Merck KGaA and Cancer Research Technology Ltd. have synthesized 2,8-dihydropyrazolo[3,4-b]indoles acting as transcriptional coactivator YAP1/transcriptional enhancer factor (TEAD) interaction inhibitors reported to be useful for the treatment of cancer, cardiovascular disorders and liver fibrosis.
Forendo Pharma Oy has presented aldo-keto reductase family 1 member C3 (AKR1C3) and/or prostaglandin F2-α synthase inhibitors reported to be useful for the treatment of acne, cancer, alopecia, obesity, chronic obstructive pulmonary disease, dysmenorrhea, endometriosis and polycystic ovary syndrome, among others.
Regulatory T cells (Tregs) are known suppressors of immunity activation in the tumor microenvironment, and a high density of Tregs is tied to a poor response to cancer immunotherapy, with CCR8+ Tregs identified as being highly suppressive. Ctm Bio Co. therefore have studied the CCR8 antagonist antibody CTM-033 in preclinical cancer models.
Killer cell immunoglobulin-like receptor 3DL3 (KIR3DL3) is a member of the killer cell Ig-like (KIR) receptor family. When KIR3DL3 is expressed on T and natural killer (NK) cells in the tumor microenvironment, it suppresses immune responses following engagement with HHLA2, suggesting that the KIR3DL3-HHLA2 axis potentially represents a novel immune checkpoint pathway and that blockade of KIR3DL3 signaling could promote antitumor immunity.
Tuberous sclerosis is a genetic disease caused by loss-of-function mutations in the TSC1 or TSC2 genes. At the neurological level, this rare disease is characterized by benign tumor growth, epilepsy, cognitive deficits and autism. Epilepsy is the main neurological trait and presents mostly as infantile spasms.
Researchers from King's College London and UCB Pharma Inc. recently reported preclinical data on the effects of an anti-mouse neonatal Fc receptor (FcRn) antibody, UCB-4470, on circulating antiphospholipid (aPL) and aPL-induced thrombus formation in mice.
Brain insulin signaling is known to control peripheral energy metabolism and regulation of mood and cognition. Dysregulation in this signaling has been tied to brain pathological disorders such as Alzheimer’s disease (AD). Previous findings have reported a strong connection between type 2 diabetes (T2D) and AD, suggesting insulin resistance as a potential risk factor for AD pathology and other forms of dementia.
Investigators at the University of Bristol and Biognos AB have identified a structural feature that distinguished the deadly coronavirus strains from harmless, common cold-causing variants. The findings, which were published in the Nov. 23, 2022, issue of Science Advances, could form the basis of universal COVID antivirals, putting an end to the endless race to deal with new variants that has so far been a necessity.
The researchers showed that the same pocket, a binding site for linoleic acid (LA), was present in all variants of concern (VOCs) that have emerged since 2020. “Intriguingly, all SARS-CoV-2 VOCs stringently maintain this pocket, notably including Omicron, which accumulated a wide range of mutations in [the spike protein] elsewhere, suggesting that the pocket provides a selective advantage for the virus,” they wrote in their paper.
Chengdu Easton Biopharmaceuticals Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) ligand binding moiety covalently bound to a bromodomain-containing protein 4 (BRD4; HUNK1)-targeting moiety through a linker.
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