کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10771939 | 1050845 | 2005 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-based design of P3 moieties in the peptide mimetic factor VIIa inhibitor
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
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چکیده انگلیسی
Selective factor VIIa-tissue factor complex (FVIIa/TF) inhibition is seen as a promising target for developing new anticoagulant drugs. Structure-based designs of the P3 moiety in the peptide mimetic factor VIIa inhibitor successfully lead to novel inhibitors with selectivity for FVIIa/TF and extrinsic coagulation the same as or even higher than those of previously reported peptide mimetic factor VIIa inhibitors. X-ray crystal structure analysis reveals that one of the novel inhibitors shows improved selectivity by forming interactions between the inhibitor and FVIIa as expected. Another of the novel inhibitors achieves improved selectivity through an unexpected hydrogen bond with Gln217, with a unique bent conformation in FVIIa/TF accompanied by conformational changes of the inhibitor and the protein.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 327, Issue 2, 11 February 2005, Pages 589-596
Journal: Biochemical and Biophysical Research Communications - Volume 327, Issue 2, 11 February 2005, Pages 589-596
نویسندگان
Shojiro Kadono, Akihisa Sakamoto, Yasufumi Kikuchi, Masayoshi Oh-eda, Naohiro Yabuta, Kazutaka Yoshihashi, Takehisa Kitazawa, Tsukasa Suzuki, Takaki Koga, Kunihiro Hattori, Takuya Shiraishi, Masayuki Haramura, Hirofumi Kodama, Yoshiyuki Ono, Toru Esaki,