Researchers from Johns Hopkins University and affiliated organizations have published details on the discovery and preclinical characterization of a purine antimetabolite, Pro-905, which is being developed for the treatment of malignant peripheral nerve sheath tumors (MPNST).
Researchers from Cogent Biosciences Inc. have reported the discovery and preclinical characterization of CGT-4255, a novel EGFR-sparing, ErbB2 inhibitor with activity against oncogenic ErbB2 mutations.
Phosphoinositide 3-kinase (PI3K) is a key cell cycle pathway regulator involved in tumor growth and development. PI3Kα mutations in p110α subunit, H1047R and E542K/E545K are found in patients with several cancer types, including breast cancer and are targeted by approved drugs such as Piqray (alpelisib, Novartis AG).
Researchers from Insilico Medicine Inc. reported on ISM-5043, a novel KAT6A inhibitor aimed to be used for the treatment of refractory ER+ breast cancer.
Researchers from Gilgamesh Pharmaceuticals Inc. and affiliated organizations have presented the discovery and preclinical evaluation of GM-3009, a novel noribogaine analogue being developed for the treatment of opioid use disorder (OUD).
Myeloproliferative neoplasms (MPNs) are a group of disorders of which the main hallmarks are bone marrow fibrosis and atypical megakaryocytes (MK) accumulation. Both Rho kinase (ROCK) and Aurora kinase (ARK) pathways are involved in correct MK maturation.
A new degrader strategy has been previously proposed to mitigate platelet toxicity associated with Bcl-xL degraders. This strategy consists of selectively degrading Bcl-xL by the von Hippel-Lindau protein (VHL) E3 ligase in tumor cells, but not in platelets, which minimally express VHL. DT-2216 was developed as the first Bcl-xL degrader of this kind; however, this clinical candidate has still shown some platelet toxicity in vivo.
Psychiatric indications, such as depression, schizophrenia and bipolar disorder, share a common feature of elevated expression of pro-inflammatory markers in the periphery and/or central nervous system. Based on this, it is believed that combined immuno- and neuromodulatory activities of phosphodiesterase 4 (PDE4) inhibitors may represent a promising new therapeutic strategy for various psychiatric indications.
Nuclear receptor subfamily 1 group D member (NR1D1), also known as Rev-erbA-α, is highly expressed in the liver, adipose tissue, brain and skeletal muscle.
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