title: Hydrophobic modifications at 1-phosphate of inositol 1,4,5-trisphosphate analogues enhance receptor binding.
abstract: Inositol 1,4,5-trisphosphate (IP(3)) analogues were synthesized in order to investigate the importance of the environment of 1-phosphate of IP(3) for strong binding to the IP(3) receptor. Our results show that hydrophobic modifications of the 1-phosphate moiety enhance the binding affinity, with considerable latitude of substituent structure.
authors.affiliation: Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan.
authors.forename: Waka
authors.initials: W
authors.lastname: Nakanishi
authors.forename: Kazuya
authors.initials: K
authors.lastname: Kikuchi
authors.forename: Takanari
authors.initials: T
authors.lastname: Inoue
authors.forename: Kenzo
authors.initials: K
authors.lastname: Hirose
authors.forename: Masamitsu
authors.initials: M
authors.lastname: Iino
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Nagano
mesh_terms: D000818:Animals; D015220:Calcium Channels / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D015544:Inositol 1,4,5-Trisphosphate / Q000031:analogs & derivatives* / Q000378:metabolism; D053496:Inositol 1,4,5-Trisphosphate Receptors; D008958:Models, Molecular; D011485:Protein Binding; D018160:Receptors, Cytoplasmic and Nuclear / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D015220:Calcium Channels; C506926:ITPR1 protein, human; D053496:Inositol 1,4,5-Trisphosphate Receptors; D018160:Receptors, Cytoplasmic and Nuclear; D015544:Inositol 1,4,5-Trisphosphate