title: Identification of a new class of low molecular weight antagonists against the chemokine receptor CXCR4 having the dipicolylamine-zinc(II) complex structure.
abstract: Several low molecular weight nonpeptide compounds having the dipicolylamine-zinc(II) complex structure were identified as potent and selective antagonists of the chemokine receptor CXCR4. These compounds showed strong inhibitory activity against CXCL12 binding to CXCR4, and the top compound exhibited significant anti-HIV activity. Zinc(II)-dipicolylamine unit-containing compounds proved to be useful and attractive lead compounds for chemotherapy of these diseases as nonpeptide CXCR4 antagonists possessing the novel scaffold structure.
authors.affiliation: Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan. tamamura.mr@tmd.ac.jp
authors.forename: Hirokazu
authors.initials: H
authors.lastname: Tamamura
authors.forename: Akio
authors.initials: A
authors.lastname: Ojida
authors.forename: Teppei
authors.initials: T
authors.lastname: Ogawa
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tsutsumi
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Masuno
authors.forename: Hideki
authors.initials: H
authors.lastname: Nakashima
authors.forename: Naoki
authors.initials: N
authors.lastname: Yamamoto
authors.forename: Itaru
authors.initials: I
authors.lastname: Hamachi
authors.forename: Nobutaka
authors.initials: N
authors.lastname: Fujii
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D003412:Cricetulus; D015497:HIV-1 / Q000187:drug effects; D008958:Models, Molecular; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010847:Picolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors*; D015032:Zinc
chemical_list: D019380:Anti-HIV Agents; D002614:Chelating Agents; D009942:Organometallic Compounds; D010847:Picolines; D019718:Receptors, CXCR4; C509592:zinc(II) dipicolylamine; D015032:Zinc; D002118:Calcium