Enfuvirtid: Perbedaan antara revisi
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==Farmakologi==
===Mekanisme kerja===
HIV mengikat reseptor sel CD4+ inang melalui protein virus gp120; gp41, protein transmembran virus, kemudian mengalami perubahan konformasi yang membantu fusi membran virus ke membran sel inang. Enfuvirtid mengikat gp41 untuk mencegah terbentuknya pori masuk bagi kapsid virus, sehingga virus tidak dapat masuk ke dalam sel.<ref>{{cite journal | vauthors = Lalezari JP, Eron JJ, Carlson M, Cohen C, DeJesus E, Arduino RC, Gallant JE, Volberding P, Murphy RL, Valentine F, Nelson EL, Sista PR, Dusek A, Kilby JM | display-authors = 6 | title = A phase II clinical study of the long-term safety and antiviral activity of enfuvirtide-based antiretroviral therapy | journal = AIDS | volume = 17 | issue = 5 | pages = 691–8 | date = March 2003 | pmid = 12646792 | doi = 10.1097/00002030-200303280-00007 | s2cid = 32014873 | doi-access = free }}</ref>
Enfuvirtid juga merupakan aktivator reseptor faktor kemotaktik, reseptor peptida formil 1, dan dengan demikian mengaktifkan fagosit dan mungkin sel lain yang mengandung reseptor ini.<ref name="pmid10339497">{{cite journal | vauthors = Su SB, Gong WH, Gao JL, Shen WP, Grimm MC, Deng X, Murphy PM, Oppenheim JJ, Wang JM | display-authors = 6 | title = T20/DP178, an ectodomain peptide of human immunodeficiency virus type 1 gp41, is an activator of human phagocyte N-formyl peptide receptor | journal = Blood | volume = 93 | issue = 11 | pages = 3885–92 | date = June 1999 | pmid = 10339497 | doi = 10.1182/blood.V93.11.3885 }}</ref>
===Mikrobiologi===
Enfuvirtid dianggap aktif terhadap HIV-1 saja. Aktivitas rendah terhadap isolat HIV-2 telah dibuktikan secara ''[[in vitro]]''.<ref name="FuzeonPI">Roche Products Pty Ltd. Fuzeon (Australian Approved Product Information). Dee Why (NSW): Roche; 2005.</ref>
Kerentanan yang bervariasi terhadap enfuvirtid telah diamati pada isolat klinis, dengan resistensi yang didapat sebagai hasil dari motif 10 [[asam amino]] yang bermutasi pada gp41 virus. Namun, resistensi primer belum diamati.<ref name="Greenberg2004">{{cite journal | vauthors = Greenberg ML, Cammack N | title = Resistance to enfuvirtide, the first HIV fusion inhibitor | journal = The Journal of Antimicrobial Chemotherapy | volume = 54 | issue = 2 | pages = 333–40 | date = August 2004 | pmid = 15231762 | doi = 10.1093/jac/dkh330 | doi-access = free }}</ref>
===Rumus struktur===
Enfuvirtid adalah peptida dengan 36 asam amino dengan urutan sebagai berikut:<ref>{{cite journal | vauthors = Wild C, Greenwell T, Shugars D, Rimsky-Clarke L, Matthews T | title = The Inhibitory Activity of an HIV Type 1 Peptide Correlates with Its Ability to Interact with a Leucine Zipper Structure | journal = AIDS Research and Human Retroviruses | volume = 11 | issue = 3 | pages = 323–25 | year = 1995 | doi = 10.1089/aid.1995.11.323| pmid = 7786578 }}</ref><ref>{{cite journal | vauthors = De Clercq E | title = Toward Improved Anti-HIV Chemotherapy: Therapeutic Strategies for Intervention with HIV Infections | journal = Journal of Medicinal Chemistry | volume = 38 | issue = 14 | pages = 2491–2517 | date = July 1995 | doi = 10.1021/jm00014a001| pmid = 7543152 }}</ref>
[[Gugus asetil|CH<sub>3</sub>CO]]-[[tirosina|Tyr]]-[[treonina|Thr]]-[[serina|Ser]]-[[leusina|Leu]]-[[isoleusina|Ile]]-[[histidina|His]]-Ser-Leu-Ile-[[asam glutamat|Glu]]-Glu-Ser-[[glutamina|Gln]]-[[asparagina|Asn]]-Gln-Gln-Glu-[[lisin|Lys]]-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-[[asam aspartat|Asp]]-Lys-[[triptofan|Trp]]-[[alanina|Ala]]-Ser-Leu-Trp-Asn-Trp-[[fenilalanina|Phe]]-[[amina|NH<sub>2</sub>]] (Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-<sub>2</sub>)
==Referensi==
{{Reflist}}
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