32886-40-1Relevant academic research and scientific papers
PHARMACEUTICAL COMPOSITION COMPRISING THE PEPTIDE GLU-ASP-GLY AND USE FOR TREATING HELICOBACTER PYLORI INDUCED GASTRODUODENAL DISEASES
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Paragraph 0045, (2015/12/31)
The invention relates to medicinal means on the basis of a peptide pharmaceutical composition for treatment of Helicobacter pylori-induced gastroduodenal diseases. The technical result of the invention consists in the peptide glutamyl-aspartyl-glycine wit
Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors
Nakamura, Hiroyuki,Watanabe, Mizuyoshi,Ban, Hyun Seung,Nabeyama, Wataru,Asai, Akira
scheme or table, p. 3220 - 3224 (2010/04/05)
A series of boron peptides 11, 13, 15 and 17 were designed and synthesized as proteasome inhibitors based on the structure of Belactosin C. Matteson homologation was a key step in the synthesis of the boron peptides. Compounds 11a and 13 showed significant inhibition of 20S proteasome chymotrypsin-like (β5) activity (IC50 = 0.28 and 0.51 μM, respectively). Furthermore, like PS-341, compound 11a increased the G2/M cell distribution. A biparametric cytofluorimetric analysis with FITC-labeled annexin V and propidium iodide showed induction of apoptosis by compound 11a at >1 μM concentrations of compound.
Synthesis and neuroprotective activity of analogues of glycyl-L-prolyl-L- glutamic acid (GPE) modified at the α-carboxylic acid
Trotter, Nicholas S.,Brimble, Margaret A.,Harris, Paul W.R.,Callis, David J.,Sieg, Frank
, p. 501 - 517 (2007/10/03)
The synthesis of nine GPE* analogues, wherein the α-carboxylic acid group of glutamic acid has been modified, is described by coupling readily accessible N-benzyloxycarbonyl-glycyl-l-proline 2 with various analogues of glutamic acid. Pharmacological evaluation of the novel compounds was undertaken to further understand the role of the glutamate residue on the observed neuroprotective properties of the endogenous tripeptide GPE.
Macromolecular self-assembly of diketopiperazine tetrapeptides
Bergeron, Raymond J.,Phanstiel IV, Otto,Yao, Guo Wei,Milstein, Sam,Weimar, William R.
, p. 8479 - 8484 (2007/10/02)
Basic solutions of tetrapeptides derived from L-aspartic acid diketopiperazines are shown to form microcapsules when acidified to pH 2.4. An initial structure-activity study clearly demonstrates that a very delicate balance exists between the tetrapeptide
LARGE-SCALE SYNTHESIS OF ANTICOAGULANT DECAPEPTIDE MDL 28050
Hoekstra, William J.,Sunder, Shyam S.,Cregge, Robert J.,Ashton, Louis A.,Stewart, Kenneth T.,King, Chi-Hsin R.
, p. 307 - 318 (2007/10/02)
A solution phase synthesis of the anticoagulant decapeptide Suc-Tyr-Glu-Pro-Ile-Pro-Glu-Glu-Ala-Cha-D-Glu-OH ( 1, MDL 28050) on a large scale is decribed.Our strategy employed in the 24-step total synthesis relies on a convergent approach.The basic feature is the preparation and the coupling of two protected pentapeptides, 2 and 3.Several key intermediates were purified by crystallizations including the protected decapeptide 21.Only a single purification required preparative HPLC.Using this synthetic route, we prepared 98percent pure final product on a 40-g scale.The overall yield of this process is about 20percent.
SOLUTION PHASE SYNTHESIS OF ALAMETHICIN I
Nagaraj, R.,Balaram, P.
, p. 1263 - 1270 (2007/10/02)
The total synthesis of alamethicin I by solution phase methods is reported.
Synthesis of the Major Component of Alamethicin
Gisin, B.F.,Davis, D.G.,Borowska, Z.K.,Hall, J.E.,Kobayashi, S.
, p. 6373 - 6377 (2007/10/02)
Alamethicin (ALA), a natural membrane-active antibiotic, consists of several components.The major component, ALA I, was isolated in pure form and compared with the synthetic peptide acetyl-Aib-Pro-Aib-Ala-Aib-Ala-Gln-Aib-Val-Aib-Gly-Leu-Aib-Pro-Val-Aib-Aib-Glu-Gln-Phol obtained by stepwise segment condensation on a polystyrene support.The synthetic and natural products appeared essentially identical by amino acid analysis, high performance liquid chromatography, 600-MHz proton nuclear magnetic resonance spectroscopy, mass spectrometry, electrical activity in lipid bilayer membranes, and antimicrobial activity.It is concluded that ALA I has the structure indicated above.
