362477-50-7Relevant academic research and scientific papers
Encounter with unexpected collagenase-1 selective inhibitor: Switchover of inhibitor binding pocket induced by fluorine atom
Sawa, Masaaki,Kondo, Hirosato,Nishimura, Shinichiro
, p. 581 - 584 (2007/10/03)
Phosphonamide-based inhibitors having trifluoromethyl moiety showed highly selective inhibition against MMP-1. A possible mechanism of the selectivity of MMP-1 inhibitors through the switchover of the binding pocket was speculated by computational calculations. As a consequence of the unexpected selectivity, the specific interaction of CF3 group of the inhibitor and Arg214 in the S1′ pocket of MMP-1 conducted a low binding energy.
New type of metalloproteinase inhibitor: Design and synthesis of new phosphonamide-based hydroxamic acids
Sawa, Masaaki,Kiyoi, Takao,Kurokawa, Kiriko,Kumihara, Hiroshi,Yamamoto, Minoru,Miyasaka, Tomohiro,Ito, Yasuko,Hirayama, Ryoichi,Inoue, Tomomi,Kirii, Yasuyuki,Nishiwaki, Eiji,Ohmoto, Hiroshi,Maeda, Yu,Ishibushi, Etsuko,Inoue, Yoshimasa,Yoshino, Kohichiro,Kondo, Hirosato
, p. 919 - 929 (2007/10/03)
A series of phosphonamide-based hydroxamate derivatives were synthesized, and the inhibitory activities were evaluated against various metalloproteinases in order to clarify its selectivity profile. Among the four diastereomeric isomers resulting from the
