2j9m
From Proteopedia
(New page: 200px<br /> <applet load="2j9m" size="450" color="white" frame="true" align="right" spinBox="true" caption="2j9m, resolution 2.50Å" /> '''CRYSTAL STRUCTURE O...) |
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| - | <applet load="2j9m" size="450" color="white" frame="true" align="right" spinBox="true" | + | |
caption="2j9m, resolution 2.50Å" /> | caption="2j9m, resolution 2.50Å" /> | ||
'''CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE'''<br /> | '''CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2J9M 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 PY8 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] | + | 2J9M 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 PY8 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] Known structural/functional Site: <scene name='pdbsite=AC1:Py8 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2J9M OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 19:56:31 2007'' |
Revision as of 17:46, 18 December 2007
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CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE
Overview
X-ray structures from CDK2-aminopyrimidine inhibitor complexes led to the, idea to stabilize the active conformation of aminopyrimidine inhibitors by, incorporating the recognition site into a macrocyclic framework. A modular, synthesis approach that relies on a new late-stage macrocyclization, protocol that enables fast and efficient synthesis of macrocyclic, aminopyrimidines was developed. A set of structurally diverse derivatives, was prepared. Macrocyclic aminopyrimidines were shown to be multitarget, inhibitors of CDK1/2 and VEGF-RTKs. In addition, potent antiproliferative, activities toward various human tumor cells and a human tumor xenograft, model were demonstrated.
About this Structure
2J9M is a Single protein structure of sequence from Homo sapiens with PY8 as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
Macrocyclic Aminopyrimidines as Multitarget CDK and VEGF-R Inhibitors with Potent Antiproliferative Activities., Lucking U, Siemeister G, Schafer M, Briem H, Kruger M, Lienau P, Jautelat R, ChemMedChem. 2007 Jan 15;2(1):63-77. PMID:17131463
Page seeded by OCA on Tue Dec 18 19:56:31 2007
Categories: Homo sapiens | Non-specific serine/threonine protein kinase | Single protein | Briem, H. | Jautelat, R. | Krueger, M. | Lienau, P. | Luecking, U. | Schaefer, M. | Siemeister, G. | PY8 | Arylamine n-acetyltransferase | Atp-binding | Cell cycle | Cell division | Drug metabolism | Isoniazid | Kinase | Mitosis | Mycobacteria | Nat | Nucleotide-binding | Phosphorylation | Polymorphism | Serine-threonine protein kinase | Serine/threonine-protein kinase | Transferase
