Literature DB >> 15579327

Low-calcemic, efficacious, 1alpha,25-dihydroxyvitamin D3 analog QW-1624F2-2: calcemic dose-response determination, preclinical genotoxicity testing, and revision of A-ring stereochemistry.

Gary H Posner1, Heung Bae Jeon, Amy Sarjeant, Edward S Riccio, Rupa S Doppalapudi, Izet M Kapetanovic, Uttam Saha, Patrick Dolan, Thomas W Kensler.   

Abstract

Based on an X-ray crystal structure determination, the A-ring stereochemistry of hybrid analog QW-1624F2-2 (1alpha-hydroxymethyl-16-ene-24,24-difluoro-25-hydroxy-26,27-bis-homovitamin D3) is revised to be 1alpha-CH2OH-3beta-OH. This analog is shown to be approximately 80-100 times less calciuric than the natural hormone 1alpha,25-dihydoxyvitamin D3. This analog is shown also to be non-genotoxic in three different standard assays.

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Year:  2004        PMID： 15579327     DOI： 10.1016/j.steroids.2004.09.004

Source DB:  PubMed          Journal:  Steroids        ISSN： 0039-128X            Impact factor:   2.668


  8 in total

1.  Apc(MIN) modulation of vitamin D secosteroid growth control.

Authors:  Haibo Xu; Gary H Posner; Michael Stevenson; Frederick C Campbell
Journal:  Carcinogenesis       Date:  2010-05-20       Impact factor: 4.944

2.  Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation.

Authors:  Gary H Posner; Byung Chul Suh; Kimberly S Petersen; Patrick Dolan; Elin S Agoston; Thomas W Kensler; John T Koh; Sara Peleg
Journal:  J Steroid Biochem Mol Biol       Date:  2007-01-10       Impact factor: 4.292

3.  The response of creatine kinase specific activity in rat pituitary to estrogenic compounds and vitamin d less-calcemic analogs.

Authors:  D Somjen; N Mirsky; S Tamir; J Vaya; G H Posner; A M Kaye
Journal:  Int J Cell Biol       Date:  2009-09-10

4.  Less-calcemic vitamin D analogs enhance creatine kinase specific activity and modulate responsiveness to gonadal steroids in rat skeletal tissues.

Authors:  D Somjen; G H Posner; Y Weisman; A M Kaye
Journal:  J Endocrinol Invest       Date:  2007-02       Impact factor: 4.256

5.  Differentiation-inducing potency of the seco-steroid JK-1624F2-2 can be increased by combination with an antioxidant and a p38MAPK inhibitor which upregulates the JNK pathway.

Authors:  Jing Zhang; Gary H Posner; Michael Danilenko; George P Studzinski
Journal:  J Steroid Biochem Mol Biol       Date:  2007-05-16       Impact factor: 4.292

6.  Rapid access to preventive intervention development program in the Division of Cancer Prevention of the U.S. National Cancer Institute: an overview.

Authors:  Izet M Kapetanovic
Journal:  Cancer Epidemiol Biomarkers Prev       Date:  2009-02-24       Impact factor: 4.254

7.  Cooperation between BRCA1 and vitamin D is critical for histone acetylation of the p21waf1 promoter and growth inhibition of breast cancer cells and cancer stem-like cells.

Authors:  Itay Pickholtz; Shira Saadyan; Gilmor I Keshet; Victor S Wang; Rachel Cohen; Peter Bouwman; Jos Jonkers; Stephen W Byers; Moshe Z Papa; Ronit I Yarden
Journal:  Oncotarget       Date:  2014-12-15

Review 8.  Novel vitamin D compounds and skin cancer prevention.

Authors:  Wannit Tongkao-On; Clare Gordon-Thomson; Katie M Dixon; Eric J Song; Tan Luu; Sally E Carter; Vanessa B Sequeira; Vivienne E Reeve; Rebecca S Mason
Journal:  Dermatoendocrinol       Date:  2013-01-01
  8 in total

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