2j9m: Difference between revisions
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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 <scene name='pdbligand=PY8:'>PY8</scene> 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://oca.weizmann.ac.il/oca-bin/ocashort?id=2J9M OCA]. | 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 <scene name='pdbligand=PY8:'>PY8</scene> 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://oca.weizmann.ac.il/oca-bin/ocashort?id=2J9M OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
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Revision as of 11:43, 3 February 2008
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CRYSTAL STRUCTURE OF CDK2 IN COMPLEX WITH MACROCYCLIC AMINOPYRIMIDINE
OverviewOverview
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 StructureAbout this Structure
2J9M is a Single protein structure of sequence from Homo sapiens with 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.
ReferenceReference
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
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Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- 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.
- 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