2j9m: Difference between revisions
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[[Image:2j9m.jpg|left|200px]] | [[Image:2j9m.jpg|left|200px]] | ||
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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
Proteopedia Page Contributors and Editors (what is this?)
Categories:
- Pages with broken file links
- 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
