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== Licensing == | == Licensing == | ||
{{subst:No license from license selector|Don't know}} | {{subst:No license from license selector|Don't know}} | ||
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| + | Imatinib binds to Abl domain via six hydrogen bond interactions. This stabilizes the imatinib Bcr-Abl complex and prevents ATP from reaching its binding site.[3][7][9] The hydrogen bonds involve the pyridine-N and backbone-NH of Met-318, the aminopyrimidine and side chain hydroxyl of Thr-315, the amide-NH and side chain carboxylate of Glu-285, the carbonyl and backbone-NH of Asp-381, the protonated methylpiperazine with the backbone-carbonyl atoms of Ile-360 and His-361. Additionally, a number of van der Waals interactions contribute to binding.[7] A hydrophobic pocket is formed by amino acid residues Ile-293, Leu-298, Leu-354 and Val-379 around the phenyl ring adjacent to the piperazinyl-methyl group of imatinib.[9] At the time of its discovery, in the absence of structural information, no clear explanation for the impressive selectivity of imatinib could be found | ||
Revision as of 12:27, 10 December 2012
Licensing
{{subst:No license from license selector|Don't know}}
Imatinib binds to Abl domain via six hydrogen bond interactions. This stabilizes the imatinib Bcr-Abl complex and prevents ATP from reaching its binding site.[3][7][9] The hydrogen bonds involve the pyridine-N and backbone-NH of Met-318, the aminopyrimidine and side chain hydroxyl of Thr-315, the amide-NH and side chain carboxylate of Glu-285, the carbonyl and backbone-NH of Asp-381, the protonated methylpiperazine with the backbone-carbonyl atoms of Ile-360 and His-361. Additionally, a number of van der Waals interactions contribute to binding.[7] A hydrophobic pocket is formed by amino acid residues Ile-293, Leu-298, Leu-354 and Val-379 around the phenyl ring adjacent to the piperazinyl-methyl group of imatinib.[9] At the time of its discovery, in the absence of structural information, no clear explanation for the impressive selectivity of imatinib could be found
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| (current) | 18:24, 9 December 2012 | Cristina Murga (Talk | contribs) | 529×221 | 9 KB |
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