2E5B
 
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2E5D
 | | Crystal structure of Human NMPRTase complexed with nicotinamide | | Descriptor: | NICOTINAMIDE, Nicotinamide phosphoribosyltransferase | | Authors: | Takahashi, R, Nakamura, S, Kobayashi, Y, Ohkubo, T. | | Deposit date: | 2006-12-20 | | Release date: | 2007-12-25 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structure and reaction mechanism of human nicotinamide phosphoribosyltransferase
J.Biochem., 147, 2010
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3DHD
 | | Crystal structure of human NAMPT complexed with nicotinamide mononucleotide and pyrophosphate | | Descriptor: | BETA-NICOTINAMIDE RIBOSE MONOPHOSPHATE, MAGNESIUM ION, Nicotinamide phosphoribosyltransferase, ... | | Authors: | Ho, M, Burgos, E.S, Almo, S.C, Schramm, V.L. | | Deposit date: | 2008-06-17 | | Release date: | 2009-08-18 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | A phosphoenzyme mimic, overlapping catalytic sites and reaction coordinate motion for human NAMPT.
Proc.Natl.Acad.Sci.USA, 106, 2009
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5NSD
 | | Co-crystal structure of NAMPT dimer with KPT-9274 | | Descriptor: | (~{E})-3-(6-azanylpyridin-3-yl)-~{N}-[[5-[4-[4,4-bis(fluoranyl)piperidin-1-yl]carbonylphenyl]-7-(4-fluorophenyl)-1-benzofuran-2-yl]methyl]prop-2-enamide, GLYCEROL, Nicotinamide phosphoribosyltransferase, ... | | Authors: | Neggers, J.E, Kwanten, B, Dierckx, T, Noguchi, H, Voet, A, Vercruysse, T, Baloglu, E, Senapedis, W, Jacquemyn, M, Daelemans, D. | | Deposit date: | 2017-04-26 | | Release date: | 2018-02-14 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.046 Å) | | Cite: | Target identification of small molecules using large-scale CRISPR-Cas mutagenesis scanning of essential genes.
Nat Commun, 9, 2018
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4O0Z
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5WI0
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8IVU
 | | Crystal Structure of Human NAMPT in complex with A4276 | | Descriptor: | N-[[4-(6-methyl-1,3-benzoxazol-2-yl)phenyl]methyl]pyridine-3-carboxamide, Nicotinamide phosphoribosyltransferase, PHOSPHATE ION | | Authors: | Kang, B.G, Cha, S.S. | | Deposit date: | 2023-03-28 | | Release date: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.09000921 Å) | | Cite: | Discovery of a novel NAMPT inhibitor that selectively targets NAPRT-deficient EMT-subtype cancer cells and alleviates chemotherapy-induced peripheral neuropathy.
Theranostics, 13, 2023
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4O1C
 | | The crystal structures of a mutant NAMPT H191R | | Descriptor: | 1,2-ETHANEDIOL, Nicotinamide phosphoribosyltransferase, PHOSPHATE ION | | Authors: | Oh, A, Coons, M, Brillantes, B, Wang, W. | | Deposit date: | 2013-12-15 | | Release date: | 2014-10-22 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.092 Å) | | Cite: | Structural Basis for Resistance to Diverse Classes of NAMPT Inhibitors.
Plos One, 9, 2014
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5LX3
 | | CRYSTAL STRUCTURE OF VISFATIN IN COMPLEX WITH SAR154782. | | Descriptor: | 6-[4-[(6-azanylpyridin-3-yl)methylcarbamoylamino]-3-fluoranyl-phenyl]-2-(ethylamino)-~{N}-(2-piperidin-1-ylethyl)pyridine-3-carboxamide, Nicotinamide phosphoribosyltransferase | | Authors: | Bertrand, T, Marquette, J.P. | | Deposit date: | 2016-09-20 | | Release date: | 2017-10-25 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | CRYSTAL STRUCTURE OF VISFATIN IN COMPLEX WITH SAR154782.
To Be Published
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3DGR
 | | Crystal structure of human NAMPT complexed with ADP analogue | | Descriptor: | Nicotinamide phosphoribosyltransferase, PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | | Authors: | Ho, M, Burgos, E.S, Almo, S.C, Schramm, V.L. | | Deposit date: | 2008-06-15 | | Release date: | 2009-08-18 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | A phosphoenzyme mimic, overlapping catalytic sites and reaction coordinate motion for human NAMPT.
Proc.Natl.Acad.Sci.USA, 106, 2009
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2GVJ
 | | Crystal Structure of Human NMPRTase in complex with FK866 | | Descriptor: | (2E)-N-{4-[1-(benzenecarbonyl)piperidin-4-yl]butyl}-3-(pyridin-3-yl)prop-2-enamide, Nicotinamide phosphoribosyltransferase | | Authors: | Khan, J.A, Tao, X, Tong, L. | | Deposit date: | 2006-05-02 | | Release date: | 2006-06-20 | | Last modified: | 2016-11-09 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents.
Nat.Struct.Mol.Biol., 13, 2006
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8DTJ
 | | Human NAMPT in complex with small molecule activator ZN-43-S | | Descriptor: | (3S)-N-[(1-benzothiophen-5-yl)methyl]-1-{2-[4-(trifluoromethyl)phenyl]-2H-pyrazolo[3,4-d]pyrimidin-4-yl}piperidine-3-carboxamide, CHLORIDE ION, GLYCEROL, ... | | Authors: | Ratia, K, Xiong, R, Shen, Z, Thatcher, G.R. | | Deposit date: | 2022-07-25 | | Release date: | 2023-03-08 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.118 Å) | | Cite: | Mechanism of Allosteric Modulation of Nicotinamide Phosphoribosyltransferase to Elevate Cellular NAD.
Biochemistry, 62, 2023
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4L4L
 | | Structural Analysis of a Phosphoribosylated Inhibitor in Complex with Human Nicotinamide Phosphoribosyltransferase | | Descriptor: | 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, ... | | Authors: | Oh, A, Ho, Y, Zak, M, Liu, Y, Yuen, P, Zheng, X, Dragovich, S.P, Wang, W. | | Deposit date: | 2013-06-08 | | Release date: | 2014-06-11 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.122 Å) | | Cite: | Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.
Chembiochem, 15, 2014
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7PPG
 | | CRYSTAL STRUCTURE OF NAMPT IN COMPLEX WITH COMPOUND 9 | | Descriptor: | 1,2-ETHANEDIOL, N-[4-[(4R)-1-cyclopentyl-4-methyl-6-oxidanylidene-4,5-dihydropyridazin-3-yl]phenyl]-1,3-dihydropyrrolo[3,4-c]pyridine-2-carboxamide, Nicotinamide phosphoribosyltransferase, ... | | Authors: | Hillig, R.C. | | Deposit date: | 2021-09-13 | | Release date: | 2022-06-15 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.13 Å) | | Cite: | A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy.
Bioconjug.Chem., 33, 2022
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4JNM
 | | Discovery of Potent and Efficacious Urea-containing Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors with Reduced CYP2C9 Inhibition Properties | | Descriptor: | 1,2-ETHANEDIOL, 1-[(6-aminopyridin-3-yl)methyl]-3-[4-(phenylsulfonyl)phenyl]urea, Nicotinamide phosphoribosyltransferase, ... | | Authors: | 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. | | Deposit date: | 2013-03-15 | | Release date: | 2013-05-29 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | 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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8DSH
 | | Human NAMPT in complex with quercitrin and AMPcP | | Descriptor: | 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4-oxo-4H-chromen-3-yl 6-deoxy-alpha-L-mannopyranoside, Nicotinamide phosphoribosyltransferase, PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER | | Authors: | Ratia, K, Xiong, R, Shen, Z, Thatcher, G.R. | | Deposit date: | 2022-07-22 | | Release date: | 2023-03-08 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Mechanism of Allosteric Modulation of Nicotinamide Phosphoribosyltransferase to Elevate Cellular NAD.
Biochemistry, 62, 2023
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8F7L
 | | Human NAMPT in complex with substrate NAM and small molecule activator ZN-29-S | | Descriptor: | (3S)-N-[(1-benzothiophen-5-yl)methyl]-1-[(2P)-2-(3-fluoro-4-methylphenyl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl]piperidine-3-carboxamide, CHLORIDE ION, NICOTINAMIDE, ... | | Authors: | Ratia, K, Xiong, R, Shen, Z, Thatcher, G.R. | | Deposit date: | 2022-11-18 | | Release date: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Human NAMPT in complex with substrate NAM and small molecule activator ZN-29-S
To Be Published
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2GVG
 | | Crystal Structure of human NMPRTase and its complex with NMN | | Descriptor: | BETA-NICOTINAMIDE RIBOSE MONOPHOSPHATE, Nicotinamide phosphoribosyltransferase, PHOSPHATE ION | | Authors: | Khan, J.A, Tao, X, Tong, L. | | Deposit date: | 2006-05-02 | | Release date: | 2006-06-20 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents.
Nat.Struct.Mol.Biol., 13, 2006
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2E5C
 | | Crystal structure of Human NMPRTase complexed with 5'-phosphoribosyl-1'-pyrophosphate | | Descriptor: | 1-O-pyrophosphono-5-O-phosphono-alpha-D-ribofuranose, Nicotinamide phosphoribosyltransferase | | Authors: | Takahashi, R, Nakamura, S, Kobayashi, Y, Ohkubo, T. | | Deposit date: | 2006-12-20 | | Release date: | 2007-12-25 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structure and reaction mechanism of human nicotinamide phosphoribosyltransferase
J.Biochem., 147, 2010
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7ENQ
 | | Crystal structure of human NAMPT in complex with compound NAT | | Descriptor: | 2-(2-~{tert}-butylphenoxy)-~{N}-(4-hydroxyphenyl)ethanamide, Nicotinamide phosphoribosyltransferase, PHOSPHATE ION | | Authors: | Wang, G, Wu, C, Liu, M, Yao, H, Li, C, Wang, L, Tang, Y. | | Deposit date: | 2021-04-19 | | Release date: | 2022-05-04 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.204966 Å) | | Cite: | Discovery of small-molecule activators of nicotinamide phosphoribosyltransferase (NAMPT) and their preclinical neuroprotective activity.
Cell Res., 32, 2022
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7PPI
 | | Crystal STRUCTURE OF NAMPT IN COMPLEX WITH Compound 11 | | Descriptor: | CHLORIDE ION, GLYCEROL, N-[4-[(5R)-1-(4-azanylbutyl)-6-oxidanylidene-5-quinolin-5-yl-4,5-dihydropyridazin-3-yl]phenyl]-1,3-dihydropyrrolo[3,4-c]pyridine-2-carboxamide, ... | | Authors: | Hillig, R.C. | | Deposit date: | 2021-09-13 | | Release date: | 2022-06-15 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.33 Å) | | Cite: | A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy.
Bioconjug.Chem., 33, 2022
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7PPF
 | | CRYSTAL STRUCTURE OF NAMPT IN COMPLEX WITH COMPOUND 8 | | Descriptor: | 1,2-ETHANEDIOL, N-[4-[(4R)-1,4-dimethyl-6-oxidanylidene-4,5-dihydropyridazin-3-yl]phenyl]-5,7-dihydropyrrolo[3,4-b]pyridine-6-carboxamide, Nicotinamide phosphoribosyltransferase, ... | | Authors: | Hillig, R.C. | | Deposit date: | 2021-09-13 | | Release date: | 2022-06-15 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.36 Å) | | Cite: | A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy.
Bioconjug.Chem., 33, 2022
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4M6Q
 | | Identification of Amides Derived From 1H-Pyrazolo[3,4-b]pyridine-5-carboxylic Acid as Potent Inhibitors of Human Nicotinamide Phosphoribosyltransferase (NAMPT) | | Descriptor: | 1-(5-O-phosphono-beta-D-ribofuranosyl)-N-(4-{[3-(trifluoromethyl)phenyl]sulfonyl}benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide, Nicotinamide phosphoribosyltransferase, PHOSPHATE ION, ... | | Authors: | 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. | | Deposit date: | 2013-08-10 | | Release date: | 2013-09-25 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.406 Å) | | Cite: | 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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6B76
 | | Crystal Structure of human NAMPT in complex with NVP-LVR596 | | Descriptor: | (1S,2S)-N-{4-[(1S)-1-(propanoylamino)ethyl]phenyl}-2-(pyridin-3-yl)cyclopropane-1-carboxamide, Nicotinamide phosphoribosyltransferase, PHOSPHATE ION | | Authors: | Weihofen, W.A, Thigale, S. | | Deposit date: | 2017-10-03 | | Release date: | 2018-10-03 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.44 Å) | | Cite: | Identification and structure based design of cellularly active cyclo-propyl carboxamide Nicotinamide phosphoribosyltransferase (NAMPT) inhibitors
To Be Published
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4L4M
 | | Structural Analysis of a Phosphoribosylated Inhibitor in Complex with Human Nicotinamide Phosphoribosyltransferase | | Descriptor: | 1,2-ETHANEDIOL, N-{4-[(3,5-difluorophenyl)sulfonyl]benzyl}imidazo[1,2-a]pyridine-7-carboxamide, Nicotinamide phosphoribosyltransferase, ... | | Authors: | Oh, A, Ho, Y, Zak, M, Liu, Y, Yuen, P, Zheng, X, Dragovich, S.P, Wang, W. | | Deposit date: | 2013-06-08 | | Release date: | 2014-06-11 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.445 Å) | | Cite: | Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.
Chembiochem, 15, 2014
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