This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
2j9m
From Proteopedia
| Line 1: | Line 1: | ||
| - | [[Image:2j9m.jpg|left|200px]]<br /><applet load="2j9m" size=" | + | [[Image:2j9m.jpg|left|200px]]<br /><applet load="2j9m" size="350" 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 /> | ||
| Line 7: | Line 7: | ||
==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] Known structural/functional Site: <scene name='pdbsite=AC1:Py8 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 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== | ||
| Line 39: | Line 39: | ||
[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:21:15 2008'' |
Revision as of 10:21, 23 January 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 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.
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 Wed Jan 23 12:21:15 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. | 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
