PDTD [Potential Drug Target Database]

 

The possible binding proteins of the anti-cancer drug 4H-tamoxifen

Eleven proteins have been identified as interaction targets for 4H-tamoxifen or for its metabolite, tamoxifen (11). Five (14 entries) of the eleven experimentally confirmed targets for 4H-tamoxifen appear amongst the top 10% of the TarFisDock predicted candidates from PDTD.

 

Table 1. The top 10% candidates of 4H-tamxifen binding proteins derived by TarFisDock
RANK PDB_ID ENERGY SCORE TARGET NAME

1

1K3Y

-42.88

Glutathione Transferase A1-1

3

4FAB

-38.63

4-4-20 (IgG2A) Fab Fragment

13

1DBB

-36.54

Fab' Fragment Of The Db3 Anti-Steroid Monoclonal Antibody

18

1DHF

-36.19

Dihydrofolate Reductase

25

4DFR

-35.63

Dihydrofolate Reductase

37

1BZF

-34.25

Dihydrofolate Reductase

42

2CGR

-33.97

Igg2B Fab Fragment

46

1DBK

-33.77

Fab' Fragment Of Monoclonal Antibody Db3

47

1IGJ

-33.74

Fab (Igg2A, )

64

1DBM

-32.94

Fab' Fragment Of Monoclonal Antibody Db3

66

1MCR

-32.8

Immunoglobulin lambda Light Chain Dimer (Mcg)

67

1AYK

-32.8

Human Fibroblast Collagenase

69

1AG8

-32.75

Aldehyde dehydrogenase

71

1BAF

-32.57

Anti-dinitrophenyl-spin-label monoclonal antibody Fab fragment

* Targets highlighted by blue have been experimentally verified as listed in Table 2.

Table 2. The potential binding proteins of 4H-tamoxifen published in literatures
Known Target of 4H-tamoxifen References
Estrogen receptor (1)
Protein kinase C (2)
Collagenase (3)
Alcohol dehydrogenase (4)
17 β-hydroxysteriod dehydrogenase (5)
Prostaglandin synthetase (6)
3 α-hydroxysteroid dehydrogenase (7)
Glutathione transferase (8)
Calmodulin (2)
Dihydrofolate reductase (9, 10)
Immunoglobulin (9, 10)
*These targets were summarized by Chen et al.(11)
References:

1.   Favoni, R.E. and A. de Cupis, Trends Pharmacol Sci, 1998. 19(10): p. 406-15.
2.   Rowlands, M.G., et al., Biochem Pharmacol, 1995. 50(5): p. 723-6.
3.   Abbas Abidi, S.M., et al., Clin Exp Metastasis, 1997. 15(4): p. 432-9.
4.   Messiha, F.S., Gen Pharmacol, 1990. 21(1): p. 45-8.
5.   Santner, S.J. and R.J. Santen, J Steroid Biochem Mol Biol, 1993. 45(5): p. 383-90.
6.   Ritchie, G.A., Recent Results Cancer Res, 1980. 71: p. 96-101.
7.   Lax, E.R., et al., Endocrinology, 1983. 113(3): p. 1043-55.
8.   Nuwaysir, E.F., et al., Cancer Res, 1996. 56(16): p. 3704-10.
9.   Levine, R.M., et al., Cancer Res, 1985. 45(4): p. 1644-50.
10. Paavonen, T., et al., Apmis, 1991. 99(9): p. 849-53.
11. Chen, Y.Z. and D.G. Zhi, Proteins, 2001. 43(2): p. 217-26.