Publications by authors named "Zhikan Xia"
The adenosine A receptor (AAR), a key member of the G protein-coupled receptor family, is a promising therapeutic target for inflammatory and cancerous conditions. The selective AAR agonists, CF101 and CF102, are clinically significant, yet their recognition mechanisms remained elusive. Here we report the cryogenic electron microscopy structures of the full-length human AAR bound to CF101 and CF102 with heterotrimeric G protein in complex at 3.
View Article and Find Full Text PDFGPR84 regulates pulmonary inflammation by modulating neutrophil functions.
Acta Pharmacol Sin
August 2023
Acute lung injury (ALI) is an acute, progressive hypoxic respiratory failure that could develop into acute respiratory distress syndrome (ARDS) with very high mortality rate. ALI is believed to be caused by uncontrolled inflammation, and multiple types of immune cells, especially neutrophils, are critically involved in the development of ALI. The treatment for ALI/ARDS is very limited, a better understanding of the pathogenesis and new therapies are urgently needed.
View Article and Find Full Text PDFArticle Synopsis
- - GPR40, found in pancreatic β-cells, enhances insulin secretion and improves blood sugar control when activated by specific fatty acids or synthetic drugs, but concerns about liver toxicity have arisen from prior clinical trials.
- - Many GPR40 agonists are too fat-soluble, risking harmful side effects, prompting researchers to seek safer alternatives with better efficacy and selectivity for therapeutic applications.
- - A new drug design approach incorporating sulfoxide into a core structure has resulted in promising GPR40 agonists with improved effectiveness and safety, as shown by successful tests in mice that lowered blood sugar levels and minimized liver toxicity.