title: CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist.
abstract: Small molecules behaving as CD4 mimics were previously reported as HIV-1 entry inhibitors that block the gp120-CD4 interaction and induce a conformational change in gp120, exposing its co-receptor-binding site. A structure-activity relationship (SAR) study of a series of CD4 mimic analogs was conducted to investigate the contribution from the piperidine moiety of CD4 mimic 1 to anti-HIV activity, cytotoxicity, and CD4 mimicry effects on conformational changes of gp120. In addition, several hybrid molecules based on conjugation of a CD4 mimic analog with a selective CXCR4 antagonist were also synthesized and their utility evaluated.
authors: Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
authors: Tetsuo
authors: T
authors: Narumi
authors: Chihiro
authors: C
authors: Ochiai
authors: Kazuhisa
authors: K
authors: Yoshimura
authors: Shigeyoshi
authors: S
authors: Harada
authors: Tomohiro
authors: T
authors: Tanaka
authors: Wataru
authors: W
authors: Nomura
authors: Hiroshi
authors: H
authors: Arai
authors: Taro
authors: T
authors: Ozaki
authors: Nami
authors: N
authors: Ohashi
authors: Shuzo
authors: S
authors: Matsushita
authors: Hirokazu
authors: H
authors: Tamamura
mesh_terms: D040761:Biomimetic Materials / Q000737:chemistry* / Q000378:metabolism; D015704:CD4 Antigens / Q000737:chemistry / Q000378:metabolism; D002460:Cell Line; D015699:HIV Envelope Protein gp120 / Q000737:chemistry / Q000378:metabolism; D023581:HIV Fusion Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D006801:Humans; D010880:Piperidines / Q000737:chemistry; D011485:Protein Binding; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D023581:HIV Fusion Inhibitors; D010880:Piperidines; D019718:Receptors, CXCR4; C514793:gp120 protein, Human immunodeficiency virus 1; C032727:piperidine