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Chemical Compound Review

PELDESINE     3-amino-9-(pyridin-3- ylmethyl)-2,4,7...

Synonyms: BCX-34, SureCN61135, SureCN61136, CHEMBL311300, BCX 34, ...
 
 
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Disease relevance of BCX-34

  • A phase III, randomized, double-blind, placebo-controlled study of peldesine (BCX-34) cream as topical therapy for cutaneous T-cell lymphoma [1].
  • The antiproliferative effect of BCX-34 was tested in normal human peripheral blood mononuclear cells (PBMCs) induced to proliferate with OKT3, tetanus toxoid, the mixed lymphocyte reaction, or IL-2 [2].
  • The results demonstrate that BCX-34 inhibits human PNP and T-cell proliferation, is orally bioavailable in rodents, and pharmacologically active in vivo in rodents after oral dosing with no apparent side effects or toxicity [3].
 

High impact information on BCX-34

 

Biological context of BCX-34

 

Gene context of BCX-34

  • BCX-34 inhibits RBC PNP in vitro from humans, rats, and mice with IC50S ranging from 5 to 36 nM [3].
  • We evaluated the efficacy of a new purine nucleoside phosphorylase inhibitor, BCX-34, as an immunosuppressive agent [5].
  • BCX-1777 is a 10-100-fold more potent inhibitor of human lymphocyte proliferation than other known PNP inhibitors like PD141955 and BCX-34 [6].
 

Analytical, diagnostic and therapeutic context of BCX-34

  • Of the many classes of compounds synthesized, studied and reviewed, only one, the 3-pyridinylmethyl-9-deazaguanine (BCX-34, 39) analog has been used in clinical trials [7].
  • The object of this study was to determine the preformulation parameters of BCX-34 and subsequently prepare a sterile liquid formulation for intravenous infusion [8].

References

  1. A phase III, randomized, double-blind, placebo-controlled study of peldesine (BCX-34) cream as topical therapy for cutaneous T-cell lymphoma. Duvic, M., Olsen, E.A., Omura, G.A., Maize, J.C., Vonderheid, E.C., Elmets, C.A., Shupack, J.L., Demierre, M.F., Kuzel, T.M., Sanders, D.Y. J. Am. Acad. Dermatol. (2001) [Pubmed]
  2. Effects of a novel purine nucleoside phosphorylase inhibitor, BCX-34, on activation and proliferation of normal human lymphoid cells. Conry, R.M., Bantia, S., Turner, H.S., Barlow, D.L., Allen, K.O., LoBuglio, A.F., Montgomery, J.A., Walsh, G.M. Immunopharmacology (1998) [Pubmed]
  3. In vivo and in vitro pharmacologic activity of the purine nucleoside phosphorylase inhibitor BCX-34: the role of GTP and dGTP. Bantia, S., Montgomery, J.A., Johnson, H.G., Walsh, G.M. Immunopharmacology (1996) [Pubmed]
  4. Pharmacokinetics and pharmacodynamics of peldesine (BCX-34), a purine nucleoside phosphorylase inhibitor, following single and multiple oral doses in healthy volunteers. Viegas, T.X., Omura, G.A., Stoltz, R.R., Kisicki, J. Journal of clinical pharmacology. (2000) [Pubmed]
  5. BCX-34: a novel T-cell selective immunosuppressant: purine nucleoside phosphorylase (PNP) inhibitor. Wada, Y., Yagihashi, A., Terasawa, K., Miyao, N., Hirata, K., Cicciarelli, J., Iwaki, Y. Artificial organs. (1996) [Pubmed]
  6. Purine nucleoside phosphorylase inhibitor BCX-1777 (Immucillin-H)--a novel potent and orally active immunosuppressive agent. Bantia, S., Miller, P.J., Parker, C.D., Ananth, S.L., Horn, L.L., Kilpatrick, J.M., Morris, P.E., Hutchison, T.L., Montgomery, J.A., Sandhu, J.S. Int. Immunopharmacol. (2001) [Pubmed]
  7. Inhibitors of the enzyme purine nucleoside phosphorylase as potential therapy for psoriasis. Morris, P.E., Omura, G.A. Curr. Pharm. Des. (2000) [Pubmed]
  8. Preformulation studies for the development of a parenteral liquid formulation of the immunomodulator, peldesine. Viegas, T.X., Van Winkle, L.L. PDA journal of pharmaceutical science and technology / PDA. (1999) [Pubmed]
 
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