scholarly journals Design, synthesis and biological evaluation of a new bridged immunosuppressor.

2001 ◽  
Vol 48 (4) ◽  
pp. 1147-1150 ◽  
Author(s):  
Z Szewczuk ◽  
A Wilczyński ◽  
I Petry ◽  
I Z Siemion ◽  
Z Wieczorek
Keyword(s):  
Immune Response ◽  
Humoral Immune Response ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Discontinuous Epitope ◽  
Humoral Immune ◽  
Hla Dq ◽  
Synthesis And Biological Evaluation

A bridged peptide with the sequence: H-Thr-Pro-Gln-Arg-Gly-Asp-Val-gamma-Abu-Asn-Asp-Gln-Glu-Glu-Thr-Thr-Gly-Val-Val-Ser-Thr-Pro-Leu-Ile-Arg-Asn-Gly-OH was designed to mimic the discontinuous epitope of the HLA-DQ molecule that might interact with CD4. The bridged peptide revealed distinct suppressory effect in the humoral immune response. This result supports our suggestion that the 164-172 region of the HLA-DQ molecule may enhance its interactions with coreceptors, possibly with CD4.

scholarly journals Design, Synthesis, and Biological Evaluation of Desmuramyl Dipeptides Modified by Adamantyl-1,2,3-triazole

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6352
Author(s):  
Vesna Petrović Peroković ◽  
Željka Car ◽  
Josip Draženović ◽  
Ranko Stojković ◽  
Lidija Milković ◽  
...  
Keyword(s):  
Immune Response ◽  
Murine Model ◽  
Structural Modification ◽  
Muramyl Dipeptide ◽  
Biological Evaluation ◽  
Adjuvant Activity ◽  
Design Synthesis ◽  
C Terminus ◽  
Synthesis And Biological Evaluation

Muramyl dipeptide (MDP) is the smallest peptidoglycan fragment able to trigger the immune response. Structural modification of MDP can lead to the preparation of analogs with improved immunostimulant properties, including desmuramyl peptides (DMPs). The aim of this work was to prepare the desmuramyl peptide (L-Ala-D-Glu)-containing adamantyl-triazole moiety and its mannosylated derivative in order to study their immunomodulatory activities in vivo. The adjuvant activity of the prepared compounds was evaluated in a murine model using ovalbumin as an antigen, and compared to the reference adjuvant ManAdDMP. The results showed that the introduction of the lipophilic adamantyl-triazole moiety at the C-terminus of L-Ala-D-Glu contributes to the immunostimulant activity of DMP, and that mannosylation of DMP modified with adamantyl-triazole causes the amplification of its immunostimulant activity.

Design, Synthesis and Biological Evaluation of Hybrid Molecules Containing Conjugated Styryl Ketone and α-Bromoacryloyl Moieties

2012 ◽  
Vol 9 (2) ◽  
pp. 140-152 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Giovanni Baraldi ◽  
Olga Cruz-Lopez ◽  
Maria Kimatrai Salvador ◽  
Delia Preti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Hybrid Molecules ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Benzopyran Derivatives as KATP Channel Openers

2010 ◽  
Vol 7 (6) ◽  
pp. 415-420 ◽  
Author(s):  
Jinpei Zhou ◽  
Hai Qian ◽  
Huibin Zhang ◽  
Hui Gao ◽  
Wenlong Huang ◽  
...  
Keyword(s):  
Katp Channel ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Katp Channel Openers
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