Nelfinavir: Perbedaan antara revisi

'''Nelfinavir''' adalah [[Penanganan HIV/AIDS|obat antiretroviral]] yang digunakan dalam pengobatan HIV/[[AIDS]]. Nelfinavir termasuk dalam golongan obat yang dikenal sebagai penghambat protease (PI) dan seperti PI lainnya, hampir selalu digunakan dalam kombinasi dengan obat antiretroviral lainnya.

 

 

Obat ini dipatenkan pada tahun 1992 dan disetujui untuk penggunaan medis pada tahun 1997.<ref name=Fis2006>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=510 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA510 |language=en}}</ref>

 

==Mekanisme kerja==

==Penelitian==

Sejak tahun 2009, nelfinavir telah diteliti untuk potensi penggunaannya sebagai agen antikanker.<ref>{{cite journal | vauthors = Chow WA, Jiang C, Guan M | title = Anti-HIV drugs for cancer therapeutics: back to the future? | journal = The Lancet. Oncology | volume = 10 | issue = 1 | pages = 61–71 | date = January 2009 | pmid = 19111246 | doi = 10.1016/S1470-2045(08)70334-6 }}</ref> Ketika diaplikasikan pada sel kanker dalam kultur (''[[in vitro]]''), ia dapat menghambat pertumbuhan berbagai jenis kanker dan dapat memicu kematian sel ([[apoptosis]]).<ref name="pmid17785575">{{cite journal | vauthors = Gills JJ, Lopiccolo J, Tsurutani J, Shoemaker RH, Best CJ, Abu-Asab MS, Borojerdi J, Warfel NA, Gardner ER, Danish M, Hollander MC, Kawabata S, Tsokos M, Figg WD, Steeg PS, Dennis PA | display-authors = 6 | title = Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo | journal = Clinical Cancer Research | volume = 13 | issue = 17 | pages = 5183–5194 | date = September 2007 | pmid = 17785575 | doi = 10.1158/1078-0432.CCR-07-0161 | doi-access = free }}</ref> Ketika Nelfinavir diberikan kepada mencit laboratorium dengan tumor prostat atau otak, ia dapat menekan pertumbuhan tumor pada hewan-hewan tersebut.<ref>{{cite journal | vauthors = Pyrko P, Kardosh A, Wang W, Xiong W, Schönthal AH, Chen TC | title = HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress | journal = Cancer Research | volume = 67 | issue = 22 | pages = 10920–10928 | date = November 2007 | pmid = 18006837 | doi = 10.1158/0008-5472.CAN-07-0796 | doi-access = free }}</ref><ref>{{cite journal | vauthors = Yang Y, Ikezoe T, Takeuchi T, Adachi Y, Ohtsuki Y, Takeuchi S, Koeffler HP, Taguchi H | display-authors = 6 | title = HIV-1 protease inhibitor induces growth arrest and apoptosis of human prostate cancer LNCaP cells in vitro and in vivo in conjunction with blockade of androgen receptor STAT3 and AKT signaling | journal = Cancer Science | volume = 96 | issue = 7 | pages = 425–433 | date = July 2005 | pmid = 16053514 | doi = 10.1111/j.1349-7006.2005.00063.x | s2cid = 44702882 | doi-access = | pmc = 11158579 }}</ref> Pada tingkat seluler, nelfinavir memberikan banyak efek untuk menghambat pertumbuhan kanker; dua efek utama tampaknya adalah penghambatan jalur pensinyalan Akt/PKB dan aktivasi stres [[retikulum endoplasma]] dengan respons protein yang tidak terlipat berikutnya.<ref>{{cite journal | vauthors = Koltai T | title = Nelfinavir and other protease inhibitors in cancer: mechanisms involved in anticancer activity | journal = F1000Research | volume = 4 | issue = 2 | pages = 9 | date = 2015 | pmid = 26097685 | pmc = 4457118 | doi = 10.12688/f1000research.5827.2 | doi-access = free }}</ref>

* {{cite journal | vauthors = Bardsley-Elliot A, Plosker GL | title = Nelfinavir: an update on its use in HIV infection | journal = Drugs | volume = 59 | issue = 3 | pages = 581–620 | date = March 2000 | pmid = 10776836 | doi = 10.2165/00003495-200059030-00014 | doi-access = free }}

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