Talk:Selective glucocorticoid receptor modulator/GA1

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GA Review[edit]

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Here is a list of issues, most of which are related to GA criteria. I can't see anything else at the moment that makes the article not meet them.

  • "is a type of experimental drug which shares many of the desirable anti-inflammatory and immunosuppressive properties of classical glucocorticoid drugs but with fewer side effects such as skin atrophy" it's not proven until there have been clinical trials
  • transrepression/transactivation: the complex is a transcription factor in both cases
    •  Done, I think. Can you check whether this makes sense now? --ἀνυπόδητος (talk) 12:15, 28 March 2010 (UTC)[reply]
      • Haven't helped. The transrepression section of http://www.ncbi.nlm.nih.gov/pubmed/17630119 was helpul though, you ought to use it instead of the German ref. Dimer vs monomer looks like an important point. Narayanese (talk) 21:08, 29 March 2010 (UTC)[reply]
        • Boghog2 has written a detailed account of that mechanism. I don't have access to the source you mentioned, so I don't want to exchange the reference without knowing what Schäcke actually says. Feel free to do it yourself if you object to the German source. --ἀνυπόδητος (talk) 14:29, 30 March 2010 (UTC)[reply]
  • Mechanism of action section: when saying it causes an effect, say which model (mouse? cell line?)
    • Done for some of the physiological effects, and will try to source and re-add the rest later. (Note to self: catabolic and lipolytic action, atrophy of muscle and connective tissue.) Should I do the same with the molecular mechanisms (up-regulation of COX etc. etc.)? That will need some time, but of course I'll do it if you think it is necessary. --ἀνυπόδητος (talk) 16:27, 29 March 2010 (UTC)[reply]
  • Potential applications last paragraph: give reference
    • Referenced statement that the antiproliferative properties of GCs are used in psoriasis. The second sentence, "SEGRAs would likely be less effective in such conditions", is hard to source. My main intention with this paragraph was to show that transactivation is not all bad (just as COX-2 is not all bad), and that SEGRAs are unlikely to render CGs obsolete. What do you think, can it be saved somehow? --ἀνυπόδητος (talk) 13:22, 30 March 2010 (UTC)[reply]
  • in vitro: means different things in different disciplines, avoid the word
  • "benzopyrano-quinoline A 276575 or in octahydrophenanthrene-2,7-diol" etc: I don't like the linking of particular groups, think you should unlink
  • The wikilinking in general is in bad shape, with metabolic linked when about metabolic side-effects, infection instead of eye infection, connective tissue when discussig atrophy of it
  • pictures: add sources to the image description pages or captions
  • Image captions: I recommend removing full stop at end
  • "Compounds were investigated in cellular[7] and animal models[8] of inflammation" a summary of the results would be in order
  • ZK 245186: move from lead to history
  • "the cytosolic glucocorticoid receptor" jargonish shorthand for glucocorticoid receptor when in is in the cytosol, explain better for non-biologists
  • "and a number of other pro-inflammatory molecules" you just listed proteins, molecules sounds like the small ones.
  • "It is testing concentrations of 0.01%" what type of percent? Don't you normally count in weight?
    • Usually m/m is implied, but this is hard to source and doesn't make much difference anyway for an organic compound in an organic/water ointment. My point was to show that the therapeutic concentration will probably be between 0.01% and 0.1% as opposed to, say, 5%. I don't think it is important to know whether it is 0.008 or 0.012% (m/m). --ἀνυπόδητος (talk) 10:07, 28 March 2010 (UTC)[reply]
      • As long as it's the same unit as you could expect on the final product it's all fine. Narayanese (talk) 11:11, 28 March 2010 (UTC)[reply]
  • "and will include about 64 patients" will sounds strange when it has started since long
    • It is still recruiting, and the total number of patients will be about 64. Tried to rephrase, is it better now? --ἀνυπόδητος (talk) 10:07, 28 March 2010 (UTC)[reply]
      • Yup, it's better. Still takes a moment of thought, but nothing bad. Narayanese (talk) 11:11, 28 March 2010 (UTC)[reply]

Reviewer: Narayanese (talk) 20:21, 27 March 2010 (UTC)[reply]

Stereochemistry[edit]

A concern from me: Do you think this source establishes R configuration of ZK 216348 (OH in front)? Fig. 1 looks much like it in my opinion, but the text only calls it the (+)-enantiomer which isn't helpful. The other structures of trifluoropropanolamines are here and here. Both look like R but aren't exactly clear. --ἀνυπόδητος (talk) 14:17, 28 March 2010 (UTC)[reply]

It does look like OH is at front, with the stereochemistry is drawn in perspective. Narayanese (talk) 18:16, 1 April 2010 (UTC)[reply]