Current antiviral agents for COVID-19 treatment target viral proteins, which are susceptible to mutation during SARS-CoV-2 evolution. A potential strategy to fight emerging drug resistances is the development of compounds targeting host proteins that are indispensable for the viral life cycle.
Researchers at Dana-Farber Cancer Institute are advancing a fourth-generation allosteric EGFR inhibitor, EAI-432, to treat non-small-cell lung cancer driven by mutations in the EGFR gene, particularly the L858R mutation.
Proteoglycan glypican-1 (GPC1) is a tumor-associated antigen that is highly expressed in tumor tissues from patients with pancreatic ductal adenocarcinoma (PDAC), while its expression is very low on benign neoplastic lesions, chronic pancreatitis and normal adult pancreatic tissue. Researchers from Centro Di Riferimento Oncologico (CRO Aviano) and L'Università degli studi di Trieste have reported the development and preclinical characterization of AT-101, a novel complement-fixing IgM antibody targeting GPC1, as a potential immunotherapy candidate for the treatment of PDAC.
Researchers have developed a new approach for the development of improved CAR T cells with bifunctional degraders, which linked ubiquitin to an endogenous target protein. The key to the design was the use of multispecific protein degraders and E3 ligases, which increased the proliferation of CAR T cells and their antitumor potency. This combination can be adapted to different uses of cell therapies.
Cancer Research Technology Ltd. has described inhibitors of nuclear factor κB kinase subunit α (CHUK; IKK-1; IKK-α) reported to be useful for the treatment of inflammation and cancer.
Cytokinetics Inc. has identified bicyclic piperazinones with the ability to modulate skeletal muscle contractility reported to be useful for the treatment of amyotrophic lateral sclerosis, spinal muscular atrophy, myasthenia gravis, chronic obstructive pulmonary disease, stress urinary incontinence, sarcopenia, obesity and peripheral vascular disease, among others.
Researchers at F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche Inc. have synthesized radiolabeled compounds acting as GABA(A) receptor subunit α2β2γ1 (GABRA2) positive allosteric modulators acting as positron-emission tomography (PET) and autoradiography imaging agents reported to be useful for the diagnosis of neurological disorders.