Enfuvirtid je 36 aminokiselina dug sintetički peptid koji inhibira HIV-1 fuziju sa CD4 ćelijama. On je acetilisan na N-kraju.[1][2][3]

Enfuvirtid
Klinički podaci
Prodajno imeFuzeon
Drugs.comMonografija
Kategorija trudnoće
Način primeneSubkutano (SC)
Pravni status
Pravni status
  • S4 (Au), POM (UK), ℞-only (SAD)
Farmakokinetički podaci
Bioraspoloživost84,3% (SC)
Vezivanje proteina92%
MetabolizamHepatički
Poluvreme eliminacije3.8 sata
Izlučivanjenepoznato
Identifikatori
CAS broj159519-65-0 ДаY
ATC kodJ05AX07 (WHO)
PubChemCID 16130199
DrugBankDB00109 ДаY
ChemSpider16743716 ДаY
UNII19OWO1T3ZE ДаY
KEGGD02499 ДаY
ChEBICHEBI:608828 ДаY
ChEMBLCHEMBL525076 ДаY
NIAID ChemDB059486
Hemijski podaci
FormulaC202H298N50O64
Molarna masa4492,1 g/mol
  • CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)O)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)O)C(=O)NC(CCCCN)C(=O)NC(Cc1c[nH]c2c1cccc2)C(=O)NC(C)C(=O)NC(CO)C(=O)NC(CC(C)C)C(=O)NC(Cc3c[nH]c4c3cccc4)C(=O)NC(CC(=O)N)C(=O)NC(Cc5c[nH]c6c5cccc6)C(=O)NC(Cc7ccccc7)C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CO)NC(=O)C(Cc8cnc[nH]8)NC(=O)C(C(C)CC)NC(=O)C(CC(C)C)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(Cc9ccc(cc9)O)NC(=O)C
  • InChI=1S/C204H301N51O64/c1-20-102(15)166(253-195(310)137(75-100(11)12)239-200(315)150(93-258)251-190(305)143(82-112-90-215-95-219-112)248-203(318)167(103(16)21-2)254-196(311)138(76-101(13)14)240-201(316)151(94-259)252-204(319)168(105(18)260)255-197(312)139(221-106(19)261)78-108-45-47-113(262)48-46-108)202(317)233-131(58-68-164(280)281)178(293)228-130(57-67-163(278)279)182(297)250-149(92-257)198(313)232-125(52-62-155(210)266)179(294)245-145(84-157(212)268)191(306)229-124(51-61-154(209)265)175(290)224-122(49-59-152(207)263)173(288)226-126(53-63-159(270)271)176(291)222-120(43-31-33-69-205)172(287)244-144(83-156(211)267)192(307)231-127(54-64-160(272)273)177(292)225-123(50-60-153(208)264)174(289)227-128(55-65-161(274)275)180(295)235-134(72-97(5)6)185(300)237-133(71-96(3)4)184(299)230-129(56-66-162(276)277)181(296)236-135(73-98(7)8)187(302)247-147(86-165(282)283)194(309)223-121(44-32-34-70-206)171(286)241-140(79-109-87-216-117-40-28-25-37-114(109)117)183(298)220-104(17)170(285)249-148(91-256)199(314)238-136(74-99(9)10)186(301)242-142(81-111-89-218-119-42-30-27-39-116(111)119)189(304)246-146(85-158(213)269)193(308)243-141(80-110-88-217-118-41-29-26-38-115(110)118)188(303)234-132(169(214)284)77-107-35-23-22-24-36-107/h22-30,35-42,45-48,87-90,95-105,120-151,166-168,216-218,256-260,262H,20-21,31-34,43-44,49-86,91-94,205-206H2,1-19H3,(H2,207,263)(H2,208,264)(H2,209,265)(H2,210,266)(H2,211,267)(H2,212,268)(H2,213,269)(H2,214,284)(H,215,219)(H,220,298)(H,221,261)(H,222,291)(H,223,309)(H,224,290)(H,225,292)(H,226,288)(H,227,289)(H,228,293)(H,229,306)(H,230,299)(H,231,307)(H,232,313)(H,233,317)(H,234,303)(H,235,295)(H,236,296)(H,237,300)(H,238,314)(H,239,315)(H,240,316)(H,241,286)(H,242,301)(H,243,308)(H,244,287)(H,245,294)(H,246,304)(H,247,302)(H,248,318)(H,249,285)(H,250,297)(H,251,305)(H,252,319)(H,253,310)(H,254,311)(H,255,312)(H,270,271)(H,272,273)(H,274,275)(H,276,277)(H,278,279)(H,280,281)(H,282,283)/t102-,103-,104-,105+,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,166-,167-,168-/m0/s1 ДаY
  • Key:PEASPLKKXBYDKL-FXEVSJAOSA-N ДаY

Strukturna formula уреди

 

Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH2

Reference уреди

  1. ^ Greenberg ML, Cammack N: Resistance to enfuvirtide, the first HIV fusion inhibitor. J Antimicrob Chemother. 2004 Aug;54(2):333-40. Epub 2004 Jul 1. PMID 15231762
  2. ^ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035—41. PMID 21059682. 
  3. ^ Wishart DS, Knox C, Guo AC, Cheng D, Shrivastava S, Tzur D, Gautam B, Hassanali M (Nucleic Acids Res) (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. 36 (Database issue): D901—6. PMID 18048412. 

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