Post by Discngine

𝗔 𝘀𝘁𝗿𝘂𝗰𝘁𝘂𝗿𝗲-𝗴𝘂𝗶𝗱𝗲𝗱 𝗽𝗮𝘁𝗵 𝘁𝗼 𝗮 𝘀𝗲𝗹𝗲𝗰𝘁𝗶𝘃𝗲, 𝗯𝗿𝗮𝗶𝗻-𝗽𝗲𝗻𝗲𝘁𝗿𝗮𝗻𝘁 𝗣𝗥𝗠𝗧𝟱 𝗶𝗻𝗵𝗶𝗯𝗶𝘁𝗼𝗿 Our June Protein of the Month is PRMT5 (protein arginine methyltransferase 5) - a target involved in glioblastoma which is an area of highly unmet medical need. TNG456, a highly potent, selective, and brain-penetrant PRMT5 inhibitor by Tango Therapeutics, has recently entered Phase 1/2 trials. It follows TNG908, an earlier candidate whose limited brain penetration prevented further clinical development. Medicinal chemistry strategies combined with structural insights into the PRMT5–MTA complex have guided the optimization of TNG456, helping shape its selectivity and brain penetrance. Learn more about PRMT5 and TNG456's key structural and optimization insights in the article here: https://bit.ly/4eYFGvA ℹ️ 𝘞𝘩𝘢𝘵 𝘪𝘴 𝘵𝘩𝘦 𝘗𝘳𝘰𝘵𝘦𝘪𝘯 𝘰𝘧 𝘵𝘩𝘦 𝘔𝘰𝘯𝘵𝘩 𝘚𝘦𝘳𝘪𝘦𝘴? - Each month, we spotlight exciting structural discoveries of existing and emerging drug targets that inspire innovative drug design. #drugdiscovery #3decision #POM #SBDD #PRMT5 #TNG456 #oncology