pf-8380 has been researched along with Pulmonary-Fibrosis* in 2 studies
2 other study(ies) available for pf-8380 and Pulmonary-Fibrosis
| Article | Year |
|---|---|
Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great
Autotaxin (ATX) is the dominant catalytic enzyme accounting for the lipid mediator lysophosphatidic acid (LPA) through hydrolysis of lysophosphatidylcholine (LPC). There is great interest in developing nonacidic ATX inhibitors with a specific binding mode to serve as potential Topics: Allosteric Site; Animals; Binding Sites; Bleomycin; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Discovery; Enzyme Inhibitors; High-Throughput Screening Assays; Humans; Hydrazones; Indoles; Male; Mice, Inbred C57BL; Models, Molecular; Phosphoric Diester Hydrolases; Protein Conformation; Pulmonary Fibrosis; Structure-Activity Relationship | 2020 |
Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit in Vivo Efficacy in a Pulmonary Fibrosis Model.
Autotaxin (ATX) catalyzes the hydrolysis of lysophosphatidylcholine (LPC) generating the lipid mediator lysophosphatidic acid (LPA). Both ATX and LPA are involved in various pathological inflammatory conditions, including fibrosis and cancer, and have attracted great interest as medicinal targets over the past decade. Thus, the development of novel potent ATX inhibitors is of great importance. We have developed a novel class of ATX inhibitors containing the zinc binding functionality of hydroxamic acid. Such novel hydroxamic acids that incorporate a non-natural δ-amino acid residue exhibit high in vitro inhibitory potency over ATX (IC Topics: Animals; Bleomycin; Catalytic Domain; Drug Design; Hydroxamic Acids; Mice; Molecular Docking Simulation; Molecular Structure; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Pulmonary Fibrosis; Structure-Activity Relationship | 2018 |