- ACYLATION OF TYROSINE UNITS IN PEPTIDE COMPOUNDS
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The present invention refers to a process for the selective modification of tyrosine units in a peptide sequence, in particular, by incorporating acyl groups in the ortho position of the hydroxyl residue of its aromatic ring. Likewise, the invention also
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Page/Page column 25; 26
(2021/08/27)
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- Phosphotyrosine prodrugs: design, synthesis and anti-STAT3 activity of ISS-610 aryloxy triester phosphoramidate prodrugs
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Unmasked phohate groups of phosphotyrosine-containing molecules carry two negative charges at physiological pH, which compromise their (passive) cellular uptake. Also, these phosphate groups are often cleaved off by phosphatases. Together, these ultimatel
- Miccoli, Ageo,Dhiani, Binar A.,Mehellou, Youcef
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p. 200 - 208
(2019/03/05)
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- Design, synthesis and biological evaluation of novel L-isoserine tripeptide derivatives as aminopeptidase N inhibitors
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Aminopeptidase N (APN/CD13) is one of the essential proteins for tumour invasion, angiogenesis and metastasis as it is over-expressed on the surface of different tumour cells. Based on our previous work that L-isoserine dipeptide derivatives were potent APN inhibitors, we designed and synthesized L-isoserine tripeptide derivatives as APN inhibitors. Among these compounds, one compound 16l (IC50=2.51±0.2 M) showed similar inhibitory effect compared with control compound Bestatin (IC50=6.25±0.4 M) and it could be used as novel lead compound for the APN inhibitors development as anticancer agents in the future.
- Pan, Huili,Yang, Kanghui,Zhang, Jian,Xu, Yingying,Jiang, Yuqi,Yuan, Yumei,Zhang, Xiaopan,Xu, Wenfang
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p. 717 - 726
(2013/07/26)
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- Helical pores self-assembled from homochiral dendritic dipeptides based on L-Tyr and nonpolar α-amino acids
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The synthesis of dendritic dipeptides (4-3,4-3,5)12G2-CH 2-Boc-L-Tyr-X-OMe where X = Gly, L-Val, L-Leu, L-lle, L-Phe, and L-Pro is reported. Their self-assembly in bulk and in solution and the structural and retrostructural analysis of their pe
- Percec, Virgil,Dulcey, Andres E.,Peterca, Mihai,Adelman, Peter,Samant, Ritika,Balagurusamy, Venkatachalapathy S. K.,Heiney, Paul A.
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p. 5992 - 6002
(2008/02/04)
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- Synthetic and biological activity studies on a new cyclic pentapeptide, cyclonitroproctolin
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The synthesis of a new biologically active cyclic pentapeptide, cyclonitroproctolin, cyclo(-Arg (NO2)-Tyr-Leu-Pro-Thr-) by solution phase synthesis is described. The structure of the synthetic peptide was characterized by IR, NMR, FAB mass and
- Poojary, Boja,Belagali, Shiddappa L.
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p. 1308 - 1312
(2008/02/08)
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- ENZYMATIC PEPTIDE SYNTHESIS IN ORGANIC SOLVENT MEDIATED BY MODIFIED α-CHYMOTRYPSIN
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Peptide couplings have been catalyzed in organic medium containing a slight amount of water (0.5percent) by PEG modified α-Chymotrypsin.
- Babonneau, Marie-Therese,Jacquier, Robert,Lazaro, Rene,Viallefont, Philippe
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p. 2787 - 2790
(2007/10/02)
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