scholarly journals Synthesis of N-Peptide-6-Amino-d-Luciferin Conjugates with Optimized Fragment Condensation Strategy

2018 ◽  
Vol 25 (3) ◽  
pp. 1209-1215
Author(s):  
Anita K. Kovács ◽  
Péter Hegyes ◽  
Gábor J. Szebeni ◽  
Krisztián Bogár ◽  
László G. Puskás ◽  
...  
Keyword(s):  
Fragment Condensation

Oxytocin analogues with non-coded amino acid residues in position 8: [8-Neopentylglycine]oxytocin and [8-cycloleucine]oxytocin

1987 ◽  
Vol 52 (9) ◽  
pp. 2317-2325 ◽  
Author(s):  
Jan Hlaváček ◽  
Jan Pospíšek ◽  
Jiřina Slaninová ◽  
Walter Y. Chan ◽  
Victor J. Hruby
Keyword(s):  
Amino Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
The Other ◽  
Amino Acid Residues ◽  
Phase Synthesis ◽  
Other Hand ◽  
Fragment Condensation

[8-Neopentylglycine]oxytocin (II) and [8-cycloleucine]oxytocin (III) were prepared by a combination of solid-phase synthesis and fragment condensation. Both analogues exhibited decreased uterotonic potency in vitro, each being about 15-30% that of oxytocin. Analogue II also displayed similarly decreased uterotonic potency in vivo and galactogogic potency. On the other hand, analogue III exhibited almost the same potency as oxytocin in the uterotonic assay in vivo and in the galactogogic assay.

Inhibitors of pancreatic and leukocyte elastase

1987 ◽  
Vol 52 (12) ◽  
pp. 3034-3041 ◽  
Author(s):  
Evžen Kasafírek ◽  
Přemysl Frič ◽  
Jan Slabý ◽  
Petr Kocna
Keyword(s):  
Leukocyte Elastase ◽  
Pancreatic Elastase ◽  
Fragment Condensation ◽  
Inhibition Constants

The following alkylamides of ω-carboxyalkanoyldi- and tripeptides of the Ala-Pro or Ala-Ala-Pro sequence have been prepared: ethylamide-, propylamide-, and isobutylamide of 3-carboxypropionylalanyl-proline, ethylamide of 3-carboxypropionylalanyl-alanyl-proline and ethylamide-, propylamide, and isobutylamide of 4-carboxybutyrylalanyl-alanyl-proline. The inhibitors were synthesized by fragment condensation in solution or by gradual construction. The inhibition constants Ki were determined by means of pancreatic elastase (substrates - p-nitroanilides of 4-carboxybutyrylalanyl-alanyl-alanyl-alanine and 3-carboxypropionylalanyl-alanyl-alanyl-alanine) and leukocyte elastase (substrate - p-nitroanilide of 4-carboxybutyrylalanyl-alanyl-alanyl-valine). The strongest inhibitions (Ki) were recorded in ethylamide of 4-carboxybutyrylalanyl-alanyl-proline, 2.0 and 1.6 μmol l-1 for pancreatic elastase, and in propylamide of 4-carboxybutyrylalanyl-alanyl-proline, 0.4 mmol l-1 for leukocyte elastase.

Preparation and properties of three analogues of [5-leucine]enkephalin, substrates for enzyme conversion studies

1985 ◽  
Vol 50 (6) ◽  
pp. 1329-1334
Author(s):  
Jaroslav Vičar ◽  
Linda Servítová ◽  
Martin Flegel ◽  
Karel Hauzer ◽  
Tomislav Barth
Keyword(s):  
High Pressure ◽  
Liquid Chromatography ◽  
Guinea Pig ◽  
Ion Exchange Chromatography ◽  
Exchange Chromatography ◽  
Guinea Pig Ileum ◽  
Opioid Activity ◽  
C Terminus ◽  
N Terminus ◽  
Fragment Condensation

Analogues of [5-Leu]enkephalin, prolonged by methionine on the N-terminus or, by lysine or methionine on the C-terminus were prepared by fragment condensation, purified by ion exchange chromatography or high-pressure liquid chromatography. The substances were characterised by their opioid activity in a test on guinea-pig ileum in comparison with the activity of [5-Leu]enkephalin.

Synthesis of homologous peptides using fragment condensation: analogs of an HIV proteinase substrate

2009 ◽  
Vol 38 (5) ◽  
pp. 453-458 ◽  
Author(s):  
IVO BLÁHA ◽  
JOSEF NEMEC ◽  
JÓZSEF TÖZSÉR ◽  
STEPHEN OROSZLAN
Keyword(s):  
Fragment Condensation

Solid-phase fragment condensation for synthesis of peptides from the immunodominant sequence of β1-adrenoreceptor

2017 ◽  
Vol 43 (4) ◽  
pp. 351-358 ◽  
Author(s):  
M. V. Sidorova ◽  
M. E. Palkeeva ◽  
A. A. Az’muko ◽  
M. V. Ovchinnikov ◽  
A. S. Molokoedov ◽  
...  
Keyword(s):  
Solid Phase ◽  
Fragment Condensation

Synthesis of thymosin α1 by fragment condensation using tert.-butyl side chain protection

2009 ◽  
Vol 26 (2) ◽  
pp. 130-148 ◽  
Author(s):  
ARTHUR M. FELIX ◽  
EDGAR P. HEIMER ◽  
CHING-TSO WANG ◽  
THEODORE J. LAMBROS ◽  
JOSEPH SWISTOK ◽  
...  
Keyword(s):  
Side Chain ◽  
Thymosin Α1 ◽  
Tert Butyl ◽  
Fragment Condensation

Solid-phase synthesis of carboxyamidomethyl peptide esters: Application to enzymatic fragment condensation

Peptides 1992 ◽  
1993 ◽  
pp. 423-424 ◽  
Author(s):  
P. Clapés ◽  
Y. M. Sanchez ◽  
F. Albericio ◽  
J. L. Torres ◽  
G. Valencia
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Phase Synthesis ◽  
Fragment Condensation ◽  
Peptide Esters
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