molecularly targeted drugs, such as LP-182 (University of Michigan), a multitargeted kinase inhibitor that researchers have tested in vitro and in vivo for the treatment of myelofibrosis.
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