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Pathway Description
Raltegravir Action Pathway
Homo sapiens
Category:
Metabolite Pathway
Sub-Category:
Drug Action
Created: 2023-03-15
Last Updated: 2023-10-25
Raltegravir is an antiretroviral agent used for the treatment of HIV infections in conjunction with other antiretrovirals.
Raltegravir is transported into the infected cell then transported into the nucleus via importin nuclear transporter.The viral RNA is injected into the cell then transcribed into viral DNA via reverse transcriptase. It is then transported into the nucleus where it is integrated into the host DNA. Raltegravir inhibits HIV integrase which prevents the viral DNA from being integrated into the host DNA. This prevents viral replication and further progression of the virus.
References
Raltegravir Pathway References
Arora R, de Beauchene IC, Polanski J, Laine E, Tchertanov L: Raltegravir flexibility and its impact on recognition by the HIV-1 IN targets. J Mol Recognit. 2013 Sep;26(9):383-401. doi: 10.1002/jmr.2277.
Pubmed: 23836466
Eron JJ, Cooper DA, Steigbigel RT, Clotet B, Gatell JM, Kumar PN, Rockstroh JK, Schechter M, Markowitz M, Yeni P, Loutfy MR, Lazzarin A, Lennox JL, Strohmaier KM, Wan H, Barnard RJ, Nguyen BY, Teppler H: Efficacy and safety of raltegravir for treatment of HIV for 5 years in the BENCHMRK studies: final results of two randomised, placebo-controlled trials. Lancet Infect Dis. 2013 Jul;13(7):587-96. doi: 10.1016/S1473-3099(13)70093-8. Epub 2013 May 7.
Pubmed: 23664333
Winston A, Mallon PW, Boffito M: The clinical pharmacology of antiretrovirals in development. Expert Opin Drug Metab Toxicol. 2006 Jun;2(3):447-58. doi: 10.1517/17425255.2.3.447.
Pubmed: 16863445
O'Neal R: MK-0518 and GS-9137: two promising integrase inhibitors in the pipeline. BETA. 2006 Summer;18(4):13-6.
Pubmed: 17019786
James JS: Integrase inhibitor MK-0518: Merck opens expanded-access program. AIDS Treat News. 2006 Jul-Sep;(419):5.
Pubmed: 17096488
Markowitz M, Morales-Ramirez JO, Nguyen BY, Kovacs CM, Steigbigel RT, Cooper DA, Liporace R, Schwartz R, Isaacs R, Gilde LR, Wenning L, Zhao J, Teppler H: Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr. 2006 Dec 15;43(5):509-15. doi: 10.1097/QAI.0b013e31802b4956.
Pubmed: 17133211
Colquitt AR, Pham PA: Expanded access drug profile: raltegravir (RAL, MK-0518). Hopkins HIV Rep. 2007 Jan;19(1):11-2.
Pubmed: 17569171
Evering TH, Markowitz M: Raltegravir: an integrase inhibitor for HIV-1. Expert Opin Investig Drugs. 2008 Mar;17(3):413-22. doi: 10.1517/13543784.17.3.413.
Pubmed: 18321239
Anker M, Corales RB: Raltegravir (MK-0518): a novel integrase inhibitor for the treatment of HIV infection. Expert Opin Investig Drugs. 2008 Jan;17(1):97-103. doi: 10.1517/13543784.17.1.97.
Pubmed: 18095922
Tseng SF, Chang CY, Wu KJ, Teng SC: Importin KPNA2 is required for proper nuclear localization and multiple functions of NBS1. J Biol Chem. 2005 Nov 25;280(47):39594-600. doi: 10.1074/jbc.M508425200. Epub 2005 Sep 27.
Pubmed: 16188882
Weis K, Mattaj IW, Lamond AI: Identification of hSRP1 alpha as a functional receptor for nuclear localization sequences. Science. 1995 May 19;268(5213):1049-53. doi: 10.1126/science.7754385.
Pubmed: 7754385
Dorr SN, Schlicker MN, Hansmann IN: Genomic structure of karyopherin alpha2 ( KPNA2) within a low-copy repeat on chromosome 17q23-q24 and mutation analysis in patients with Russell-Silver syndrome. Hum Genet. 2001 Nov;109(5):479-86. doi: 10.1007/s004390100605. Epub 2001 Oct 3.
Pubmed: 11735022
Chi NC, Adam EJ, Adam SA: Sequence and characterization of cytoplasmic nuclear protein import factor p97. J Cell Biol. 1995 Jul;130(2):265-74. doi: 10.1083/jcb.130.2.265.
Pubmed: 7615630
Gorlich D, Kostka S, Kraft R, Dingwall C, Laskey RA, Hartmann E, Prehn S: Two different subunits of importin cooperate to recognize nuclear localization signals and bind them to the nuclear envelope. Curr Biol. 1995 Apr 1;5(4):383-92. doi: 10.1016/s0960-9822(95)00079-0.
Pubmed: 7627554
Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. doi: 10.1038/ng1285. Epub 2003 Dec 21.
Pubmed: 14702039
Srimaroeng C, Chatsudthipong V, Aslamkhan AG, Pritchard JB: Transport of the natural sweetener stevioside and its aglycone steviol by human organic anion transporter (hOAT1; SLC22A6) and hOAT3 (SLC22A8). J Pharmacol Exp Ther. 2005 May;313(2):621-8. doi: 10.1124/jpet.104.080366. Epub 2005 Jan 11.
Pubmed: 15644426
Mizuno N, Takahashi T, Iwase Y, Kusuhara H, Niwa T, Sugiyama Y: Human organic anion transporters 1 (hOAT1/SLC22A6) and 3 (hOAT3/SLC22A8) transport edaravone (MCI-186; 3-methyl-1-phenyl-2-pyrazolin-5-one) and its sulfate conjugate. Drug Metab Dispos. 2007 Aug;35(8):1429-34. doi: 10.1124/dmd.106.013912. Epub 2007 May 14.
Pubmed: 17502342
Bleasby K, Hall LA, Perry JL, Mohrenweiser HW, Pritchard JB: Functional consequences of single nucleotide polymorphisms in the human organic anion transporter hOAT1 (SLC22A6). J Pharmacol Exp Ther. 2005 Aug;314(2):923-31. doi: 10.1124/jpet.105.084301. Epub 2005 May 24.
Pubmed: 15914676
Misumi Y, Ogata S, Ohkubo K, Hirose S, Ikehara Y: Primary structure of human placental 5'-nucleotidase and identification of the glycolipid anchor in the mature form. Eur J Biochem. 1990 Aug 17;191(3):563-9. doi: 10.1111/j.1432-1033.1990.tb19158.x.
Pubmed: 2129526
Hansen KR, Resta R, Webb CF, Thompson LF: Isolation and characterization of the promoter of the human 5'-nucleotidase (CD73)-encoding gene. Gene. 1995 Dec 29;167(1-2):307-12. doi: 10.1016/0378-1119(95)00574-9.
Pubmed: 8566797
Knapp K, Zebisch M, Pippel J, El-Tayeb A, Muller CE, Strater N: Crystal structure of the human ecto-5'-nucleotidase (CD73): insights into the regulation of purinergic signaling. Structure. 2012 Dec 5;20(12):2161-73. doi: 10.1016/j.str.2012.10.001. Epub 2012 Nov 8.
Pubmed: 23142347
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