Integraza — разлика између измена

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'''[[HIV]] integraza''' je 32 [[kilodalton|kDa]] dug [[protein]] koji se formira iz C-terminalne porcije [[Polimeraza|Pol genskog]] produkta. Ona je atraktivna meta za anti-HIV lekove.
 
Novembra 2005, nalazi [[Kliničko ispitivanje|studije faze 2]] ispitivanja HIV [[inhibitor integraze|inhibitora integraze]], [[Raltegravir|MK-0518]], su pokazali da to jedinjenje ima potentno antiviralno dejstvo.<ref>Morales-Ramirez JO, Teppler H, Kovacs C, et al. Antiretroviral effect of MK-0518, a novel HIV-1 integrase inhibitor, in ART-naïve HIV-1 infected patients. Program and abstracts of the 10th European AIDS Conference; November 17–20, 2005; Dublin, Ireland. Abstract LBPS1/6. Online summary: http://clinicaloptions.com/HIV/Conference%20Coverage/Dublin%202005/Capsules/LBPS1-6.aspx {{Wayback|url=http://clinicaloptions.com/HIV/Conference%20Coverage/Dublin%202005/Capsules/LBPS1-6.aspx |date=20061029111040 }}</ref><ref name="pmid17107277">{{cite journal | author = Savarino A | title = A historical sketch of the discovery and development of HIV-1 integrase inhibitors | journal = Expert Opin Investig Drugs | volume = 15 | issue = 12 | pages = 1507–22 |date= 2006 | pmid = 17107277 | doi = 10.1517/13543784.15.12.1507 }}</ref> [[FDA]] je 12. oktobra 2007. odobrila upotrebu integraznog inhibitora [[Raltegravir]]a (MK-0518, prodajno ime Isentress <sup>TM</sup>).<ref>{{cite news| url=http://www.cnn.com/2007/HEALTH/10/12/hiv.drug/index.html#cnnSTCText | work=CNN | title=FDA approves drug that fights HIV in new way - CNN.com | date= 2007-10-12 | accessdate= 2010-05-05 }}</ref> Drugi inhibitor integraze, [[elvitegravir]], je odobren u SAD avgusta 2012.<ref name="pmid22748591">{{cite journal |vauthors=Sax PE, DeJesus E, Mills A, Zolopa A, Cohen C, Wohl D, Gallant JE, Liu HC, Zhong L, Yale K, White K, Kearney BP, Szwarcberg J, Quirk E, Cheng AK | title = Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3 trial, analysis of results after 48 weeks | journal = Lancet | volume = 379 | issue = 9835 | pages = 2439–48 |date= 2012 | pmid = 22748591 | doi = 10.1016/S0140-6736(12)60917-9 }}</ref>
 
Kristalna struktura [[ljudski penasti virus|HFV]] integraze je uzpešno ispitana.<ref name="pmid20118915">{{cite journal |vauthors=Hare S, Gupta SS, Valkov E, Engelman A, Cherepanov P | title = Retroviral intasome assembly and inhibition of DNA strand transfer | journal = Nature | volume = 464 | issue = 7286 | pages = 232–6 |date= 2010 | pmid = 20118915 | pmc = 2837123 | doi = 10.1038/nature08784 | url = }}</ref> Smatra se da ovaj protein koristi [[morfein]]ski model [[alosterna regulacija|alosterne regulacije]].<ref name="pmid22182754">{{cite journal |vauthors=Selwood T, Jaffe EK | title = Dynamic dissociating homo-oligomers and the control of protein function | journal = Arch. Biochem. Biophys. | volume = 519 | issue = 2 | pages = 131–43 |date= 2012 | pmid = 22182754 | doi = 10.1016/j.abb.2011.11.020 | pmc=3298769}}</ref>
Преузето из „https://sr.wikipedia.org/wiki/Integraza