Large-scale manufacture of peptide therapeutics by chemical synthesis

被引:475
作者
Bray, BL [1 ]
机构
[1] Trimeris Inc, Durham, NC 27707 USA
关键词
D O I
10.1038/nrd1133
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
The large-scale commercial production of a 36-amino-acid peptide by chemical synthesis has been demonstrated in the development of enfuvirtide (T-20 or Fuzeon), a first-in-class membrane fusion inhibitor for the treatment of HIV. The rationale behind route selection and the scale-up of the process used to manufacture enfuvirtide are discussed.
引用
收藏
页码:587 / 593
页数:7
相关论文
共 27 条
[1]   MILD PROCEDURE FOR SOLID-PHASE PEPTIDE-SYNTHESIS - USE OF "FLUORENYLMETHOXYCARBONYLAMINO-ACIDS [J].
ATHERTON, E ;
FOX, H ;
HARKISS, D ;
LOGAN, CJ ;
SHEPPARD, RC ;
WILLIAMS, BJ .
JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS, 1978, (13) :537-539
[2]   APPLICATION OF POLYAMIDE RESINS TO POLYPEPTIDE-SYNTHESIS - IMPROVED SYNTHESIS OF BETA-ENDORPHIN USING "FLUORENYLMETHOXYCARBONYLAMINO-ACIDS [J].
ATHERTON, E ;
FOX, H ;
HARKISS, D ;
SHEPPARD, RC .
JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS, 1978, (13) :539-540
[3]   SYNTHESIS OF PROTHYMOSIN ALPHA (PRO T-ALPHA) - A PROTEIN CONSISTING OF 109 AMINO-ACID-RESIDUES [J].
BARLOS, K ;
GATOS, D ;
SCHAFER, W .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION IN ENGLISH, 1991, 30 (05) :590-593
[4]   ESTERIFICATION OF PARTIALLY PROTECTED PEPTIDE-FRAGMENTS WITH RESINS - UTILIZATION OF 2-CHLOROTRITYLCHLORIDE FOR SYNTHESIS OF LEU-15-GASTRIN-I [J].
BARLOS, K ;
GATOS, D ;
KAPOLOS, S ;
PAPAPHOTIU, G ;
SCHAFER, W ;
YAO, WQ .
TETRAHEDRON LETTERS, 1989, 30 (30) :3947-3950
[5]   SYNTHESIS OF PROTECTED PEPTIDE-FRAGMENTS USING SUBSTITUTED TRIPHENYLMETHYL RESINS [J].
BARLOS, K ;
GATOS, D ;
KALLITSIS, J ;
PAPAPHOTIU, G ;
SOTIRIU, P ;
YAO, WQ ;
SCHAFER, W .
TETRAHEDRON LETTERS, 1989, 30 (30) :3943-3946
[6]  
BENOITON NL, 1992, PEPTIDES CHEM BIOL, P496
[7]  
Bodanszky M., 1993, PRINCIPLES PEPTIDE S, V2nd
[8]   PEPTIDE-SYNTHESIS .13. FEEDBACK-CONTROL IN SOLID-PHASE SYNTHESIS - USE OF FLUORENYLMETHOXYCARBONYL AMINO-ACID 3,4-DIHYDRO-4-OXO-1,2,3-BENZOTRIAZIN-3-YL ESTERS IN A FULLY AUTOMATED-SYSTEM [J].
CAMERON, LR ;
HOLDER, JL ;
MELDAL, M ;
SHEPPARD, RC .
JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1988, (10) :2895-2901
[9]   9-FLUORENYLMETHOXYCARBONYL AMINO-PROTECTING GROUP [J].
CARPINO, LA ;
HAN, GY .
JOURNAL OF ORGANIC CHEMISTRY, 1972, 37 (22) :3404-&
[10]   NEW AMINO-PROTECTING GROUPS IN ORGANIC SYNTHESIS [J].
CARPINO, LA .
ACCOUNTS OF CHEMICAL RESEARCH, 1973, 6 (06) :191-198