7QXB
 
 | | Cryo-EM map of human telomerase-DNA-TPP1-POT1 complex (sharpened map) | | 分子名称: | Adrenocortical dysplasia homolog (Mouse), isoform CRA_a, Histone H2A, ... | | 著者 | Sekne, Z, Ghanim, G.E, van Roon, A.M.M, Nguyen, T.H.D. | | 登録日 | 2022-01-26 | | 公開日 | 2022-03-02 | | 最終更新日 | 2022-03-23 | | 実験手法 | ELECTRON MICROSCOPY (3.91 Å) | | 主引用文献 | Structural basis of human telomerase recruitment by TPP1-POT1.
Science, 375, 2022
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4DDR
 | | Human dihydrofolate reductase complexed with NADPH and P218 | | 分子名称: | 3-(2-{3-[(2,4-diamino-6-ethylpyrimidin-5-yl)oxy]propoxy}phenyl)propanoic acid, Dihydrofolate reductase, NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE | | 著者 | Yuthavong, Y, Tarnchompoo, B, Vilaivan, T, Chitnumsub, P, Kamchonwongpaisan, S, Charman, S.A, McLennan, D.N, White, K.L, Vivas, L, Bongard, E, Thongphanchang, C, Taweechai, S, Vanichtanankul, J, Rattanajak, R, Arwon, U, Fantauzzi, P, Yuvaniyama, J, Charman, W.N, Matthews, D. | | 登録日 | 2012-01-19 | | 公開日 | 2012-11-14 | | 最終更新日 | 2023-11-08 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target
Proc.Natl.Acad.Sci.USA, 109, 2012
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2BED
 | | Structure of FPT bound to inhibitor SCH207736 | | 分子名称: | (11S)-8-CHLORO-11-[1-(METHYLSULFONYL)PIPERIDIN-4-YL]-6-PIPERAZIN-1-YL-11H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDINE, FARNESYL DIPHOSPHATE, Protein farnesyltransferase beta subunit, ... | | 著者 | Strickland, C. | | 登録日 | 2005-10-24 | | 公開日 | 2006-08-08 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.7 Å) | | 主引用文献 | Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.
Bioorg.Med.Chem.Lett., 16, 2006
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2E5D
 | | Crystal structure of Human NMPRTase complexed with nicotinamide | | 分子名称: | NICOTINAMIDE, Nicotinamide phosphoribosyltransferase | | 著者 | Takahashi, R, Nakamura, S, Kobayashi, Y, Ohkubo, T. | | 登録日 | 2006-12-20 | | 公開日 | 2007-12-25 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Structure and reaction mechanism of human nicotinamide phosphoribosyltransferase
J.Biochem., 147, 2010
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2E5C
 | | Crystal structure of Human NMPRTase complexed with 5'-phosphoribosyl-1'-pyrophosphate | | 分子名称: | 1-O-pyrophosphono-5-O-phosphono-alpha-D-ribofuranose, Nicotinamide phosphoribosyltransferase | | 著者 | Takahashi, R, Nakamura, S, Kobayashi, Y, Ohkubo, T. | | 登録日 | 2006-12-20 | | 公開日 | 2007-12-25 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Structure and reaction mechanism of human nicotinamide phosphoribosyltransferase
J.Biochem., 147, 2010
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3BYH
 | | Model of actin-fimbrin ABD2 complex | | 分子名称: | Actin, fimbrin ABD2 | | 著者 | Galkin, V.E, Orlova, A, Cherepanova, O, Lebart, M.C, Egelman, E.H. | | 登録日 | 2008-01-16 | | 公開日 | 2008-02-19 | | 最終更新日 | 2024-02-21 | | 実験手法 | ELECTRON MICROSCOPY (12 Å) | | 主引用文献 | High-resolution cryo-EM structure of the F-actin-fimbrin/plastin ABD2 complex.
Proc.Natl.Acad.Sci.Usa, 105, 2008
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2BDN
 | | Crystal structure of human MCP-1 bound to a blocking antibody, 11K2 | | 分子名称: | Antibody heavy chain 11K2, Antibody light chain 11K2, Small inducible cytokine A2 | | 著者 | Boriack-Sjodin, P.A, Rushe, M, Reid, C, Jarpe, M, van Vlijmen, H, Bailly, V. | | 登録日 | 2005-10-20 | | 公開日 | 2006-06-13 | | 最終更新日 | 2024-04-03 | | 実験手法 | X-RAY DIFFRACTION (2.53 Å) | | 主引用文献 | Structure activity relationships of monocyte chemoattractant proteins in complex with a blocking antibody.
Protein Eng.Des.Sel., 19, 2006
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1YVL
 | | Structure of Unphosphorylated STAT1 | | 分子名称: | 5-residue peptide, GOLD ION, Signal transducer and activator of transcription 1-alpha/beta | | 著者 | Mao, X, Ren, Z, Parker, G.N, Sondermann, H, Pastorello, M.A, Wang, W, McMurray, J.S, Demeler, B, Darnell Jr, J.E, Chen, X. | | 登録日 | 2005-02-16 | | 公開日 | 2005-03-22 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (3 Å) | | 主引用文献 | Structural bases of unphosphorylated STAT1 association and receptor binding.
Mol.Cell, 17, 2005
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2G97
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5U2M
 | | Crystal structure of human NAMPT with A-1293201 | | 分子名称: | N-[4-({[(3S)-oxolan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide, Nicotinamide phosphoribosyltransferase, SULFATE ION | | 著者 | Longenecker, K.L, Raich, D, Korepanova, A.V. | | 登録日 | 2016-11-30 | | 公開日 | 2017-06-28 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | | 主引用文献 | Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors.
Mol. Cancer Ther., 16, 2017
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5U2N
 | | Crystal structure of human NAMPT with A-1326133 | | 分子名称: | N-{4-[1-(2-methylpropanoyl)piperidin-4-yl]phenyl}-2H-pyrrolo[3,4-c]pyridine-2-carboxamide, Nicotinamide phosphoribosyltransferase, SULFATE ION | | 著者 | Longenecker, K.L, Raich, D, Korepanova, A.V. | | 登録日 | 2016-11-30 | | 公開日 | 2017-06-28 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.73 Å) | | 主引用文献 | Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors.
Mol. Cancer Ther., 16, 2017
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3S7A
 | | Human dihydrofolate reductase binary complex with PT684 | | 分子名称: | 4-({5-[(2,4-diaminopteridin-6-yl)methyl]-5H-dibenzo[b,f]azepin-2-yl}oxy)butanoic acid, Dihydrofolate reductase, SULFATE ION | | 著者 | Cody, V, Pace, J, Nowak, J. | | 登録日 | 2011-05-26 | | 公開日 | 2011-10-05 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | Structural analysis of human dihydrofolate reductase as a binary complex with the potent and selective inhibitor 2,4-diamino-6-{2'-O-(3-carboxypropyl)oxydibenz[b,f]-azepin-5-yl}methylpteridine reveals an unusual binding mode.
Acta Crystallogr.,Sect.D, 67, 2011
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5UPE
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5UPF
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3S3V
 | | human dihydrofolate reductase Q35K/N64F double mutant binary complex with trimethoprim | | 分子名称: | Dihydrofolate reductase, SULFATE ION, TRIMETHOPRIM | | 著者 | Cody, V, Pace, J, Piraino, J, Queener, S.F. | | 登録日 | 2011-05-18 | | 公開日 | 2011-09-28 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.53 Å) | | 主引用文献 | Crystallographic analysis reveals a novel second binding site for trimethoprim in active site double mutants of human dihydrofolate reductase.
J.Struct.Biol., 176, 2011
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4JR5
 | | Structure-based Identification of Ureas as Novel Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors | | 分子名称: | 1,2-ETHANEDIOL, 1-[4-(piperidin-1-ylsulfonyl)phenyl]-3-(pyridin-3-ylmethyl)thiourea, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Zheng, X, Bauer, P, Baumeister, T, Buckmelter, A.J, Caligiuri, M, Clodfelter, K.H, Han, B, Ho, Y, Kley, N, Lin, J, Reynolds, D.J, Sharma, G, Smith, C.C, Wang, Z, Dragovich, P.S, Oh, A, Wang, W, Zak, M, Gunzner-Toste, J, Zhao, G, Yuen, P, Bair, K.W. | | 登録日 | 2013-03-21 | | 公開日 | 2013-05-08 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.906 Å) | | 主引用文献 | Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (nampt) inhibitors.
J.Med.Chem., 56, 2013
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4JNM
 | | Discovery of Potent and Efficacious Urea-containing Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors with Reduced CYP2C9 Inhibition Properties | | 分子名称: | 1,2-ETHANEDIOL, 1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Gunzner-Toste, J, Zhao, G, Bauer, P, Baumeister, T, Buckmelter, A.J, Caligiuri, M, Clodfelter, K.H, Fu, B, Han, B, Ho, Y, Kley, N, Liederer, B, Lin, J, Mukadam, S, O'Brien, T, Reynolds, D.J, Sharma, G, Skelton, N, Smith, C.C, Oh, A, Wang, W, Wang, Z, Xiao, Y, Yuen, P, Zak, M, Zhang, L, Zheng, X, Bair, K.W, Dragovich, P.S. | | 登録日 | 2013-03-15 | | 公開日 | 2013-05-29 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties.
Bioorg.Med.Chem.Lett., 23, 2013
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4KFN
 | | Structure-Based Discovery of Novel Amide-Containing Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors | | 分子名称: | 1,2-ETHANEDIOL, N-[4-(piperidin-1-ylsulfonyl)benzyl]-1H-pyrrolo[3,2-c]pyridine-2-carboxamide, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Zheng, X, Bauer, P, Baumeister, T, Buckmelter, A.J, Caligiuri, M, Clodfelter, K.H, Han, B, Ho, Y, Kley, N, Lin, J, Reynolds, D.J, Sharma, G, Smith, C.C, Wang, Z, Dragovich, P.S, Gunzner-Toste, J, Liederer, B.M, Ly, J, O'Brien, T, Oh, A, Wang, L, Wang, W, Xiao, Y, Zak, M, Zhao, G, Yuen, P, Bair, K.W. | | 登録日 | 2013-04-27 | | 公開日 | 2013-05-08 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (nampt) inhibitors.
J.Med.Chem., 56, 2013
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4L4L
 | | Structural Analysis of a Phosphoribosylated Inhibitor in Complex with Human Nicotinamide Phosphoribosyltransferase | | 分子名称: | 1,2-ETHANEDIOL, 6-({4-[(3,5-difluorophenyl)sulfonyl]benzyl}carbamoyl)-1-(5-O-phosphono-beta-D-ribofuranosyl)imidazo[1,2-a]pyridin-1-ium, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Oh, A, Ho, Y, Zak, M, Liu, Y, Yuen, P, Zheng, X, Dragovich, S.P, Wang, W. | | 登録日 | 2013-06-08 | | 公開日 | 2014-06-11 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.122 Å) | | 主引用文献 | Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.
Chembiochem, 15, 2014
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4LTS
 | | Discovery of Potent and Efficacious Cyanoguanidine-containing Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors | | 分子名称: | 1,2-ETHANEDIOL, 2-cyano-1-pyridin-4-yl-3-(4-{[3-(trifluoromethoxy)phenyl]sulfonyl}benzyl)guanidine, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Zheng, X, Baumeister, T, Buckmelter, A.J, Caligiuri, M, Clodfelter, K.H, Han, B, Ho, Y, Kley, N, Lin, J, Reynoids, D.J, Sharma, G, Smith, C.C, Wang, Z, Dragovich, P.S, Oh, A, Wang, W, Zak, M, Wang, L, Yuen, P, Bair, K.W. | | 登録日 | 2013-07-23 | | 公開日 | 2013-12-25 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (1.692 Å) | | 主引用文献 | Discovery of potent and efficacious cyanoguanidine-containing nicotinamide phosphoribosyltransferase (Nampt) inhibitors.
Bioorg.Med.Chem.Lett., 24, 2014
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4LVB
 | | Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT) | | 分子名称: | 1,2-ETHANEDIOL, N-[4-(acetylamino)phenyl]cyclopropanecarboxamide, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Giannetti, A.M, Zheng, X, Skelton, N, Wang, W, Bravo, B, Feng, Y, Gunzner-Toste, J, Ho, Y, Hua, R, Wang, C, Zhao, Q, Liederer, B.M, Liu, Y, O'Brien, T, Oeh, J, Sampath, D, Shen, Y, Wang, L, Wu, H, Xiao, Y, Yuen, P, Zak, M, Zhao, G, Dragovich, P.S. | | 登録日 | 2013-07-26 | | 公開日 | 2013-09-25 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.836 Å) | | 主引用文献 | Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Bioorg.Med.Chem.Lett., 23, 2013
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4LVF
 | | Fragment-based Identification of Amides Derived From trans-2-(Pyridin-3-yl)cyclopropanecarboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT) | | 分子名称: | (1S,2S)-2-phenyl-N-(pyridin-4-yl)cyclopropanecarboxamide, 1,2-ETHANEDIOL, Nicotinamide phosphoribosyltransferase, ... | | 著者 | Giannetti, A.M, Zheng, X, Skelton, N, Wang, W, Bravo, B, Feng, Y, Gunzner-Toste, J, Ho, Y, Hua, R, Wang, C, Zhao, Q, Liederer, B.M, Liu, Y, O'Brien, T, Oeh, J, Sampath, D, Shen, Y, Wang, L, Wu, H, Xiao, Y, Yuen, P, Zak, M, Zhao, G, Dragovich, P.S. | | 登録日 | 2013-07-26 | | 公開日 | 2013-09-25 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).
Bioorg.Med.Chem.Lett., 23, 2013
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1X81
 | | Farnesyl transferase structure of Jansen compound | | 分子名称: | 6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE, Protein farnesyltransferase beta subunit, Protein farnesyltransferase/geranylgeranyltransferase type I alpha subunit, ... | | 著者 | Li, Q, Claiborne, A, Li, T, Hasvold, L, Stoll, V.S, Muchmore, S, Jakob, C.G, Gu, W, Cohen, J, Hutchins, C, Frost, D, Rosenberg, S.H, Sham, H.L. | | 登録日 | 2004-08-16 | | 公開日 | 2004-12-21 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (3.5 Å) | | 主引用文献 | Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors.
Bioorg.Med.Chem.Lett., 14, 2004
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3DGR
 | | Crystal structure of human NAMPT complexed with ADP analogue | | 分子名称: | Nicotinamide phosphoribosyltransferase, PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | | 著者 | Ho, M, Burgos, E.S, Almo, S.C, Schramm, V.L. | | 登録日 | 2008-06-15 | | 公開日 | 2009-08-18 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | A phosphoenzyme mimic, overlapping catalytic sites and reaction coordinate motion for human NAMPT.
Proc.Natl.Acad.Sci.USA, 106, 2009
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3DHF
 | | Crystal structure of phosphorylated mimic form of human NAMPT complexed with nicotinamide mononucleotide and pyrophosphate | | 分子名称: | BERYLLIUM TRIFLUORIDE ION, BETA-NICOTINAMIDE RIBOSE MONOPHOSPHATE, MAGNESIUM ION, ... | | 著者 | Ho, M, Burgos, E.S, Almo, S.C, Schramm, V.L. | | 登録日 | 2008-06-17 | | 公開日 | 2009-08-18 | | 最終更新日 | 2023-08-30 | | 実験手法 | X-RAY DIFFRACTION (1.8 Å) | | 主引用文献 | A phosphoenzyme mimic, overlapping catalytic sites and reaction coordinate motion for human NAMPT.
Proc.Natl.Acad.Sci.USA, 106, 2009
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