Insulin-like growth factor 2 mRNA binding protein 3 (IGF2BP3) is an oncofetal RNA-binding protein aberrantly overexpressed in multiple cancers, where it promotes tumor growth by stabilizing oncogenic mRNAs. Researchers at the University of California described the efficacy of I3IN-002, a potent IGF2BP3 inhibitor, in leukemia models.
A University of California patent describes new poly(ADP-ribose) polymerase 1 (PARP-1; ARTD1), DNA repair and serine/threonine-protein kinase ATR inhibitors potentially useful for the treatment of cancer.
The University of California has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase Von Hippel-Lindau disease tumor suppressor (VHL)-binding moiety coupled to cAMP-dependent protein kinase catalytic subunit α (PRKACA) targeting moiety through a linker.
Cymirafen is a novel antibody-drug conjugate (ADC) from the University of California that targets leucine-rich repeat-containing G-protein coupled receptor 4 (LGR4)/LGR5/LGR6 and is composed of a potent cytotoxic payload, monomethyl auristatin E (MMAE), plus an Fc domain fused to the receptor binding domain of RSPO1.
The University of California has reported new azocino[4,5,6-cd]indoles acting as 5-HT2A receptor agonists and thus potentially useful for the treatment of neurological and psychiatric disorders.
Tau is an intrinsically disordered protein that regulates the stability and dynamics of microtubules in physiological conditions. Recent work has revealed the involvement of tau in various neuronal processes. Researchers from the University of California and collaborators aimed to systematically investigate the cellular factors that control the accumulation of tau aggregates in human neurons.
Opioid use disorder (OUD) causes high morbidity and mortality rates, with fentanyl driving unprecedented overdose rates. Researchers from the University of California have used an AI-based drug discovery platform with the aim of identifying preclinical drug candidates for OUD.
The University of California has synthesized proprotein convertase subtilisin/kexin-type 9 (PCSK9) inhibitors reported to be useful for the treatment of cancer, atherosclerosis and stroke.
The University of California has synthesized α-synuclein (SNCA) and/or amyloid-β protein and/or microtubule-associated protein tau (PHF-tau; MAPT) propagation inhibitors reported to be useful for diagnosis and treatment of multiple system atrophy, Parkinson’s disease and Alzheimer’s disease.