| ชื่อเรื่อง | : | New tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidine |
| นักวิจัย | : | Chen, Hongyuan , Jiao, Wanting , Jones, Matthew A. , Coxon, James M. , Morton, James D. , Bickerstaffe, Roy , Pehere, Ashok D. , Zvarec, Ondrej , Abell, Andrew D. |
| คำค้น | : | - |
| หน่วยงาน | : | Nanyang Technological University, Singapore |
| ผู้ร่วมงาน | : | - |
| ปีพิมพ์ | : | 2555 |
| อ้างอิง | : | Chen, H., Jiao, W., Jones, M. A., Coxon, J. M., Morton, J. D., Bickerstaffe, R., Pehere, A. D., Zvarec, O.,& Abell, A. D. (2012). New Tripeptide-Based Macrocyclic Calpain Inhibitors Formed by N-Alkylation of Histidine. Chemistry & Biodiversity, 9(11), 2473-2484. , 1612-1872 , http://hdl.handle.net/10220/13036 , http://dx.doi.org/10.1002/cbdv.201200320 |
| ที่มา | : | - |
| ความเชี่ยวชาญ | : | - |
| ความสัมพันธ์ | : | Chemistry & biodiversity |
| ขอบเขตของเนื้อหา | : | - |
| บทคัดย่อ/คำอธิบาย | : | Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the peptide backbone are linked by a bridge containing a 1,4-disubstituted 1H-imidazole, are reported. The structure with an aldehyde at the C-terminus and the imidazole at P3, i.e., 4c, shows significant inhibitory activity against calpain 2, with an IC50 value of 238 nM. The macrocyclic aldehyde with the imidazole at the alternative P1 position, i.e., 5c, is significantly less active. The relative activities are linked to the ability of the component macrocycles to mimic a β-strand geometry that is known to favor active-site binding. This ability is defined by conformational searches and docking studies with calpain. |
| บรรณานุกรม | : |
Chen, Hongyuan , Jiao, Wanting , Jones, Matthew A. , Coxon, James M. , Morton, James D. , Bickerstaffe, Roy , Pehere, Ashok D. , Zvarec, Ondrej , Abell, Andrew D. . (2555). New tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidine.
กรุงเทพมหานคร : Nanyang Technological University, Singapore. Chen, Hongyuan , Jiao, Wanting , Jones, Matthew A. , Coxon, James M. , Morton, James D. , Bickerstaffe, Roy , Pehere, Ashok D. , Zvarec, Ondrej , Abell, Andrew D. . 2555. "New tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidine".
กรุงเทพมหานคร : Nanyang Technological University, Singapore. Chen, Hongyuan , Jiao, Wanting , Jones, Matthew A. , Coxon, James M. , Morton, James D. , Bickerstaffe, Roy , Pehere, Ashok D. , Zvarec, Ondrej , Abell, Andrew D. . "New tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidine."
กรุงเทพมหานคร : Nanyang Technological University, Singapore, 2555. Print. Chen, Hongyuan , Jiao, Wanting , Jones, Matthew A. , Coxon, James M. , Morton, James D. , Bickerstaffe, Roy , Pehere, Ashok D. , Zvarec, Ondrej , Abell, Andrew D. . New tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidine. กรุงเทพมหานคร : Nanyang Technological University, Singapore; 2555.
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