Talk:CCR5 receptor antagonist

Hidden Talk of unknown origin, by edit history, initial entry, moved into own section

Celsentri® er nýtt andretróveirulyf, framleitt af lyfjafyrirtækinu Pfizer. Virka efnið í lyfinu er maraviroc. Lyfið fékk markaðsleyfi í Bandaríkjunum í ágúst 2007 og var samþykkt í Evrópu í september sama ár. Enn hefur lyfið ekki verið skráð hérlendis. Lyfið er Z-merkt, það er að segja ávísun þess er bundin við sérfræðinga í smitsjúkdómum [1,3].

The translation of the above from Icelandic, with typographic corrections, is, approximately:

Celsentri® is a new antiretroviral drug, manufactured by Pfizer. The active ingredient in the drug maraviroc. The product was authorized in the United States in August 2007, and was approved in Europe in September of the same year. The drug has not [yet] been reported in this country [Iceland?]. The product is Z-marked, that is to say, it is restricted [in its presecription] to specialists in infectious diseases [1,3].

71.239.87.100 (talk) 19:55, 29 December 2014 (UTC)

Wow!

Big drop of knowledge you've just recently laid down with very little previous editing experience. I'm impressed! Structure, refs, neutral tone and everything. Good stuff!

Some feedback as well. First off, the article, even with a very good understanding of HIV/AIDS (although not any in depth formal molecular/cellular biology knowledge), it is still a bit of a struggle to read through the article easily. Maybe it would be ham-handed to simplify it, but I wanted to put that out there. Secondly, the swath of subject chosen for this article seems focused, but I have an itch to propose moving some of it to CCR5 or individual drug articles. Lastly, I want to make sure that this content was not largely copied from anywhere (website/publication etc) - there are little signs that hint at the possibility (e.g. 'the following summarizes' + 'as mentioned' tend to be prose found in publications and not Wikipedia, this is a huge article for just one person). Just wanted to check, don't mean anything bad by it. :) JoeSmack ^Talk 03:03, 7 November 2009 (UTC)

I agree. Very well laid out article. I have done a couple of preliminary searches, and haven't found anything suggesting that any large portions have been copied verbatim from anywhere else. I believe this research was published fairly recently (Spetember of this year?), but I could be mistaken. I would agree that the article should be renamed to something shorter, and that it would be rather "ham handed" to go about simplifying it to any great extent. It is obviously a very technical article, and without a thorough understanding of molecular biology, chemistry and pharmacology one may come off as ignorant in trying to edit it to any great extent. Neuromancer (talk) 23:57, 7 November 2009 (UTC)

Being fearless - or stupid, I've done some copyediting to improve the flow and grammar, but the further I got the less I understood the science, so it needs checking through for accuracy. I was, however stumped by the following sentence in the Pharmacophore section - "In B part is usually a basic nitrogen group." Is there a word missing here? Richerman (talk) 13:09, 12 November 2009 (UTC)

That sentence is referring to Figure 4, and because Figure 4 and the paragraph are discussing the molecular model, I'd imagine the sentence should read, "Part B is usually a basic nitrogen group." I'll give this a few hours and might make that edit tonight if I remember. Acetyl256 (talk) 15:35, 12 November 2009 (UTC)

Assessment for WP:MED

I've assessed the article by using the rating from the Pharmacology box, to be conservative. The article needs attention from someone well-versed in the subject, so I've put an {{expert}} tag on it, too. Whoever has enough knowledge to improve or copy-edit it without compromising content can re-assess it. MMagdalene722^{talk to me} 13:12, 18 November 2009 (UTC)

PRO 140

Shouldn't PRO 140 be mentioned here? It isn't related chemically (being a monoclonal antibody), but two or three sentences would be nice. --ἀνυπόδητος (talk) 17:25, 12 November 2009 (UTC)

Article too limited (to preclinical small molecule drug discovery)

Here is the content for the gene encoding this receptor, at the NIH's NCBI Gene website:

This gene encodes a member of the beta chemokine receptor family, which is predicted to be a seven transmembrane protein similar to G protein-coupled receptors. This protein is expressed by T cells and macrophages, and is known to be an important co-receptor for macrophage-tropic virus, including HIV, to enter host cells. Defective alleles of this gene have been associated with the HIV infection resistance. The ligands of this receptor include monocyte chemoattractant protein 2 (MCP-2), macrophage inflammatory protein 1 alpha (MIP-1 alpha), macrophage inflammatory protein 1 beta (MIP-1 beta) and regulated on activation normal T expressed and secreted protein (RANTES). Expression of this gene was also detected in a promyeloblastic cell line, suggesting that this protein may play a role in granulocyte lineage proliferation and differentiation. This gene is located at the chemokine receptor gene cluster region. Two transcript variants encoding the same protein have been found for this gene. [ref: NCBI Gene, 2014, "CCR5 chemokine (C-C motif) receptor 5 (gene/pseudogene) [Homo sapiens (human)]," Gene ID: 1234, updated on 22-Dec-2014, see [1], accessed 29 December 2014.]

This makes clear the known information on the receptor is broader than HIV. Three-quarters of the article content on the chemistry of small molecule antagonist design—though in line with my personal interests—is over much, and is not representative of what should appear in this article. There is far too much on one narrow area (small molecule design, via medichem) of one subtopic (preclinical small molecule discovery), and so the article lacks balance—and specific other subtopics, some of which appear in the quoted information above. As noted in the tags—which should remain until this matter of overemphasis on the chemistry of the small molecule inhibitor design by pharma is addressed—the article needs to be generalized to cover the notion of the antagonism itself—what the molecules do, and how—and specifically to how the antagonism functions (biological chem and cell biol), how it relates to and impacts other functions of the receptor, etc. 71.239.87.100 (talk) 19:44, 29 December 2014 (UTC)