Hui-Xia Dou

TL;DR: Findings indicate that eFABP4 interferes with adipocyte differentiation, induces p 38/HSL mediated lipolysis and p38/NF-κB mediated inflammation in adipocytes in vitro and in vivo.

TL;DR: The identification of naphthalene-1-sulfonamide derivatives as novel, potent and selective FABP4 inhibitors by applying a structure-based design strategy and it is demonstrated that 16dk and 16do exhibited a dramatic improvement in glucose and lipid metabolism, by decreasing fasting blood glucose and serum lipid levels, enhancing insulin sensitivity, and ameliorating hepatic steatosis in obese diabetic (db/db) mice.

TL;DR: A series of novel tetrahydroisoquinoline derivatives were developed based on the crystal structure of PDE4D in complex with compound 1, and an in vivo study demonstrated that a topical administration of 36 achieved more significant efficacy than calcipotriol to improve the features of psoriasis-like skin inflammation.

TL;DR: A series of 2-(phenylamino)benzoic acids as novel and potent FABP4 inhibitors are rationally designed based on an interesting fragment which adopts multiple binding poses within FABp4, resulting in a promising lead with the highest binding affinity among all the inhibitors, exerting a significant anti-inflammatory effect in cells and effectively attenuating a systemic inflammatory damage in mice.

TL;DR: Two compounds A16 and B8 were identified to show inhibitory activities against both FABP4/5 and good selectivity over FABp3, which could also reduce the level of forskolin-stimulated lipolysis in mature 3T3-L1 adipocytes.