《S1PR2 inhibitors potently reverse 5-FU resistance by downregulating DPD expression in colorectal cancer》 was published in Pharmacological Research in 2020. These research results belong to Zhang, Yu-Hang; Luo, Dong-Dong; Wan, Sheng-Biao; Qu, Xian-Jun. Computed Properties of C5H6BNO2 The article mentions the following:
In this study, S1PR2 was reckoned as a brand-new GPCR target for designing inhibitors to reverse 5-FU resistance. Herein a series of pyrrolidine pyrazoles as the S1PR2 inhibitors were designed, synthesized and evaluated for their activities of anti-FU-resistance. Among them, the most promising compound JTE-013, exhibited excellent inhibition on DPD expression and potent anti-FU-resistance activity in various human cancer cell lines, along with the in vivo HCT116DPD cells xenograft model, in which the inhibition rate of 5-FU was greatly increased from 13.01%-75.87%. The underlying mechanism was uncovered that JTE-013 demonstrated an anti-FU-resistance activity by blocking S1PR2 internalization to the endoplasmic reticulum (ER), which inhibited the degradation of 5-FU into α-fluoro-β-alanine (FBAL) by downregulating tumoral DPD expression. Overall, JTE-013 could serve as the lead compound for the discovery of new anti-FU-resistance drugs. This study provides novel insights that S1PR2 inhibitors could sensitize 5-FU therapy in colorectal cancer. The experimental process involved the reaction of Pyridin-3-ylboronic acid(cas: 1692-25-7Computed Properties of C5H6BNO2)
Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridines are often used as catalysts or reagents; particular notice has been paid recently to how pyridine coordinates to metal centers enabling a wide range of valuable reactions. Computed Properties of C5H6BNO2