The protease mucosa-associated lymphoid tissue lymphoma translocation 1 (MALT1) is a signaling protein with both molecular scaffolding and protease activity involved in lymphocyte activation. MALT1 is considered a therapeutic target for chronic lymphocytic leukemia (CLL) in patients who develop resistance to Bruton tyrosine kinase (BTK) inhibitors.
Gait instability and somnolence are the main hindbrain-related adverse effects associated with the inhibition of AMPA receptors (AMPARs). Transmembrane AMPAR regulatory proteins (TARPs) modulate AMPAR function, with the specific member TARPγ8 being highly expressed in brain regions associated with seizures and expressed at low or negligible levels in the hindbrain.
Pimavanserin is a 5-HT2A inverse agonist that is FDA approved for treating Parkinson’s disease psychosis. Acadia Pharmaceuticals Inc. searched for a compound that relies on pimavanserin but with an improved profile, including shorter half-life and reduced QT prolongation risk, which led to the identification of ACP-204.
Beigene Co. Ltd. has presented data on a CDK4 selective inhibitor, BGB-43395, for the potential treatment of this cancer type and which would reduce the neutropenia associated with CDK6 inhibition.
Recent research has established that Insulin-like Growth Factor 2 mRNA Binding Protein 3 (IGF2BP3) RNA-binding protein is involved in leukemia development, particularly in the KMT2A-translocated B-acute lymphoblastic leukemia (B-ALL) subtype.
The regular use of agonists of the μ-opioid receptor for acute pain relief usually leads to tolerance, respiratory depression, constipation and importantly, abuse potential.
Researchers from Atyr Pharma Inc. presented preclinical efficacy data of ATYR-0101, a potential therapeutic biologic based on a domain appended to aspartyl-tRNA synthetase (DARS) in models of lung and kidney fibrosis. By targeting latent-transforming growth factor beta-binding protein 1 (LTBP-1), ATYR-0101 induced apoptosis in myofibroblasts which play a central role in fibrosis and tissue remodeling.
Researchers from Engrail Therapeutics Inc. recently described the pharmacological characterization of ENX-105, a new class of molecule that combines 5-HT1A/2A receptor agonism with D2/3 receptor antagonism, to be used for its antianhedonic and antipsychotic effects.
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