1Z8D
 
 | | Crystal Structure of Human Muscle Glycogen Phosphorylase a with AMP and Glucose | | Descriptor: | ADENINE, ADENOSINE MONOPHOSPHATE, Glycogen phosphorylase, ... | | Authors: | Lukacs, C.M, Oikonomakos, N.G, Crowther, R.L, Hong, L.N, Kammlott, R.U, Levin, W, Li, S, Liu, C.M, Lucas-McGady, D, Pietranico, S, Reik, L. | | Deposit date: | 2005-03-30 | | Release date: | 2006-03-21 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | The crystal structure of human muscle glycogen phosphorylase a with bound glucose and AMP: An intermediate conformation with T-state and R-state features.
Proteins, 63, 2006
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1C3I
 | | HUMAN STROMELYSIN-1 CATALYTIC DOMAIN COMPLEXED WITH RO-26-2812 | | Descriptor: | 2-(2-{2-[(BIPHENYL-4-YLMETHYL)-AMINO]-3-MERCAPTO-PENTANOYLAMINO}-ACETYLAMINO)-3-METHYL-BUTYRIC ACID METHYL ESTER, CALCIUM ION, STROMELYSIN-1, ... | | Authors: | Steele, D.L, Kammlott, R.U, Crowther, R.L, Birktoft, J.J, Dunten, P, Engler, J.E. | | Deposit date: | 1999-07-27 | | Release date: | 2000-07-26 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (1.83 Å) | | Cite: | Expression, characterization and structure determination of an active site mutant (Glu202-Gln) of mini-stromelysin-1.
Protein Eng., 13, 2000
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4IPF
 | | The 1.7A crystal structure of humanized Xenopus MDM2 with RO5045337 | | Descriptor: | E3 ubiquitin-protein ligase Mdm2, SULFATE ION, [(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1H-imidazol-1-yl]{4-[3-(methylsulfonyl)propyl]piperazin-1-yl}methanone | | Authors: | Graves, B.J, Lukacs, C, Kammlott, R.U, Crowther, R. | | Deposit date: | 2013-01-09 | | Release date: | 2013-02-20 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | MDM2 Small-Molecule Antagonist RG7112 Activates p53 Signaling and Regresses Human Tumors in Preclinical Cancer Models.
Cancer Res., 73, 2013
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2FVD
 | | Cyclin Dependent Kinase 2 (CDK2) with diaminopyrimidine inhibitor | | Descriptor: | (4-AMINO-2-{[1-(METHYLSULFONYL)PIPERIDIN-4-YL]AMINO}PYRIMIDIN-5-YL)(2,3-DIFLUORO-6-METHOXYPHENYL)METHANONE, Cell division protein kinase 2 | | Authors: | Crowther, R.L, Lukacs, C.M, Kammlott, R.U. | | Deposit date: | 2006-01-30 | | Release date: | 2006-10-10 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
J.Med.Chem., 49, 2006
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3LE6
 | | The structure of cyclin dependent kinase 2 (CKD2) with a pyrazolobenzodiazepine inhibitor | | Descriptor: | 5-(2-chlorophenyl)-3-methyl-7-nitropyrazolo[3,4-b][1,4]benzodiazepine, Cell division protein kinase 2 | | Authors: | Lukacs, C.M, Swain, A, Crowther, R.L, Kammlott, R.U, Liu, J.J. | | Deposit date: | 2010-01-14 | | Release date: | 2010-11-17 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.
Bioorg.Med.Chem.Lett., 20, 2010
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4J3E
 | | The 1.9A crystal structure of humanized Xenopus Mdm2 with nutlin-3a | | Descriptor: | 4-({(4S,5R)-4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1H-imidazol-1-yl}carbonyl)piperazin-2-one, E3 ubiquitin-protein ligase Mdm2, SULFATE ION | | Authors: | Graves, B.J, Lukacs, C.M, Kammlott, R.U, Crowther, R. | | Deposit date: | 2013-02-05 | | Release date: | 2013-04-24 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.91 Å) | | Cite: | Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
ACS Med Chem Lett, 4, 2013
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