
Bioorganic and Medicinal Chemistry p. 5730 - 5737 (2012)
Update date:2022-09-26
Topics:
Mizuguchi, Takaaki
Ohara, Naho
Iida, Mika
Ninomiya, Ryunosuke
Wada, Shinji
Kiso, Yoshiaki
Saito, Kazuki
Akaji, Kenichi
Structure-activity relationships of cyclic peptides mimicking the β-hairpin structure of the 'dimerization arm' at residues 242-259 of the EGF receptor are examined. Cyclic peptides containing the arm head of the β-hairpin loop showed inhibitory activity toward the EGF receptor's dimerization. Cyclic peptides containing a Retro-Inverso sequence of the dimerization arm showed clear inhibitory effects on the dimerization in vitro and efficiently suppressed the proliferation of A431 cells, which abundantly express the EGF receptor on their surface. The effects at a specific hydrophobic site of the loop structure were expected to enhance the interactions with the receptor.
Contact:86-310-8067016
Address:East Fuhua Road,Tiexi Chemical Industrial Estate,Hebei,China
Shanghai Yudiao Chemistry Technology Co.,Ltd
Contact:0086-18964703211
Address:Building NO.5, NO.218,Rongtian Road,ganxiang town,Jinshan District,shanghai,201518,china
Nantong Kaixin Pharma Chemical Co.,Ltd.
Contact:86-513-85250786
Address:2-1103 Huachen Mansion, 111 Gongnong Road,Nantong, Jiangsu, China
Contact:0833-5590788/5590338/5590055
Address:Victory in the town of Red Star Village,Mount Emei City,industrial concentration area storage processing logistics parkpark
Contact:0833-5590788/5590338/5590055
Address:Victory in the town of Red Star Village,Mount Emei City,industrial concentration area storage processing logistics parkpark
Doi:10.1016/0022-328X(92)85006-I
(1992)Doi:10.1016/S0040-4039(01)84550-0
(1972)Doi:10.1016/j.jorganchem.2015.02.050
(2015)Doi:10.1016/0584-8539(93)80121-P
()Doi:10.1016/S0223-5234(98)80009-3
(1998)Doi:10.1021/jo301688d
(2012)