메뉴 건너뛰기




Volumn 57, Issue 3, 2014, Pages 770-792

Fragment-based identification of amides derived from trans-2-(pyridin-3-yl) cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)

Author keywords

[No Author keywords available]

Indexed keywords

AMIDES; ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; CYCLOPROPANES; DRUG SCREENING ASSAYS, ANTITUMOR; HETEROGRAFTS; HUMANS; MICE; MICE, NUDE; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE; PROTEIN CONFORMATION; PYRIDINES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES;

EID: 84894102697     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm4015108     Document Type: Article
Times cited : (33)

References (73)
  • 3
    • 40849119972 scopus 로고    scopus 로고
    • 3: From metabolism to therapies
    • 3: from metabolism to therapies J. Pharmacol. Exp. Ther. 2008, 324, 883-893
    • (2008) J. Pharmacol. Exp. Ther. , vol.324 , pp. 883-893
    • Sauve, A.A.1
  • 4
    • 70449212074 scopus 로고
    • Biosynthesis of diphosphopyridine nucleotide. I. Identification of intermediates
    • Mammalian cells can also efficiently synthesize NAD from nicotinic acid (niacin) via the Preiss-Handler pathway
    • Mammalian cells can also efficiently synthesize NAD from nicotinic acid (niacin) via the Preiss-Handler pathway: Preiss, J.; Handler, P. Biosynthesis of diphosphopyridine nucleotide. I. Identification of intermediates J. Biol. Chem. 1958, 233, 488-492
    • (1958) J. Biol. Chem. , vol.233 , pp. 488-492
    • Preiss, J.1    Handler, P.2
  • 5
    • 79957955614 scopus 로고    scopus 로고
    • NAMPT in regulated NAD biosynthesis and its pivotal role in human metabolism
    • Burgos, E. S. NAMPT in regulated NAD biosynthesis and its pivotal role in human metabolism Curr. Med. Chem. 2011, 18, 1947-1961
    • (2011) Curr. Med. Chem. , vol.18 , pp. 1947-1961
    • Burgos, E.S.1
  • 6
    • 84864269536 scopus 로고    scopus 로고
    • Visfatin/NAMPT: A multifaceted molecule with diverse roles in physiology and pathophysiology
    • Dahl, T. B.; Holm, S.; Aukrust, P.; Halvorsen, B. Visfatin/NAMPT: a multifaceted molecule with diverse roles in physiology and pathophysiology Annu. Rev. Nutr. 2012, 32, 229-243
    • (2012) Annu. Rev. Nutr. , vol.32 , pp. 229-243
    • Dahl, T.B.1    Holm, S.2    Aukrust, P.3    Halvorsen, B.4
  • 7
    • 69549117127 scopus 로고    scopus 로고
    • A phosphoenzyme mimic, overlapping catalytic sites and reaction coordinate motion for human NAMPT
    • Burgos, E. S.; Ho, M.-C.; Almo, S. C.; Schramm, V. L. A phosphoenzyme mimic, overlapping catalytic sites and reaction coordinate motion for human NAMPT Proc. Natl. Acad. Sci. U.S.A. 2009, 106, 13748-13753
    • (2009) Proc. Natl. Acad. Sci. U.S.A. , vol.106 , pp. 13748-13753
    • Burgos, E.S.1    Ho, M.-C.2    Almo, S.C.3    Schramm, V.L.4
  • 8
    • 33747624726 scopus 로고    scopus 로고
    • Crystal structure of visfatin/pre-B cell colony enhancing factor 1/nicotinamide phosphoribosyltransferase, free and in complex with the anti-cancer agent FK-866
    • Kim, M.-K.; Lee, J. H.; Kim, H.; Park, S. J.; Kim, S. H.; Kang, G. B.; Lee, Y. S.; Kim, J. B.; Kim, K. K.; Suh, S. W.; Eom, S. H. Crystal structure of visfatin/pre-B cell colony enhancing factor 1/nicotinamide phosphoribosyltransferase, free and in complex with the anti-cancer agent FK-866 J. Mol. Biol. 2006, 362, 66-77
    • (2006) J. Mol. Biol. , vol.362 , pp. 66-77
    • Kim, M.-K.1    Lee, J.H.2    Kim, H.3    Park, S.J.4    Kim, S.H.5    Kang, G.B.6    Lee, Y.S.7    Kim, J.B.8    Kim, K.K.9    Suh, S.W.10    Eom, S.H.11
  • 10
    • 33745817828 scopus 로고    scopus 로고
    • Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents
    • Khan, J. A.; Tao, X.; Tong, L. Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents Nat. Struct. Mol. Biol. 2006, 13, 582-588
    • (2006) Nat. Struct. Mol. Biol. , vol.13 , pp. 582-588
    • Khan, J.A.1    Tao, X.2    Tong, L.3
  • 11
    • 54349088713 scopus 로고    scopus 로고
    • Weak coupling of ATP hydrolysis to the chemical equilibrium of human nicotinamide phosphoribosyltransferase
    • Burgos, E. S.; Schramm, V. L. Weak coupling of ATP hydrolysis to the chemical equilibrium of human nicotinamide phosphoribosyltransferase Biochemistry 2008, 47, 11086-11096
    • (2008) Biochemistry , vol.47 , pp. 11086-11096
    • Burgos, E.S.1    Schramm, V.L.2
  • 12
    • 84874908355 scopus 로고    scopus 로고
    • Recycling nicotinamide. the transition-state structure of human nicotinamide phosphoribosyltransferase
    • Burgos, E. S.; Vetticatt, M. J.; Schramm, V. L. Recycling nicotinamide. The transition-state structure of human nicotinamide phosphoribosyltransferase J. Am. Chem. Soc. 2013, 135, 3485-3493
    • (2013) J. Am. Chem. Soc. , vol.135 , pp. 3485-3493
    • Burgos, E.S.1    Vetticatt, M.J.2    Schramm, V.L.3
  • 13
    • 84869009687 scopus 로고    scopus 로고
    • How cancer metabolism is tuned for proliferation and vulnerable to disruption
    • Schulze, A.; Harris, A. L. How cancer metabolism is tuned for proliferation and vulnerable to disruption Nature 2012, 491, 364-373
    • (2012) Nature , vol.491 , pp. 364-373
    • Schulze, A.1    Harris, A.L.2
  • 14
    • 84858604270 scopus 로고    scopus 로고
    • Metabolic reprogramming: A cancer hallmark even Warburg did not anticipate
    • Ward, P. S.; Thompson, C. B. Metabolic reprogramming: a cancer hallmark even Warburg did not anticipate Cancer Cell 2012, 21, 297-308
    • (2012) Cancer Cell , vol.21 , pp. 297-308
    • Ward, P.S.1    Thompson, C.B.2
  • 15
    • 84857992195 scopus 로고    scopus 로고
    • Tagreting cancer metabolism - Aiming at a tumor's sweet spot
    • Jones, N. P.; Schulze, A. Tagreting cancer metabolism-aiming at a tumor's sweet spot Drug Discovery Today 2012, 17, 232-241
    • (2012) Drug Discovery Today , vol.17 , pp. 232-241
    • Jones, N.P.1    Schulze, A.2
  • 16
    • 77949967131 scopus 로고    scopus 로고
    • Targeting metabolic transformation for cancer therapy
    • Tennant, D. A.; Durán, R. V.; Gottlieb, E. Targeting metabolic transformation for cancer therapy Nat. Rev. Cancer 2010, 10, 267-277
    • (2010) Nat. Rev. Cancer , vol.10 , pp. 267-277
    • Tennant, D.A.1    Durán, R.V.2    Gottlieb, E.3
  • 17
    • 84862697493 scopus 로고    scopus 로고
    • Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by the small molecule GMX1778 regulates ROS-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner
    • Cerna, D.; Li, H.; Flaherty, S.; Takebe, N.; Coleman, C. N.; Yoo, S. S. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by the small molecule GMX1778 regulates ROS-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner J. Biol. Chem. 2012, 287, 22408-22417
    • (2012) J. Biol. Chem. , vol.287 , pp. 22408-22417
    • Cerna, D.1    Li, H.2    Flaherty, S.3    Takebe, N.4    Coleman, C.N.5    Yoo, S.S.6
  • 18
    • 66249108601 scopus 로고    scopus 로고
    • Understanding the Warburg effect: The metabolic requirements of cell proliferation
    • Vander Heiden, M. G.; Cantley, L. C.; Thompson, C. B. Understanding the Warburg effect: the metabolic requirements of cell proliferation Science 2009, 324, 1029-1033
    • (2009) Science , vol.324 , pp. 1029-1033
    • Vander Heiden, M.G.1    Cantley, L.C.2    Thompson, C.B.3
  • 19
    • 84867877340 scopus 로고    scopus 로고
    • The NAD metabolome - A key determinant of cancer cell biology
    • Chiarugi, A.; Dölle, C.; Felici, R.; Ziegler, M. The NAD metabolome-a key determinant of cancer cell biology Nat. Rev. Cancer 2012, 12, 741-752
    • (2012) Nat. Rev. Cancer , vol.12 , pp. 741-752
    • Chiarugi, A.1    Dölle, C.2    Felici, R.3    Ziegler, M.4
  • 20
    • 84873980688 scopus 로고    scopus 로고
    • Nampt/visfatin/PBEF: A functionally multi-faceted protein with a pivotal role in malignant tumors
    • He, J.; Tu, C.; Li, M.; Wang, S.; Guan, X.; Lin, J.; Li, Z. Nampt/visfatin/PBEF: a functionally multi-faceted protein with a pivotal role in malignant tumors Curr. Pharm. Des. 2012, 18, 6123-6132
    • (2012) Curr. Pharm. Des. , vol.18 , pp. 6123-6132
    • He, J.1    Tu, C.2    Li, M.3    Wang, S.4    Guan, X.5    Lin, J.6    Li, Z.7
  • 22
    • 34248357083 scopus 로고    scopus 로고
    • Nicotinamide adenine dinucleotide metabolism as an attractive target for drug discovery
    • Khan, J. A.; Forouhar, F.; Tao, X.; Tong, L. Nicotinamide adenine dinucleotide metabolism as an attractive target for drug discovery Expert Opin. Ther. Targets 2007, 11, 695-705
    • (2007) Expert Opin. Ther. Targets , vol.11 , pp. 695-705
    • Khan, J.A.1    Forouhar, F.2    Tao, X.3    Tong, L.4
  • 26
    • 0242526050 scopus 로고    scopus 로고
    • FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis
    • Hasmann, M.; Schemainda, I. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis Cancer Res. 2003, 63, 7436-7442
    • (2003) Cancer Res. , vol.63 , pp. 7436-7442
    • Hasmann, M.1    Schemainda, I.2
  • 27
    • 0036170579 scopus 로고    scopus 로고
    • WK175, a novel antitumor agent, decreases the intracellular nicotinamide adenine dinucleotide concentration and induces the apoptotic cascade in human leukemia cells
    • Wosikowski, K.; Mattern, K.; Schemainda, I.; Hasmann, M.; Rattel, B.; Löser, R. WK175, a novel antitumor agent, decreases the intracellular nicotinamide adenine dinucleotide concentration and induces the apoptotic cascade in human leukemia cells Cancer Res. 2002, 62, 1057-1062
    • (2002) Cancer Res. , vol.62 , pp. 1057-1062
    • Wosikowski, K.1    Mattern, K.2    Schemainda, I.3    Hasmann, M.4    Rattel, B.5    Löser, R.6
  • 28
    • 14844291424 scopus 로고    scopus 로고
    • Phase i study and pharmacokinetic of CHS-828, a guanidino-containing compound, administered orally as a single dose every 3 weeks in solid tumours: An ECSG/EORTC study
    • Ravaud, A.; Cerny, T.; Terret, C.; Wanders, J.; Bui, B. N.; Hess, D.; Droz, J.-P.; Fumoleau, P.; Twelves, C. Phase I study and pharmacokinetic of CHS-828, a guanidino-containing compound, administered orally as a single dose every 3 weeks in solid tumours: an ECSG/EORTC study Eur. J. Cancer. 2005, 41, 702-707
    • (2005) Eur. J. Cancer. , vol.41 , pp. 702-707
    • Ravaud, A.1    Cerny, T.2    Terret, C.3    Wanders, J.4    Bui, B.N.5    Hess, D.6    Droz, J.-P.7    Fumoleau, P.8    Twelves, C.9
  • 34
    • 38149105811 scopus 로고    scopus 로고
    • The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor
    • Holen, K.; Saltz, L. B.; Hollywood, E.; Burk, K.; Hanauske, A.-R. The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor Invest. New Drugs 2008, 26, 45-51
    • (2008) Invest. New Drugs , vol.26 , pp. 45-51
    • Holen, K.1    Saltz, L.B.2    Hollywood, E.3    Burk, K.4    Hanauske, A.-R.5
  • 41
    • 79952281704 scopus 로고    scopus 로고
    • Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents
    • You, H.; Youn, H.-S.; Im, I.; Bae, M.-H.; Lee, S.-K.; Ko, H.; Eom, S. H.; Kim, Y.-C. Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents Eur. J. Med. Chem. 2011, 46, 1153-1164
    • (2011) Eur. J. Med. Chem. , vol.46 , pp. 1153-1164
    • You, H.1    Youn, H.-S.2    Im, I.3    Bae, M.-H.4    Lee, S.-K.5    Ko, H.6    Eom, S.H.7    Kim, Y.-C.8
  • 49
    • 84881367747 scopus 로고    scopus 로고
    • Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors
    • For a recent review of NAMPT and associated inhibitors, see the following: Galli, U.; Travelli, C.; Massarrotti, A.; Fakhfouri, G.; Rahimian, R.; Tron, G. C.; Genazzani, A. A. Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors J. Med. Chem. 2013, 56, 6279-6296
    • (2013) J. Med. Chem. , vol.56 , pp. 6279-6296
    • Galli, U.1    Travelli, C.2    Massarrotti, A.3    Fakhfouri, G.4    Rahimian, R.5    Tron, G.C.6    Genazzani, A.A.7
  • 55
    • 84870401411 scopus 로고    scopus 로고
    • Fragment based drug design: From experimental to computational approaches
    • Kumar, A.; Voet, A.; Zhang, K. Y. J. Fragment based drug design: from experimental to computational approaches Curr. Med. Chem. 2012, 19, 5128-5147
    • (2012) Curr. Med. Chem. , vol.19 , pp. 5128-5147
    • Kumar, A.1    Voet, A.2    Zhang, K.Y.J.3
  • 56
    • 67649494337 scopus 로고    scopus 로고
    • Transforming fragments into candidates: Small becomes big in medicinal chemistry
    • de Kloe, G. e.; Bailey, D.; Leurs, R.; de Esch, I. J. P. Transforming fragments into candidates: small becomes big in medicinal chemistry Drug Discovery Today 2009, 14, 630-646
    • (2009) Drug Discovery Today , vol.14 , pp. 630-646
    • De Kloe, G.E.1    Bailey, D.2    Leurs, R.3    De Esch, I.J.P.4
  • 57
    • 46849089254 scopus 로고    scopus 로고
    • Recent developments in fragment-based drug discovery
    • Congreve, M.; Chessari, G.; Tisi, D.; Woodhead, A. J. Recent developments in fragment-based drug discovery J. Med. Chem. 2008, 51, 3661-3680
    • (2008) J. Med. Chem. , vol.51 , pp. 3661-3680
    • Congreve, M.1    Chessari, G.2    Tisi, D.3    Woodhead, A.J.4
  • 58
    • 1942453243 scopus 로고    scopus 로고
    • Ligand efficiency: A useful metric for lead selection
    • Hopkins, A. L.; Groom, C. R.; Alex, A. Ligand efficiency: a useful metric for lead selection Drug Discovery Today 2004, 9, 430-431
    • (2004) Drug Discovery Today , vol.9 , pp. 430-431
    • Hopkins, A.L.1    Groom, C.R.2    Alex, A.3
  • 59
    • 61949390938 scopus 로고    scopus 로고
    • Tautomer enumeration and stability prediction for virtual screening on large chemical databases
    • The benzothiadiazine tautomer depicted for compound 9 in Table 1 was predicted by the software package MoKa (v1.1; Molecular Discovery) to be preferred over the alternative tautomeric form (calculated population 100%). Similar preferences were found for compounds 10 and 11. These predictions are consistent with hydrogen bonds observed crystallographically between compounds 9 and 11 and NAMPT (cf., Figures 6 and 7). For additional information regarding MoKa, see the following: Milletti, F.; Storchi, L.; Sforna, G.; Cross, S.; Cruciani, G. Tautomer enumeration and stability prediction for virtual screening on large chemical databases J. Chem. Inf. Model. 2009, 49, 68-75
    • (2009) J. Chem. Inf. Model. , vol.49 , pp. 68-75
    • Milletti, F.1    Storchi, L.2    Sforna, G.3    Cross, S.4    Cruciani, G.5
  • 60
    • 84884205885 scopus 로고    scopus 로고
    • Design, synthesis, and biological evaluation of cyclopropyl analogues of stilbene with raloxifene side chain as subtypeselective ligands for estrogen receptor
    • Yeo, H. L.; Song, Y. S.; Ryu, J.-H.; Kim, H.-D. Design, synthesis, and biological evaluation of cyclopropyl analogues of stilbene with raloxifene side chain as subtypeselective ligands for estrogen receptor Arch. Pharm. Res. 2013, 36, 1096-1103
    • (2013) Arch. Pharm. Res. , vol.36 , pp. 1096-1103
    • Yeo, H.L.1    Song, Y.S.2    Ryu, J.-H.3    Kim, H.-D.4
  • 61
    • 34249304805 scopus 로고    scopus 로고
    • Dihydro-[1 H ]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia
    • Lagu, B.; Lebedev, R.; Pio, B.; Yang, M.; Pelton, P. D. Dihydro-[1 H ]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia Bioorg. Med. Chem. Lett. 2007, 17, 3491-3496
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 3491-3496
    • Lagu, B.1    Lebedev, R.2    Pio, B.3    Yang, M.4    Pelton, P.D.5
  • 62
    • 12344287392 scopus 로고    scopus 로고
    • Convergent approach to (E)-alkene and cyclopropane peptide isosteres
    • Wipf, P.; Xiao, J. Convergent approach to (E)-alkene and cyclopropane peptide isosteres Org. Lett. 2005, 7, 103-106
    • (2005) Org. Lett. , vol.7 , pp. 103-106
    • Wipf, P.1    Xiao, J.2
  • 63
    • 0037029805 scopus 로고    scopus 로고
    • Synthesis of the racemic forms of carbon-carbon double bond locked analogues of strobilurins which are characterized by a 2-arylcyclopropane ring cis -substituted at C-1 by the methyl (E)-3-methoxypropenoate unit
    • Carpita, A.; Ribecai, A.; Rossi, R.; Stabile, P. Synthesis of the racemic forms of carbon-carbon double bond locked analogues of strobilurins which are characterized by a 2-arylcyclopropane ring cis -substituted at C-1 by the methyl (E)-3-methoxypropenoate unit Tetrahedron 2002, 58, 3673-3680
    • (2002) Tetrahedron , vol.58 , pp. 3673-3680
    • Carpita, A.1    Ribecai, A.2    Rossi, R.3    Stabile, P.4
  • 65
    • 0019302256 scopus 로고
    • Studies on anticoccidial agents. 13. Synthesis and anticoccidial activity of nitropyridine-2- and -3-sulfonamides and derivatives
    • Morisawa, Y.; Kataoka, M.; Nagahori, H.; Sakamoto, T.; Kitano, N.; Kusano, K.; Sato, K. Studies on anticoccidial agents. 13. Synthesis and anticoccidial activity of nitropyridine-2- and -3-sulfonamides and derivatives J. Med. Chem. 1980, 23, 1376-1380
    • (1980) J. Med. Chem. , vol.23 , pp. 1376-1380
    • Morisawa, Y.1    Kataoka, M.2    Nagahori, H.3    Sakamoto, T.4    Kitano, N.5    Kusano, K.6    Sato, K.7
  • 66
    • 0027359857 scopus 로고
    • 3-(Alkylamino)-4 H -pyrido[4,3- e ]-l,2,4-thiadiazine 1,l-dioxides as powerful inhibitors of insulin release from rat pancreatic B-cells: A new class of potassium channel openers?
    • Pirotte, B.; de Tullio, P.; Lebrun, P.; Antoine, M.-H.; Fontaine, J.; Masereel, B.; Schynts, M.; Dupont, L.; Herchuelz, A.; Delarget, J. 3-(Alkylamino)-4 H -pyrido[4,3- e ]-l,2,4-thiadiazine 1,l-dioxides as powerful inhibitors of insulin release from rat pancreatic B-cells: a new class of potassium channel openers? J. Med. Chem. 1993, 36, 3211-3213
    • (1993) J. Med. Chem. , vol.36 , pp. 3211-3213
    • Pirotte, B.1    De Tullio, P.2    Lebrun, P.3    Antoine, M.-H.4    Fontaine, J.5    Masereel, B.6    Schynts, M.7    Dupont, L.8    Herchuelz, A.9    Delarget, J.10
  • 67
    • 0000456008 scopus 로고    scopus 로고
    • A substituted hypersensitive radical probe for enzyme-catalyzed hydroxylations: Synthesis of racemic and enantiomerically enriched forms and application in a cytochrome P450-catalyzed oxidation
    • Toy, P. H.; Dhanabalasingam, B.; Newcomb, M.; Hanna, I. H.; Hollenberg, P. F. A substituted hypersensitive radical probe for enzyme-catalyzed hydroxylations: synthesis of racemic and enantiomerically enriched forms and application in a cytochrome P450-catalyzed oxidation J. Org. Chem. 1997, 62, 9114-9122
    • (1997) J. Org. Chem. , vol.62 , pp. 9114-9122
    • Toy, P.H.1    Dhanabalasingam, B.2    Newcomb, M.3    Hanna, I.H.4    Hollenberg, P.F.5
  • 68
    • 0026028019 scopus 로고
    • A novel route to cyclopropyl ketones, aldehydes, and carboxylic acids
    • Rodriques, K. E. A novel route to cyclopropyl ketones, aldehydes, and carboxylic acids Tetrahedron Lett. 1991, 32, 1275-1278
    • (1991) Tetrahedron Lett. , vol.32 , pp. 1275-1278
    • Rodriques, K.E.1
  • 70
    • 84856021026 scopus 로고    scopus 로고
    • Synthesis of a C -iminoribofuranoside analog of the nicotinamide phosphoribosyltransferase (NAMPT) inhibitor FK866
    • Gillig, A.; Majjigapu, S. R.; Sordat, B.; Vogel, P. Synthesis of a C -iminoribofuranoside analog of the nicotinamide phosphoribosyltransferase (NAMPT) inhibitor FK866 Helv. Chim. Acta 2012, 95, 34-42
    • (2012) Helv. Chim. Acta , vol.95 , pp. 34-42
    • Gillig, A.1    Majjigapu, S.R.2    Sordat, B.3    Vogel, P.4
  • 71
    • 79952281704 scopus 로고    scopus 로고
    • Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents
    • You, H.; Youn, H.-S.; Im, I.; Bae, M.-H.; Lee, S.-K.; Ko, H.; Eom, S. H.; Kim, Y.-C. Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents Eur. J. Med. Chem. 2011, 46, 1153-1164
    • (2011) Eur. J. Med. Chem. , vol.46 , pp. 1153-1164
    • You, H.1    Youn, H.-S.2    Im, I.3    Bae, M.-H.4    Lee, S.-K.5    Ko, H.6    Eom, S.H.7    Kim, Y.-C.8
  • 72
    • 79952383501 scopus 로고    scopus 로고
    • From experimental design to validated hits: A comprehensive walk-through of fragment lead identification using surface plasmon resonance
    • Giannetti, A. M. From experimental design to validated hits: a comprehensive walk-through of fragment lead identification using surface plasmon resonance Methods Enzymol. 2011, 493, 169-218
    • (2011) Methods Enzymol. , vol.493 , pp. 169-218
    • Giannetti, A.M.1
  • 73
    • 39149130730 scopus 로고    scopus 로고
    • Surface plasmon resonance based assay for the detection and characterization of promiscuous inhibitors
    • Giannetti, A. M.; Koch, B. D.; Browner, M. F. Surface plasmon resonance based assay for the detection and characterization of promiscuous inhibitors J. Med. Chem. 2008, 51, 574-580
    • (2008) J. Med. Chem. , vol.51 , pp. 574-580
    • Giannetti, A.M.1    Koch, B.D.2    Browner, M.F.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.