1G1U
 
 | | THE 2.5 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE RXRALPHA LIGAND BINDING DOMAIN IN TETRAMER IN THE ABSENCE OF LIGAND | | Descriptor: | RETINOIC ACID RECEPTOR RXR-ALPHA | | Authors: | Gampe Jr, R.T, Montana, V.G, Lambert, M.H, Wisely, G.B, Milburn, M.V, Xu, H.E. | | Deposit date: | 2000-10-13 | | Release date: | 2001-04-25 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix.
Genes Dev., 14, 2000
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1G5Y
 | | THE 2.0 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE RXRALPHA LIGAND BINDING DOMAIN TETRAMER IN THE PRESENCE OF A NON-ACTIVATING RETINOIC ACID ISOMER. | | Descriptor: | RETINOIC ACID, RETINOIC ACID RECEPTOR RXR-ALPHA | | Authors: | Gampe Jr, R.T, Montana, V.G, Lambert, M.H, Wisely, G.B, Milburn, M.V, Xu, H.E. | | Deposit date: | 2000-11-02 | | Release date: | 2001-05-02 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix.
Genes Dev., 14, 2000
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1FM9
 | | THE 2.1 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE HETERODIMER OF THE HUMAN RXRALPHA AND PPARGAMMA LIGAND BINDING DOMAINS RESPECTIVELY BOUND WITH 9-CIS RETINOIC ACID AND GI262570 AND CO-ACTIVATOR PEPTIDES. | | Descriptor: | (9cis)-retinoic acid, 2-(2-BENZOYL-PHENYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA, ... | | Authors: | Gampe Jr, R.T, Montana, V.G, Lambert, M.H, Miller, A.B, Bledsoe, R.K, Milburn, M.V, Kliewer, S.A, Willson, T.M, Xu, H.E. | | Deposit date: | 2000-08-16 | | Release date: | 2001-02-16 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.
Mol.Cell, 5, 2000
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1FM6
 | | THE 2.1 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE HETERODIMER OF THE HUMAN RXRALPHA AND PPARGAMMA LIGAND BINDING DOMAINS RESPECTIVELY BOUND WITH 9-CIS RETINOIC ACID AND ROSIGLITAZONE AND CO-ACTIVATOR PEPTIDES. | | Descriptor: | (9cis)-retinoic acid, 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), ... | | Authors: | Gampe Jr, R.T, Montana, V.G, Lambert, M.H, Miller, A.B, Bledsoe, R.K, Milburn, M.V, Kliewer, S.A, Willson, T.M, Xu, H.E. | | Deposit date: | 2000-08-16 | | Release date: | 2001-02-16 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.
Mol.Cell, 5, 2000
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2AO6
 | | Crystal structure of the human androgen receptor ligand binding domain bound with TIF2(iii) 740-753 peptide and R1881 | | Descriptor: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, 14-mer fragment of Nuclear receptor coactivator 2, androgen receptor | | Authors: | He, B, Gampe Jr, R.T, Kole, A.J, Hnat, A.T, Stanley, T.B, An, G, Stewart, E.L, Kalman, R.I, Minges, J.T, Wilson, E.M. | | Deposit date: | 2005-08-12 | | Release date: | 2005-08-30 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.89 Å) | | Cite: | Structural basis for androgen receptor interdomain and coactivator interactions suggests a transition in nuclear receptor activation function dominance
Mol.Cell, 16, 2004
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1XOW
 | | Crystal structure of the human androgen receptor ligand binding domain bound with an androgen receptor NH2-terminal peptide, AR20-30, and R1881 | | Descriptor: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, androgen receptor, decamer fragment of androgen receptor | | Authors: | He, B, Gampe Jr, R.T, Kole, A.J, Hnat, A.T, Stanley, T.B, An, G, Stewart, E.L, Kalman, R.I, Minges, J.T, Wilson, E.M. | | Deposit date: | 2004-10-07 | | Release date: | 2004-11-16 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structural basis for androgen receptor interdomain and coactivator interactions suggests a transition in nuclear receptor activation function dominance
Mol.Cell, 16, 2004
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1XQ3
 | | Crystal structure of the human androgen receptor ligand binding domain bound with R1881 | | Descriptor: | (17BETA)-17-HYDROXY-17-METHYLESTRA-4,9,11-TRIEN-3-ONE, androgen receptor | | Authors: | He, B, Gampe Jr, R.T, Kole, A.J, Hnat, A.T, Stanley, T.B, An, G, Stewart, E.L, Kalman, R.I, Minges, J.T, Wilson, E.M. | | Deposit date: | 2004-10-11 | | Release date: | 2004-11-16 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | Structural basis for androgen receptor interdomain and coactivator interactions suggests a transition in nuclear receptor activation function dominance
Mol.Cell, 16, 2004
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1RDT
 | | Crystal Structure of a new rexinoid bound to the RXRalpha ligand binding doamin in the RXRalpha/PPARgamma heterodimer | | Descriptor: | (S)-(2E)-3[4-(5,5,8,8-TETRAMETHYL-5,6,7,8-TETRAHYDRO-2-NAPHTHALENYL)TETRAHYDRO-1-BENZOFURAN-2-YL]-2-PROPENOIC ACID, 2-(2-BENZOYL-PHENYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, LxxLL motif coactivator, ... | | Authors: | Haffner, C.D, Lenhard, J.M, Miller, A.B, McDougald, D.L, Dwornik, K, Ittoop, O.R, Gampe Jr, R.T, Xu, H.E, Blanchard, S, Montana, V.G. | | Deposit date: | 2003-11-06 | | Release date: | 2004-11-09 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Structure-based design of potent retinoid X receptor alpha agonists.
J.Med.Chem., 47, 2004
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1K74
 | | The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides. | | Descriptor: | (9cis)-retinoic acid, 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, Peroxisome proliferator activated receptor gamma, ... | | Authors: | Xu, H.E, Lambert, M.H, Montana, V.G, Moore, L.B, Collins, J.L, Oplinger, J.A, Kliewer, S.A, Gampe Jr, R.T, McKee, D.D, Moore, J.T, Willson, T.M. | | Deposit date: | 2001-10-18 | | Release date: | 2001-12-05 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
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1K7L
 | | The 2.5 Angstrom resolution crystal structure of the human PPARalpha ligand binding domain bound with GW409544 and a co-activator peptide. | | Descriptor: | 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, Peroxisome proliferator activated receptor alpha, YTTRIUM (III) ION, ... | | Authors: | Xu, H.E, Lambert, M.H, Montana, V.G, Moore, L.B, Collins, J.L, Oplinger, J.A, Kliewer, S.A, Gampe Jr, R.T, McKee, D.D, Moore, J.T, Willson, T.M. | | Deposit date: | 2001-10-19 | | Release date: | 2001-12-05 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
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3L0E
 | | X-ray crystal structure of a Potent Liver X Receptor Modulator | | Descriptor: | N-(2-chloro-6-fluorobenzyl)-1-methyl-N-{[3'-(methylsulfonyl)biphenyl-4-yl]methyl}-1H-imidazole-4-sulfonamide, Nuclear receptor coactivator 2, Oxysterols receptor LXR-beta | | Authors: | Gampe Jr, R.T. | | Deposit date: | 2009-12-09 | | Release date: | 2010-04-07 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
J.Med.Chem., 53, 2010
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1FVT
 | | THE STRUCTURE OF CYCLIN-DEPENDENT KINASE 2 (CDK2) IN COMPLEX WITH AN OXINDOLE INHIBITOR | | Descriptor: | 4-[(2Z)-2-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazinyl]benzene-1-sulfonamide, CELL DIVISION PROTEIN KINASE 2 | | Authors: | Davis, S.T, Benson, B.G, Bramson, H.N, Chapman, D.E, Dickerson, S.H, Dold, K.M, Eberwein, D.J, Edelstein, M, Frye, S.V, Gampe Jr, R.T, Griffin, R.J, Harris, P.A, Hassell, A.M, Holmes, W.D, Hunter, R.N, Knick, V.B, Lackey, K, Lovejoy, B, Luzzio, M.J, Murray, D, Parker, P, Rocque, W.J, Shewchuk, L, Veal, J.M, Walker, D.H, Kuyper, L.K. | | Deposit date: | 2000-09-20 | | Release date: | 2001-01-17 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors.
Science, 291, 2001
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1FVV
 | | THE STRUCTURE OF CDK2/CYCLIN A IN COMPLEX WITH AN OXINDOLE INHIBITOR | | Descriptor: | 4-[(7-OXO-7H-THIAZOLO[5,4-E]INDOL-8-YLMETHYL)-AMINO]-N-PYRIDIN-2-YL-BENZENESULFONAMIDE, CYCLIN A, CYCLIN-DEPENDENT KINASE 2 | | Authors: | Davis, S.T, Benson, B.G, Bramson, H.N, Chapman, D.E, Dickerson, S.H, Dold, K.M, Eberwein, D.J, Edelstein, M, Frye, S.V, Gampe Jr, R.T, Griffin, R.J, Harris, P.A, Hassell, A.M, Holmes, W.D, Hunter, R.N, Knick, V.B, Lackey, K, Lovejoy, B, Luzzio, M.J, Murray, D, Parker, P, Rocque, W.J, Shewchuk, L, Veal, J.M, Walker, D.H, Kuyper, L.K. | | Deposit date: | 2000-09-20 | | Release date: | 2001-01-17 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Prevention of chemotherapy-induced alopecia in rats by CDK inhibitors.
Science, 291, 2001
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1HCT
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1HCS
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1KE8
 | | CYCLIN-DEPENDENT KINASE 2 (CDK2) COMPLEXED WITH 4-{[(2-OXO-1,2-DIHYDRO-3H-INDOL-3-YLIDENE)METHYL]AMINO}-N-(1,3-THIAZOL-2-YL)BENZENESULFONAMIDE | | Descriptor: | 4-{[(2-OXO-1,2-DIHYDRO-3H-INDOL-3-YLIDENE)METHYL]AMINO}-N-(1,3-THIAZOL-2-YL)BENZENESULFONAMIDE, CELL DIVISION PROTEIN KINASE 2 | | Authors: | Bramson, H.N, Corona, J, Davis, S.T, Dickerson, S.H, Edelstein, M, Frye, S.V, Gampe, R.T, Hassell, A.M, Shewchuk, L.M, Kuyper, L.F. | | Deposit date: | 2001-11-14 | | Release date: | 2002-05-14 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
J.Med.Chem., 44, 2001
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1KE6
 | | CYCLIN-DEPENDENT KINASE 2 (CDK2) COMPLEXED WITH N-METHYL-{4-[2-(7-OXO-6,7-DIHYDRO-8H-[1,3]THIAZOLO[5,4-E]INDOL-8-YLIDENE)HYDRAZINO]PHENYL}METHANESULFONAMIDE | | Descriptor: | Cell division protein kinase 2, N-METHYL-{4-[2-(7-OXO-6,7-DIHYDRO-8H-[1,3]THIAZOLO[5,4-E]INDOL-8-YLIDENE)HYDRAZINO]PHENYL}METHANESULFONAMIDE | | Authors: | Bramson, H.N, Corona, J, Davis, S.T, Dickerson, S.H, Edelstein, M, Frye, S.V, Gampe, R.T, Hassell, A.H, Shewchuk, L.M, Kuyper, L.F. | | Deposit date: | 2001-11-14 | | Release date: | 2002-05-14 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
J.Med.Chem., 44, 2001
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1KE9
 | | CYCLIN-DEPENDENT KINASE 2 (CDK2) COMPLEXED WITH 3-{[4-({[AMINO(IMINO)METHYL]AMINOSULFONYL)ANILINO]METHYLENE}-2-OXO-2,3-DIHYDRO-1H-INDOLE | | Descriptor: | 3-{[4-([AMINO(IMINO)METHYL]AMINOSULFONYL)ANILINO]METHYLENE}-2-OXO-2,3-DIHYDRO-1H-INDOLE, Cell division protein kinase 2 | | Authors: | Bramson, H.N, Corona, J, Davis, S.T, Dickerson, S.H, Edelstein, M, Frye, S.V, Gampe, R.T, Hassell, A.M, Shewchuk, L.M, Kuyper, L.F. | | Deposit date: | 2001-11-14 | | Release date: | 2002-05-14 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
J.Med.Chem., 44, 2001
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1KE7
 | | CYCLIN-DEPENDENT KINASE 2 (CDK2) COMPLEXED WITH 3-{[(2,2-DIOXIDO-1,3-DIHYDRO-2-BENZOTHIEN-5-YL)AMINO]METHYLENE}-5-(1,3-OXAZOL-5-YL)-1,3-DIHYDRO-2H-INDOL-2-ONE | | Descriptor: | 3-{[(2,2-DIOXIDO-1,3-DIHYDRO-2-BENZOTHIEN-5-YL)AMINO]METHYLENE}-5-(1,3-OXAZOL-5-YL)-1,3-DIHYDRO-2H-INDOL-2-ONE, Cell division protein kinase 2 | | Authors: | Bramson, H.N, Corona, J, Davis, S.T, Dickerson, S.H, Edelstein, M, Frye, S.V, Gampe, R.T, Hassell, A.H, Shewchuk, L.M, Kuyper, L.F. | | Deposit date: | 2001-11-14 | | Release date: | 2002-05-14 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
J.Med.Chem., 44, 2001
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1KE5
 | | CDK2 complexed with N-methyl-4-{[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]amino}benzenesulfonamide | | Descriptor: | Cell division protein kinase 2, N-METHYL-4-{[(2-OXO-1,2-DIHYDRO-3H-INDOL-3-YLIDENE)METHYL]AMINO}BENZENESULFONAMIDE | | Authors: | Bramson, H.N, Corona, J, Davis, S.T, Dickerson, S.H, Edelstein, M, Frye, S.V, Gampe, R.T, Hassell, A.M, Shewchuk, L.M, Kuyper, L.F. | | Deposit date: | 2001-11-14 | | Release date: | 2002-05-14 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
J.Med.Chem., 44, 2001
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