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2j9m

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|PDB= 2j9m |SIZE=350|CAPTION= <scene name='initialview01'>2j9m</scene>, resolution 2.50&Aring;
|PDB= 2j9m |SIZE=350|CAPTION= <scene name='initialview01'>2j9m</scene>, resolution 2.50&Aring;
|SITE= <scene name='pdbsite=AC1:Py8+Binding+Site+For+Chain+A'>AC1</scene>
|SITE= <scene name='pdbsite=AC1:Py8+Binding+Site+For+Chain+A'>AC1</scene>
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|LIGAND= <scene name='pdbligand=PY8:6-BROMO-13-THIA-2,4,8,12,19-PENTAAZATRICYCLO[12.3.1.1~3,7~]NONADECA-1(18),3(19),4,6,14,16-HEXAENE 13,13-DIOXIDE'>PY8</scene>
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|LIGAND= <scene name='pdbligand=PY8:6-BROMO-13-THIA-2,4,8,12,19-PENTAAZATRICYCLO[12.3.1.1~3,7~]NONADECA-1(18),3(19),4,6,14,16-HEXAENE+13,13-DIOXIDE'>PY8</scene>
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|ACTIVITY= [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]
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|ACTIVITY= <span class='plainlinks'>[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] </span>
|GENE=
|GENE=
 +
|DOMAIN=
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|RELATEDENTRY=[[1aq1|1AQ1]], [[1b38|1B38]], [[1b39|1B39]], [[1buh|1BUH]], [[1ckp|1CKP]], [[1di8|1DI8]], [[1dm2|1DM2]], [[1e1v|1E1V]], [[1e1x|1E1X]], [[1e9h|1E9H]], [[1f5q|1F5Q]], [[1fin|1FIN]], [[1fq1|1FQ1]], [[1fvt|1FVT]], [[1fvv|1FVV]], [[1g5s|1G5S]], [[1gih|1GIH]], [[1gii|1GII]], [[1gij|1GIJ]], [[1gy3|1GY3]], [[1gz8|1GZ8]], [[1h00|1H00]], [[1h01|1H01]], [[1h07|1H07]], [[1h08|1H08]], [[1h0v|1H0V]], [[1h0w|1H0W]], [[1h1p|1H1P]], [[1h1q|1H1Q]], [[1h1r|1H1R]], [[1h1s|1H1S]], [[1h24|1H24]], [[1h25|1H25]], [[1h26|1H26]], [[1h27|1H27]], [[1h28|1H28]], [[1hck|1HCK]], [[1hcl|1HCL]], [[1jst|1JST]], [[1jsu|1JSU]], [[1jsv|1JSV]], [[1jvp|1JVP]], [[1ke5|1KE5]], [[1ke6|1KE6]], [[1ke7|1KE7]], [[1ke8|1KE8]], [[1ke9|1KE9]], [[1ogu|1OGU]], [[1oi9|1OI9]], [[1oiq|1OIQ]], [[1oir|1OIR]], [[1oit|1OIT]], [[1oiu|1OIU]], [[1oiy|1OIY]], [[1okv|1OKV]], [[1okw|1OKW]], [[1ol1|1OL1]], [[1ol2|1OL2]], [[1p2a|1P2A]], [[1p5e|1P5E]], [[1pf8|1PF8]], [[1pkd|1PKD]], [[1pw2|1PW2]], [[1pxi|1PXI]], [[1pxj|1PXJ]], [[1pxk|1PXK]], [[1pxl|1PXL]], [[1pxm|1PXM]], [[1pxn|1PXN]], [[1pxo|1PXO]], [[1pxp|1PXP]], [[1pye|1PYE]], [[1qmz|1QMZ]], [[1r78|1R78]], [[1urc|1URC]], [[1urw|1URW]], [[1v1k|1V1K]], [[1vyw|1VYW]], [[1vyz|1VYZ]], [[1w0x|1W0X]], [[1w8c|1W8C]], [[1w98|1W98]], [[1wcc|1WCC]], [[1y8y|1Y8Y]], [[1y91|1Y91]], [[1ykr|1YKR]], [[2a0c|2A0C]], [[2a4l|2A4L]], [[2b52|2B52]], [[2b53|2B53]], [[2b54|2B54]], [[2b55|2B55]], [[2bhe|2BHE]], [[2bhh|2BHH]], [[2bkz|2BKZ]], [[2bpm|2BPM]], [[2btr|2BTR]], [[2bts|2BTS]], [[2c4g|2C4G]], [[2c5n|2C5N]], [[2c5o|2C5O]], [[2c5p|2C5P]], [[2c5t|2C5T]], [[2c5v|2C5V]], [[2c5x|2C5X]], [[2c5y|2C5Y]], [[2c68|2C68]], [[2c69|2C69]], [[2c6i|2C6I]], [[2c6k|2C6K]], [[2c6l|2C6L]], [[2c6m|2C6M]], [[2c6o|2C6O]], [[2c6t|2C6T]], [[2cch|2CCH]], [[2cci|2CCI]], [[2cjm|2CJM]], [[2clx|2CLX]], [[2exm|2EXM]], [[2iw6|2IW6]], [[2iw8|2IW8]], [[2iw9|2IW9]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2j9m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2j9m OCA], [http://www.ebi.ac.uk/pdbsum/2j9m PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2j9m RCSB]</span>
}}
}}
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[[Category: Schaefer, M.]]
[[Category: Schaefer, M.]]
[[Category: Siemeister, G.]]
[[Category: Siemeister, G.]]
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[[Category: PY8]]
 
[[Category: arylamine n-acetyltransferase]]
[[Category: arylamine n-acetyltransferase]]
[[Category: atp-binding]]
[[Category: atp-binding]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 17:39:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:55:01 2008''

Revision as of 00:55, 31 March 2008

Image:2j9m.jpg


PDB ID 2j9m

Drag the structure with the mouse to rotate
, resolution 2.50Å
Sites:
Ligands:
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Related: 1AQ1, 1B38, 1B39, 1BUH, 1CKP, 1DI8, 1DM2, 1E1V, 1E1X, 1E9H, 1F5Q, 1FIN, 1FQ1, 1FVT, 1FVV, 1G5S, 1GIH, 1GII, 1GIJ, 1GY3, 1GZ8, 1H00, 1H01, 1H07, 1H08, 1H0V, 1H0W, 1H1P, 1H1Q, 1H1R, 1H1S, 1H24, 1H25, 1H26, 1H27, 1H28, 1HCK, 1HCL, 1JST, 1JSU, 1JSV, 1JVP, 1KE5, 1KE6, 1KE7, 1KE8, 1KE9, 1OGU, 1OI9, 1OIQ, 1OIR, 1OIT, 1OIU, 1OIY, 1OKV, 1OKW, 1OL1, 1OL2, 1P2A, 1P5E, 1PF8, 1PKD, 1PW2, 1PXI, 1PXJ, 1PXK, 1PXL, 1PXM, 1PXN, 1PXO, 1PXP, 1PYE, 1QMZ, 1R78, 1URC, 1URW, 1V1K, 1VYW, 1VYZ, 1W0X, 1W8C, 1W98, 1WCC, 1Y8Y, 1Y91, 1YKR, 2A0C, 2A4L, 2B52, 2B53, 2B54, 2B55, 2BHE, 2BHH, 2BKZ, 2BPM, 2BTR, 2BTS, 2C4G, 2C5N, 2C5O, 2C5P, 2C5T, 2C5V, 2C5X, 2C5Y, 2C68, 2C69, 2C6I, 2C6K, 2C6L, 2C6M, 2C6O, 2C6T, 2CCH, 2CCI, 2CJM, 2CLX, 2EXM, 2IW6, 2IW8, 2IW9


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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

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