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. Author manuscript; available in PMC: 2021 May 24.
Published in final edited form as: Science. 2020 Mar 19;368(6489):387–394. doi: 10.1126/science.aaz8455

Fig. 5. GSK620 is efficacious in preclinical models of immuno-inflammation.

Fig. 5

(A) Chemical structure of the BD2-selective BET inhibitor in vivo tool GSK620. (B) Compound binding to the individual tandem bromodomains (BD1 (orange) and BD2(cyan)) of BRD2, 3, 4 and T determined using TR-FRET. Data are the mean ± SEM (n = 12-21). (C) Phylogenetic tree of bromodomain family demonstrating preferential compound binding for the BD2 domains of the BET family of proteins using the BROMOscan bromodomain competition binding assay. Red dots represent KD values. (D) Mouse imiquimod (IMQ)-induced psoriasis study design. (E) Histology H&P (Hematoxylin-Phloxin) staining of skin sections (F) GSK620 (20mg/kg, p.o., QD) reduces the psoriasis score, (G) the epidermal thickness and (H) the expression levels of inflammatory genes in skin biopsies. V, vehicle; Vani,vanicream; Apremilast (20 mg/kg, p.o., BID). Data represent the mean ± SEM (n = 10). One-way ANOVA followed by Dunnett’s multiple comparison test (***P<0.0001 vs V + IMQ).