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POU5F2  -  POU domain class 5, transcription factor 2

Homo sapiens

Synonyms: FLJ25680, POU domain, class 5, transcription factor 2, SPRM-1, SPRM1, Sperm 1 POU domain transcription factor
 
 
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Disease relevance of FLJ25680

 

High impact information on FLJ25680

  • The homologous protein from Schistosoma mansoni, SPRM1, also associates covalently with coexpressed h4F2hc glycoprotein, although it induces amino-acid transport of different substrate specificity [3].
  • BACKGROUND: Asoprisnil (J867) is a novel selective progesterone receptor modulator (SPRM) that exhibits partial agonist and antagonist activities and tissue selective effects [4].
  • Many PA and SPRM display direct antiproliferative effects in the endometrium, although with variable actions which seem product- and dose-dependent [5].
  • The negative abortion-related image of mifepristone has clearly limited the involvement of the major pharmaceutical companies in the development of PA and SPRM [5].
  • Recent advances in endocrinology open a door for clinical application of selective estrogen receptor modulator (SERM) and selective progesterone receptor modulator (SPRM) in the treatment of uterine leiomyoma [6].
 

Chemical compound and disease context of FLJ25680

  • Treatment with progesterone antagonist (RU486) or SPRM (J867) has been demonstrated to inhibit leiomyoma growth and improve clinical symptoms in premenopausal women [6].
 

Analytical, diagnostic and therapeutic context of FLJ25680

  • A series of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives were synthesized and tested in biological assays to evaluate scope and limitations of the nonsteroidal SPRM pharmacophore (3) [7].

References

  1. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis. Chwalisz, K., Perez, M.C., Demanno, D., Winkel, C., Schubert, G., Elger, W. Endocr. Rev. (2005) [Pubmed]
  2. A novel selective progesterone receptor modulator asoprisnil (J867) inhibits proliferation and induces apoptosis in cultured human uterine leiomyoma cells in the absence of comparable effects on myometrial cells. Chen, W., Ohara, N., Wang, J., Xu, Q., Liu, J., Morikawa, A., Sasaki, H., Yoshida, S., Demanno, D.A., Chwalisz, K., Maruo, T. J. Clin. Endocrinol. Metab. (2006) [Pubmed]
  3. Amino-acid transport by heterodimers of 4F2hc/CD98 and members of a permease family. Mastroberardino, L., Spindler, B., Pfeiffer, R., Skelly, P.J., Loffing, J., Shoemaker, C.B., Verrey, F. Nature (1998) [Pubmed]
  4. The effects of 1-month administration of asoprisnil (J867), a selective progesterone receptor modulator, in healthy premenopausal women. Chwalisz, K., Elger, W., Stickler, T., Mattia-Goldberg, C., Larsen, L. Hum. Reprod. (2005) [Pubmed]
  5. Selective progesterone receptor modulators and progesterone antagonists: mechanisms of action and clinical applications. Chabbert-Buffet, N., Meduri, G., Bouchard, P., Spitz, I.M. Hum. Reprod. Update (2005) [Pubmed]
  6. Selective estrogen receptor modulator and selective progesterone receptor modulator: therapeutic efficacy in the treatment of uterine leiomyoma. Ohara, N. Clinical and experimental obstetrics & gynecology. (2005) [Pubmed]
  7. Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators. Zhi, L., Tegley, C.M., Pio, B., Edwards, J.P., Jones, T.K., Marschke, K.B., Mais, D.E., Risek, B., Schrader, W.T. Bioorg. Med. Chem. Lett. (2003) [Pubmed]
 
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