BRENDA - Reference to 2.4.2.12; Id = 661421

pharmacology

enzyme is a potential target for development of anticancer drugs

Homo sapiens

FK866

a highly specific noncompetitive inhibitor the enzyme, represents a novel mechanism for induction of tumor cell apoptosis, counteracted by nicotinic acid and nicotinamide

Homo sapiens

mitochondrion

-

Homo sapiens

5739

-

additional information

Homo sapiens

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+

?

-

nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate

Homo sapiens

key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide

nicotinamide D-ribonucleotide + diphosphate

-

?

Homo sapiens

-

partially frim K-562 leukemic cells

Homo sapiens

Hep-G2 cell

liver carcinoma cell line

Homo sapiens

-

K-562 cell

leukemia cell line

Homo sapiens

-

additional information

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+

661421

Homo sapiens

?

-

nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate

-

661421

Homo sapiens

nicotinamide D-ribonucleotide + diphosphate

-

?

nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate

key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide

661421

Homo sapiens

nicotinamide D-ribonucleotide + diphosphate

-

?

NAPRT

-

Homo sapiens

37

-

assay at

Homo sapiens

8.8

-

assay at

Homo sapiens

0.0003

-

FK866

free enzyme

Homo sapiens

0.0004

-

FK866

enzyme-substrate complex

Homo sapiens

pharmacology

enzyme is a potential target for development of anticancer drugs

Homo sapiens

FK866

a highly specific noncompetitive inhibitor the enzyme, represents a novel mechanism for induction of tumor cell apoptosis, counteracted by nicotinic acid and nicotinamide

Homo sapiens

0.0003

-

FK866

free enzyme

Homo sapiens

0.0004

-

FK866

enzyme-substrate complex

Homo sapiens

mitochondrion

-

Homo sapiens

5739

-

additional information

Homo sapiens

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+

?

-

nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate

Homo sapiens

key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide

nicotinamide D-ribonucleotide + diphosphate

-

?

partially frim K-562 leukemic cells

Homo sapiens

Hep-G2 cell

liver carcinoma cell line

Homo sapiens

-

K-562 cell

leukemia cell line

Homo sapiens

-

additional information

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis in tissues with a high demand for NAD+

661421

Homo sapiens

?

-

nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate

-

661421

Homo sapiens

nicotinamide D-ribonucleotide + diphosphate

-

?

nicotinamide + 5-phospho-alpha-D-ribose 1-diphosphate

key enzyme in the regulation of NAD+ biosynthesis from the natural precursor nicotinamide

661421

Homo sapiens

nicotinamide D-ribonucleotide + diphosphate

-

?

37

-

assay at

Homo sapiens

8.8

-

assay at

Homo sapiens

735765

Clark

Application of virtual screeni ...

Homo sapiens

Bioorg. Med. Chem. Lett.

26

2920-2926

2016

-

17

-

1

-

2

-

1

-

1

-

13

-

13

17

-

1

-

1

-

735766

Chen

Identification of benzothiophe ...

Homo sapiens

Bioorg. Med. Chem. Lett.

26

765-768

2016

-

17

-

1

-

2

-

3

-

1

-

1

-

14

-

14

17

-

1

-

3

-

1

-

735872

Grolla

Extracellular nicotinamide pho ...

Homo sapiens

Br. J. Pharmacol.

173

2182-2194

2016

-

14

-

1

-

1

-

1

-

1

-

49

-

1

-

3

-

1

-

1

-

14

-

1

-

1

-

1

-

49

-

1

-

2

1

2

-

736091

Fang

Analysis of the nicotinamide p ...

Danio rerio

FEBS J.

282

2858-2878

2015

-

1

-

3

-

1

-

1

-

2

-

1

-

1

-

1

-

1

-

736115

Marletta

Crystal structure of human nic ...

Homo sapiens

FEBS Open Bio

5

419-428

2015

-

1

-

1

-

4

-

1

-

1

-

1

-

1

-

1

-

737247

Xu

Discovery and characterization ...

Homo sapiens

Sci. Rep.

5

10043

2015

-

49

-

1

-

2

-

4

-

1

3

-

48

-

48

49

-

1

-

4

-

1

-

737279

Zabka

Retinal toxicity, in vivo and ...

Homo sapiens, Rattus norvegicus

Toxicol. Sci.

144

163-172

2015

-

14

-

2

-

7

-

6

-

2

-

2

-

14

-

2

-

6

-

2

-

735760

Zheng

Discovery of potent and effica ...

Homo sapiens

Bioorg. Med. Chem. Lett.

24

337-343

2014

-

18

-

1

-

2

-

1

-

1

-

1

-

14

-

14

18

-

1

-

1

-

1

-

736003

Hsu

The function of nicotinamide p ...

Homo sapiens

DNA Repair

23

64-68

2014

-

1

-

1

-

1

-

2

-

1

-

1

-

3

-

1

-

1

-

1

-

1

-

1

-

1

-

736227

Pittelli

Nicotinamide phosphoribosyltra ...

Homo sapiens, Mus musculus

Immunol. Cell Biol.

92

191-199

2014

-

2

-

2

-

4

-

2

-

2

-

2

-

2

-

2

-

2

-

2

-

3

-

735758

Zheng

Identification of amides deriv ...

Homo sapiens

Bioorg. Med. Chem. Lett.

23

5488-5497

2013

-

32

-

1

-

6

-

6

-

1

-

4

-

28

-

28

32

-

1

-

6

-

1

-

736436

Tan

Pharmacological inhibition of ...

Homo sapiens

J. Biol. Chem.

288

3500-3511

2013

-

1

-

1

-

2

-

12

-

1

-

1

-

1

-

1

-

12

-

1

-

2

-

736612

Zheng

Structure-based discovery of n ...

Homo sapiens

J. Med. Chem.

56

6413-6433

2013

-

40

-

1

-

2

-

5

-

1

-

4

-

35

-

35

40

-

1

-

5

-

1

-

723576

Bowlby

Nicotinamide phosphoribosyl tr ...

Homo sapiens

PLoS ONE

7

e40195

2012

-

1

-

5

-

1

-

5

-

1

-

723588

Liu

Nicotinamide phosphoribosyltra ...

Mus musculus

PLoS ONE

7

e44933

2012

-

1

-

2

-

1

-

1

-

1

-

1

-

721273

Zhang

A fluorometric assay for high- ...

Mus musculus

Anal. Biochem.

412

18-25

2011

-

1

-

4

-

2

-

1

-

1

-

3

-

4

-

1

-

4

-

1

-

1

-

722099

Friebe

Leucocytes are a major source ...

Homo sapiens

Diabetologia

54

1200-1211

2011

-

2

-

2

-

3

-

2

-

722182

Dahl

Nicotinamide phosphoribosyltra ...

Homo sapiens

Eur. J. Clin. Invest.

41

1098-1104

2011

-

1

-

1

-

1

-

1

-

1

-

1

-

1

-

1

-

722560

Zhang

Nicotinamide phosphoribosyltra ...

Homo sapiens

J. Bioanal. Biomed.

3

13-25

2011

-

1

-

2

-

1

-

1

-

2

-

1

-

9

-

1

3

-

1

-

1

-

2

-

1

-

1

-

1

-

9

-

1

-

1

-

2

-

722718

Hong

Nicotinamide phosphoribosyltra ...

Oryctolagus cuniculus

J. Biol. Chem.

286

28619-28631

2011

-

1

-

1

-

3

-

1

-

723535

Hara

Nicotinamide phosphoribosyltra ...

Homo sapiens

PLoS ONE

6

e22781

2011

1

-

1

-

4

-

3

-

7

-

1

-

2

-

1

-

1

-

4

-

7

-

1

-

702085

Garten

Nicotinamide phosphoribosyltra ...

Homo sapiens

Biochem. Biophys. Res. Commun.

391

376-381

2010

-

2

-

3

-

3

-

2

-

2

-

3

-

2

-

704364

Takahashi

Structure and reaction mechani ...

Homo sapiens

J. Biochem.

147

95-107

2010

-

1

-

2

-

1

-

1

-

1

-

705072

Colombano

A novel potent nicotinamide ph ...

Homo sapiens

J. Med. Chem.

53

616-623

2010

-

1

-

1

-

1

-

1

-

1

-

721934

Olesen

Target enzyme mutations are th ...

Homo sapiens

BMC Cancer

10

677

2010

-

1

-

5

-

3

-

1

-

1

-

4

-

1

-

1

-

2

-

1

-

5

-

2

3

-

1

-

4

-

1

-

722688

Pittelli

Inhibition of nicotinamide pho ...

Homo sapiens

J. Biol. Chem.

285

34106-34114

2010

-

1

-

2

-

2

-

1

-

1

-

2

-

722862

Zhang

Nicotinamide phosphoribosyltra ...

Homo sapiens

J. Cell. Biochem.

110

1464-1470

2010

-

1

-

2

-

1

-

1

2

-

1

-

1

-

1

-

701720

Beauparlant

Preclinical development of the ...

Homo sapiens, Mus musculus

Anticancer Drugs

20

346-354

2009

-

2

-

2

-

4

-

3

-

2

-

2

-

3

-

703243

Hsu

Nicotinamide phosphoribosyltra ...

Mus musculus

Circ. Res.

105

481-491

2009

-

3

-

1

-

1

-

1

-

1

-

690900

Burgos

Weak Coupling of ATP Hydrolysi ...

Homo sapiens

Biochemistry

47

11086-11096

2008

3

-

1

-

8

10

-

1

-

2

-

1

-

8

-

2

-

9

1

-

14

-

3

-

1

-

8

14

10

-

1

-

1

-

8

-

9

1

-

692570

Mercader

Retinol-binding protein 4 and ...

Rattus norvegicus

Horm. Metab. Res.

40

467-472

2008

-

1

-

4

-

4

-

1

-

5

-

1

-

4

-

1

-

694813

Busso

Pharmacological inhibition of ...

Homo sapiens, Mus musculus

PLoS ONE

3

e2267

2008

-

1

-

2

-

2

-

3

-

9

-

2

-

10

-

1

-

2

-

2

-

9

-

2

-

677402

Takahashi

Crystallization of human nicot ...

Homo sapiens

Acta Crystallogr. Sect. F

F63

375-377

2007

-

1

-

2

-

1

-

1

-

1

-

1

-

1

-

680749

van der Veer

Extension of human cell lifesp ...

Homo sapiens

J. Biol. Chem.

282

10841-10845

2007

-

1

-

1

-

2

-

3

-

4

-

3

-

9

-

1

2

-

2

-

2

-

4

-

3

-

690246

Takahashi

Crystallization of human nicot ...

Homo sapiens

Acta Crystallogr. Sect. F

63

375-377

2007

-

1

-

1

-

2

-

1

-

1

2

-

1

-

1

-

1

-

1

-

1

2

-

681396

Kim

Crystal structure of visfatin/ ...

Rattus norvegicus

J. Mol. Biol.

362

66-77

2006

-

1

-

1

-

1

-

1

-

1

-

1

-

3

-

1

-

1

-

1

-

1

-

1

-

1

-

682082

Khan

Molecular basis for the inhibi ...

Homo sapiens, Mus musculus

Nat. Struct. Mol. Biol.

13

582-588

2006

-

2

-

2

-

2

-

4

-

2

-

2

-

2

-

2

-

2

-

2

-

2

-

2

-

2

-

682448

Ashihara

-

De novo and salvage biosynthet ...

no activity in Picea glauca

Plant Sci.

169

107-114

2005

-

1

-

662306

Revollo

The NAD biosynthesis pathway m ...

Mus musculus

J. Biol. Chem.

279

50754-50763

2004

-

1

-

1

-

1

-

3

-

1

-

2

1

-

3

-

1

-

1

-

1

-

1

-

1

-

1

-

2

1

-

3

-

1

-

1

-

661421

Hasmann

FK866, a highly specific nonco ...

Homo sapiens

Cancer Res.

63

7436-7442

2003

-

1

-

1

-

1

-

2

-

2

-

1

-

2

-

3

-

1

-

1

-

2

-

1

-

1

2

-

1

-

2

-

1

-

2

-

3

-

1

-

1

-

489743

Rongvaux

Pre-B-cell colony-enhancing fa ...

Mus musculus

Eur. J. Immunol.

32

3225-3234

2002

-

1

-

1

-

1

-

6

-

2

-

2

-

1

-

1

-

1

-

2

-

2

-

489744

Martin

Identification of a plasmid-en ...

Haemophilus ducreyi

J. Bacteriol.

183

1168-1174

2001

-

1

-

1

-

14

-

1

-

1

-

1

-

1

-

489742

Rocchigiani

Determination of nicotinamide ...

Homo sapiens

Anal. Biochem.

205

334-336

1992

-

2

1

-

1

-

2

-

3

1

-

1

-

1

-

1

-

2

1

-

1

-

3

1

-

1

-

489741

Shibata

-

End product inhibition of the ...

Rattus norvegicus

Agric. Biol. Chem.

53

2283-2284

1989

-

1

-

1

-

1

-

1

-

11

-

1

-

1

-

1

-

1

-

1

-

1

-

1

-

11

-

1

-

1

-

489740

Elliott

Evidence for a physiologically ...

Homo sapiens

Biochem. Biophys. Res. Commun.

104

996-1002

1982

-

1

3

1

-

1

-

2

-

2

-

2

-

1

-

1

-

1

-

1

-

3

-

1

-

1

-

2

-

2

-

1

-

489738

Lin

Pyridine nucleotide synthesis. ...

Rattus norvegicus

J. Biol. Chem.

247

8016-8022

1972

1

-

1

-

2

1

-

1

-

2

-

1

-

2

1

2

-

1

-

1

2

1

-

1

-

1

-

1

-

2

1

-

1

-

1

-

2

1

2

-

1

-

1

2

-

489739

Dietrich

Inhibition of nicotinamide pho ...

Rattus norvegicus

Biochemistry

11

1691-1695

1972

-

16

2

-

1

-

1

-

1

-

1

-

1

-

2

-

1

-

1

-

1

-

16

-

2

-

1

-

1

-

1

-

2

-

1

-

489737

Preiss

Enzymatic synthesis of nicotin ...

Homo sapiens

J. Biol. Chem.

225

759-770

1957

-

2

1

-

1

-

1

-

1

-

1

-

1

-

1

-

2

-

1

-

2

-

1

-

1

-

1

-

1

-

1

-

1

-

2

-

1

-

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis

Data extracted from this reference: