1ctr
From Proteopedia
(New page: 200px<br /> <applet load="1ctr" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ctr, resolution 2.45Å" /> '''DRUG BINDING BY CAL...) |
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caption="1ctr, resolution 2.45Å" /> | caption="1ctr, resolution 2.45Å" /> | ||
'''DRUG BINDING BY CALMODULIN: CRYSTAL STRUCTURE OF A CALMODULIN-TRIFLUOPERAZINE COMPLEX'''<br /> | '''DRUG BINDING BY CALMODULIN: CRYSTAL STRUCTURE OF A CALMODULIN-TRIFLUOPERAZINE COMPLEX'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
- | 1CTR is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CA and TFP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1CTR is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=TFP:'>TFP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1CTR OCA]. |
==Reference== | ==Reference== | ||
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[[Category: calcium-binding protein]] | [[Category: calcium-binding protein]] | ||
- | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 15:37:12 2008'' |
Revision as of 13:37, 15 February 2008
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DRUG BINDING BY CALMODULIN: CRYSTAL STRUCTURE OF A CALMODULIN-TRIFLUOPERAZINE COMPLEX
Contents |
Overview
The crystal structure of calmodulin (CaM) bound to trifluoperazine (TFP), has been determined and refined to a resolution of 2.45 A. Only one TFP is, bound to CaM, but that is sufficient to cause distortion of the central, alpha-helix and juxtaposition of the N- and C-terminal domains similar to, that seen in CaM-polypeptide complexes. The drug makes extensive contacts, with residues in the C-terminal domain of CaM but only a few contacts with, one residue in the N-terminal domain. The structure suggests that, substrate binding to the C-terminal domain is sufficient to cause the, conformational changes in calmodulin that lead to activation of its, targets.
Disease
Known diseases associated with this structure: Cavernous malformations of CNS and retina OMIM:[604214], Cerebral cavernous malformations-1 OMIM:[604214], Hyperkeratotic cutaneous capillary-venous malformations associated with cerebral capillary malformations OMIM:[604214], Leukemia, acute T-cell lymphoblastic OMIM:[603025], Leukemia, acute myeloid OMIM:[603025]
About this Structure
1CTR is a Single protein structure of sequence from Homo sapiens with and as ligands. Full crystallographic information is available from OCA.
Reference
Drug binding by calmodulin: crystal structure of a calmodulin-trifluoperazine complex., Cook WJ, Walter LJ, Walter MR, Biochemistry. 1994 Dec 27;33(51):15259-65. PMID:7803388
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