Nippon Zoki Pharmaceutical Co. Ltd. has discovered alkyne derivatives acting as GABA-A receptor subunit α1β2γ2 positive allosteric modulators. As such, they are believed to be useful for the treatment of sleep disorders.
Novacell Technology Inc. has identified oligopeptides acting as N-formyl peptide receptor 2 (FPR2; FPRL1; LXA4) agonists described as potentially useful for the treatment of cancer and inflammatory disorders.
Gachon University and Jeonbuk National University Industry Foundation have disclosed proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a serine/threonine-protein kinase PAK4-targeting moiety through a linker potentially useful for the treatment of cancer.
Hanmi Holdings Co. Ltd. has patented proteolysis targeting chimeras (PROTACs) comprising a cereblon (CRBN)-binding moiety coupled to a histone acetyltransferase p300 (EP300)-targeting moiety through a linker acting as EP300 degradation inducers reported to be useful for the treatment of cancer.
Multidrug-resistant (MDR) gram-positive bacteria can evade last-line therapies, such as vancomycin, daptomycin and linezolid, through the development of sophisticated resistance mechanisms that include inactivation of target enzymes, mutations in binding sites, alterations in membrane permeability and overexpression of efflux pumps.
Researchers at DEM Biopharma Inc. reported preclinical findings demonstrating the efficacy of DEM-301, a bifunctional antibody-drug conjugate (ADC) engineered to selectively recognize and eliminate tumor cells that express DEM-TXX.
Boundless Bio Inc. has obtained IND approval from the FDA for its novel kinesin oral degrader program, BBI-940. A first-in-human trial (KOMODO-1) for metastatic breast cancer is expected to begin in the first half of this year.
Orexin OX2 receptor agonists have demonstrated the ability to enhance wakefulness in rodent models, as well as in nonhuman primates and patients with narcolepsy and idiopathic hypersomnia. Based on recent findings, it has been hypothesized that they may also regulate cognition, mood and other neuropsychiatric functions. Furthermore, dysregulated orexin signaling has been reported in patients with major depressive disorder (MDD) with suicide attempts.
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