Daiichi Sankyo Co. Ltd. has prepared and tested new 2-azabicyclo[3.1.1]heptane compounds acting as orexin OX2 receptor agonists with potential for the treatment of narcolepsy.
Drug conjugates acting as gonadotropin-releasing hormone (GnRH) receptor ligands have been described in a recent Radionetics Oncology Inc. patent. They are reported to be useful for the diagnosis and treatment of cancer.
Work at Karuna Therapeutics Inc. has led to the identification of substituted tetrahydropyrrolo-pyridinone compounds acting as muscarinic M4 receptor agonists and/or positive allosteric modulators.
Oncopia Therapeutics Inc. has patented proteolysis targeting chimeric (PROTACs) compounds comprising cereblon (CRBN) ligands covalently bonded to a CREB-binding protein (CREBBP; CBP) and/or histone acetyltransferase KAT3B (P300)-targeting moiety through a linker.
As PD-L1 and CD73 are both overexpressed in the tumor microenvironment (TME) and inhibiting CD73 has been shown to enhance anti-PD-L1 efficacy, dual-targeting of PD-L1 and CD73 has emerged as a feasible strategy in the oncolytic field.
OTU deubiquitinase 5 (OTUD5) is a deubiquitinating enzyme that has been shown to play a key role in mediating innate immunity and inflammation development, and which is also involved in various cancers.
Researchers from the University of California San Francisco and Northwestern University recently presented findings from a study that aimed to evaluate the role of lin-28 homolog B (LIN28B), an RNA binding protein expressed in a variety of cancers, in diffuse midline glioma (DMG).
Many patients with amyotrophic lateral sclerosis (ALS) or frontotemporal dementia (FTD) harbor the (G4C2)n pathogenic repeat expansion in the C9orf72 gene, which leads to aggregating dipeptide proteins, mainly poly-glycine-alanine (poly-GA).
Abata Therapeutics Inc. has obtained FDA clearance for its IND application enabling initiation of a first-in-human study of ABA-101 in patients with progressive multiple sclerosis (MS). A phase I study will open later this year.
Brains from people with heroin use disorder have an increased number of hypocretin (Hcrt, orexin) neurons, which in turn are significantly smaller than in healthy controls. Meanwhile, human narcolepsy is known to present an average 90% loss of Hcrt neurons and no risk for drug abuse or overdose, even under methamphetamine or methylphenidate prescription, because of a greatly reduced reward activation of the ventral tegmental area (VTA).
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