Current treatments for Graves’ hyperthyroidism (GH) and Graves’ orbitopathy (GO) are ineffective. Researchers assessed the preclinical in vitro efficacy of SYD-5115 (Byondis BV), a novel low-molecular-weight thyrotropin receptor (TSH-R) antagonist. The compound comprises an N-acetylated dihydropyrrole pyrimidine core with various substituents, including a difluorinated-spirocyclohexyl ring and a chiral carbamate group on the pyrimidine ring.
Having demonstrated in previous work that drug-Fc conjugates (DFCs) are a promising treatment alternative for multidrug-resistant (MDR) gram-negative bacteria, researchers from the Center for Discovery and Innovation and Cidara Therapeutics Inc. presented results from the identification of CTC-177, a novel DFC, as a potential immunoprophylactic agent against MDR gram-negative bacterial infections.
Son of sevenless 1 (SOS1) is a guanine exchange factor (GEF) primarily responsible for linking cell-surface receptors to RAS protein activation converting the inactive form of GDP-loaded RAS proteins into the active GTP-loaded RAS. This role together with its function in inhibiting MAPK pathway reactivation suggest that SOS1 may be a therapeutic target to treat KRAS-driven cancers.
Autotaxin (ATX) is an enzyme responsible for the production of lysophosphatidic acid (LPA), which plays a role in the pathogenesis of systemic sclerosis (SSc). Researchers from Mitsubishi Tanabe Pharma Corp. and colleagues have reported on the preclinical evaluation of MT-5562, a novel oral ATX inhibitor, as a therapeutic option for SSc.
CD38 is an enzyme with NAD-depleting and intracellular signaling activity expressed on the cell surface, in intracellular compartments and in mitochondria, and is linked to inflammatory and autoimmune diseases. Studies in CD38-deficient mice have revealed that these animals develop a type of collagen-induce arthritis (CIA) which suggests a link between CD38 and CIA pathogenesis.
α-Synucleinopathies constitute a set of neurological disorders including Parkinson’s disease (PD), dementia with Lewy bodies, multiple systems atrophy (MSA), and other rare disorders. The development of positron emission tomography (PET) tracers for imaging α-synuclein aggregates is essential for performing efficient and accurate diagnosis, tracking disease progression and monitoring efficacy of potential therapies.
Researchers from Atux Iskay LLC assessed whether reactivation of protein phosphatase 2A (PP2A) using a small-molecule PP2A activator, ATUX-1215, could counter TGF-β signaling in preclinical models of idiopathic pulmonary fibrosis (IPF).
Glioblastoma multiforme (GBM) is an aggressive brain cancer with poor prognosis and survival. TNF-related apoptosis-inducing ligand (TRAIL) is a protein that induces apoptosis in cancer cells by binding death receptors type 4 and 5. Researchers at the University of North Carolina explored using hiNeuroS-TRAIL combined with the ClpP activator TR-107 as a potential treatment.
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