Structure-Based Anti-Inl ammatory Drug Discovery: Design, Synthesis and Biological Evaluation of VSP-22 as a New, Safe and Highly Potent GR Agonist

The glucocorticoid receptor(GR),also known as NR3C1(nuclear receptor subfamily 3,group C,member 1)is the receptor to which cortisol and other glucocorticoids bind.Many studies have also showed that it is the target protein for the well-known glucocorticoid class of anti-infl ammatory drugs such as prednisone,dexamethasone(DEX)and budesonide,which have proven successful for the effi cient treatment of infl ammation and autoimmune diseases such as asthma,arthritis,lupus,and Crohn’s disease.However,despite their excellent potencies in treating the above-mentioned diseases,these glucocorticoid drugs as GR agonists possess many severe side effects including diabetes,hypertension,obesity,and osteoporosis.Undoubtedly。

The glucocorticoid receptor （GR）, also known as NR3C1 （nuclear receptor subfamily 3, group C, member 1） is the receptor to which cortisol and other glucocorticoids bind. Many studies have also showed that it is the target protein for the well-known glucocorticoid class of anti-inflammatory drugs such as prednisone, dexamethasone （DEX） and budesonide, which have proven successful for the efficient treatment of inflammation and autoimmune diseases such as asthma,arthritis,lupus, and Crohn＇s disease.