2j9m
From Proteopedia
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| - | | | + | {{STRUCTURE_2j9m| PDB=2j9m | SCENE= }} |
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'''CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE''' | '''CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE''' | ||
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[[Category: Schaefer, M.]] | [[Category: Schaefer, M.]] | ||
[[Category: Siemeister, G.]] | [[Category: Siemeister, G.]] | ||
| - | [[Category: | + | [[Category: Arylamine n-acetyltransferase]] |
| - | [[Category: | + | [[Category: Atp-binding]] |
| - | [[Category: | + | [[Category: Cell cycle]] |
| - | [[Category: | + | [[Category: Cell division]] |
| - | [[Category: | + | [[Category: Drug metabolism]] |
| - | [[Category: | + | [[Category: Isoniazid]] |
| - | [[Category: | + | [[Category: Kinase]] |
| - | [[Category: | + | [[Category: Mitosis]] |
| - | [[Category: | + | [[Category: Mycobacteria]] |
| - | [[Category: | + | [[Category: Nat]] |
| - | [[Category: | + | [[Category: Nucleotide-binding]] |
| - | [[Category: | + | [[Category: Phosphorylation]] |
| - | [[Category: | + | [[Category: Polymorphism]] |
| - | [[Category: | + | [[Category: Serine-threonine protein kinase]] |
| - | [[Category: | + | [[Category: Serine/threonine-protein kinase]] |
| - | [[Category: | + | [[Category: Transferase]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 08:33:44 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 05:33, 4 May 2008
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. 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 Sun May 4 08:33:44 2008
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. | 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
