講演情報
[3B-2-03]Enhancing PROTAC Membrane Permeability by Combining Amide-to-Ester Substitution and Linker Methylation Strategies
*Mazin Abdelwahid1, Eisuke Hayakawa1, Keigo Hirai1, Mayumi Ishii2, Kayoko Kanamitsu2, Saori Yasuda1, Fumiaki Ohtake3,4, Shinichi Sato1,5, Shusuke Tomoshige1, Minoru Ishikawa1 (1. Graduate School of Life Sciences, Tohoku University, 2. Drug Discovery Initiative, The University of Tokyo, 3. School of Pharmacy and Pharmaceutical Sciences, Hoshi University, 4. Institute for Advanced Life Sciences, Hoshi University, 5. Frontier Research Institute for Interdisciplinary Sciences, Tohoku University)
キーワード:
PROTACs、Membrane permeability、Chameleonicity、Linker optimization、Beyond Rule of 5 (bRo5)、Medicinal chemistry
