Chronic kidney disease (CKD) affects hundreds of millions of people worldwide. A common phenomenon is the presence of large amounts of high molecular weight plasma proteins in the urine. In this article, we will introduce a small molecule — Bis-T-23. It is an HIV-I Integrase inhibitor for HIV and CKD research.
Bis-T-23 (AG1717) is an HIV-I integrase inhibitor that can be used for the research of HIV and CKD.
In generally, the pol gene of the human immunodeficiency virus (HIV) encode three viral enzymes. They play key roles in the virus replication cycle. Bis-T-23 is an HIV-I Integrase inhibitor. On the one hand, Bis-T-23 (0.18 μM) can inhibit HIV-1 Integrase. On the other hand, Bis-T-23 (2 μM) can inhibit the binding of Integrase to the substrate DNA.
Furthermore, Bis-T-23 can promote actin-dependent dynamin oligomerization and thus increased actin polymerization in injured podocytes. It is sufficient to improve renal health in diverse models of both transient kidney disease and CKD. Firstly, Bis-T-23 (1 ng) targets actin-dependent dynamin oligomerization in podocytes to promote proper GFB function. Secondly, Bis-T-23 (i.p.; 20, 40 mg/kg) ameliorates proteinuria by altering actin dynamics. Furthermore, Bis-T-23 (i.p.; 20, 40 mg/kg) ameliorates or prevented proteinuria and diminished mesangial matrix expansion in diverse genetic and chronic models of glomerular disease in rodents.
In a word, Bis-T-23 is a tyrphostin derivative and can be used for the research of HIV and CKD.