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Chemical Compound Review

PubChem22593     3-[4-(4- diethylaminobutylamino)-9- (3,5...

Synonyms: JSPY-st000263, S1264_Selleck, CHEMBL189584, SureCN177946, cc-523, ...
 
 
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Disease relevance of PD 173074

 

High impact information on PD 173074

  • A high degree of surface complementarity between PD 173074 and the hydrophobic, ATP-binding pocket of FGF receptor 1 underlies the potency and selectivity of this inhibitor [1].
  • PD 173074 is thus a promising candidate for a therapeutic angiogenesis inhibitor to be used in the treatment of cancer and other diseases whose progression is dependent upon new blood vessel formation [1].
  • The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects [2].
  • Nanomolar concentrations of PD 173074 prevented FGF-2, but not insulin-like growth factor-1, support of cerebellar granule neuron survival under conditions of serum/K(+) deprivation; another FGF-2 inhibitor, SU 5402, was effective only at a 1,000-fold greater concentration [2].
 

Associations of PD 173074 with other chemical compounds

  • To elucidate the determinants of selectivity, we have determined the crystal structure of PD 173074 in complex with the tyrosine kinase domain of FGF receptor 1 at 2.5 A resolution [1].

References

  1. Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. Mohammadi, M., Froum, S., Hamby, J.M., Schroeder, M.C., Panek, R.L., Lu, G.H., Eliseenkova, A.V., Green, D., Schlessinger, J., Hubbard, S.R. EMBO J. (1998) [Pubmed]
  2. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. Skaper, S.D., Kee, W.J., Facci, L., Macdonald, G., Doherty, P., Walsh, F.S. J. Neurochem. (2000) [Pubmed]
 
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