ChemInform Abstract: DERIVATIVES OF MYCOPHENOLIC ACID

1978 ◽  
Vol 9 (21) ◽  
Author(s):  
R. M. CARMAN
Keyword(s):  
Mycophenolic Acid ◽  
Derivatives Of

Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid

2020 ◽  
Vol 189 ◽  
pp. 112091
Author(s):  
Agnieszka Siebert ◽  
Grzegorz Cholewiński ◽  
Piotr Trzonkowski ◽  
Janusz Rachon
Keyword(s):  
Amino Acid ◽  
Mycophenolic Acid ◽  
Peptide Derivatives ◽  
Derivatives Of

Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cells

2017 ◽  
Vol 44 ◽  
pp. 137-142 ◽  
Author(s):  
Dorota Iwaszkiewicz-Grzes ◽  
Grzegorz Cholewinski ◽  
Agata Kot-Wasik ◽  
Piotr Trzonkowski ◽  
Krystyna Dzierzbicka
Keyword(s):  
Dendritic Cells ◽  
Mycophenolic Acid ◽  
Immunosuppressive Activity ◽  
Immature Dendritic Cells ◽  
Derivatives Of

scholarly journals Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid

2018 ◽  
Vol 143 ◽  
pp. 646-655 ◽  
Author(s):  
Agnieszka Siebert ◽  
Magdalena Wysocka ◽  
Beata Krawczyk ◽  
Grzegorz Cholewiński ◽  
Janusz Rachoń
Keyword(s):  
Antimicrobial Activity ◽  
Amino Acid ◽  
Mycophenolic Acid ◽  
Peptide Derivatives ◽  
Derivatives Of

scholarly journals Application of Docking Analysis in the Prediction and Biological Evaluation of the Lipoxygenase Inhibitory Action of Thiazolyl Derivatives of Mycophenolic Acid

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1621 ◽  
Author(s):  
Evangelia Tsolaki ◽  
Phaedra Eleftheriou ◽  
Victor Kartsev ◽  
Athina Geronikaki ◽  
Anil K. Saxena
Keyword(s):  
Mycophenolic Acid ◽  
Inhibitory Action ◽  
Biological Evaluation ◽  
Docking Analysis ◽  
Derivatives Of

Derivatives of mycophenolic acid

1978 ◽  
Vol 31 (2) ◽  
pp. 353 ◽  
Author(s):  
RM Carman
Keyword(s):  
Mycophenolic Acid ◽  
Derivatives Of

Derivatives of mycophenolic acid and of mycochromenic acid are reported. These compounds include a relatively stable tertiary iodide.

4-Methyl- and 7-methylphthalan-1-one derivatives of mycophenolic acid

Tetrahedron ◽  
1981 ◽  
Vol 37 (11) ◽  
pp. 2131-2136 ◽  
Author(s):  
N.J. McCorkindale ◽  
R.L. Baxter ◽  
W.B. Turner
Keyword(s):  
Mycophenolic Acid ◽  
Derivatives Of

Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid

2020 ◽  
Vol 20 ◽  
Author(s):  
Agnieszka Siebert ◽  
Milena Deptuła ◽  
Mirosława Cichorek ◽  
Anna Ronowska ◽  
Grzegorz Cholewiński ◽  
...  
Keyword(s):  
Amino Acid ◽  
Cell Lines ◽  
Anticancer Agents ◽  
Mycophenolic Acid ◽  
Methyl Esters ◽  
Carboxylic Group ◽  
Anticancer Properties ◽  
Peptide Derivatives ◽  
Derivatives Of

Background: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as immunosuppressant, it possesses also anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent anticancer agents like dacarbazine and cisplatin give numerous side-effects. Objective: Based on the literature data, MPA derivatives should be explored towards anticancer properties. Conversion of carboxylic group of MPA to amide could maintain antiproliferative activity. Therefore, we decided to investigate several amino acid and peptide derivatives of MPA against chosen cancer cell lines in vitro. Methods: Amides of MPA hold threonine and arginine amino acid unit. These amino acid derivatives were tested as L and D enantiomers and both in free acid and methyl esters forms. Additionally, MPA was modified with tuftsin or retro-tuftsin as biologically active peptides, which could act as a drug carrier. Results: Amino acid and peptide derivatives of MPA were investigated in vitro as potential anticancer agents on cell lines: Ab melanoma, A375 melanoma and SHSY5Y neuroblastoma. The activity of the tested compounds was compared to parent MPA and known chemotherapeutics: dacarbazine and cisplatin. Conclusion: Amino acid moiety and sequence of amino acids in peptide part influenced observed activity. The most active amino acid MPA analogues occurred to be D and L-threonine derivatives as methyl esters, probably due to better cell membrane penetration.

Hydroxamic Acid Derivatives of Mycophenolic Acid Inhibit Histone Deacetylase at the Cellular Level

2008 ◽  
Vol 72 (10) ◽  
pp. 2623-2631 ◽  
Author(s):  
Daniela I. BATOVSKA ◽  
Dong Hoon KIM ◽  
Shinya MITSUHASHI ◽  
Yoon Sun CHO ◽  
Ho Jeong KWON ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Mycophenolic Acid ◽  
Hydroxamic Acid ◽  
Cellular Level ◽  
Derivatives Of ◽  
Hydroxamic Acid Derivatives

scholarly journals Antitumor activity of derivatives of mycophenolic acid.

1976 ◽  
Vol 29 (3) ◽  
pp. 275-285 ◽  
Author(s):  
SEIKICHI SUZUKI ◽  
SAKAE TAKAKU ◽  
TAKASHI MORI
Keyword(s):  
Antitumor Activity ◽  
Mycophenolic Acid ◽  
Derivatives Of

scholarly journals IMP Dehydrogenase from the Protozoan Parasite Toxoplasma gondii

2005 ◽  
Vol 49 (6) ◽  
pp. 2172-2179 ◽  
Author(s):  
William J. Sullivan ◽  
Stacy E. Dixon ◽  
Catherine Li ◽  
Boris Striepen ◽  
Sherry F. Queener
Keyword(s):  
Toxoplasma Gondii ◽  
Mycophenolic Acid ◽  
De Novo ◽  
Protozoan Parasite ◽  
Gene Encoding ◽  
Imp Dehydrogenase ◽  
Reading Frame ◽  
Folate Pathway ◽  
Acid Protein ◽  
Derivatives Of

ABSTRACT The opportunistic apicomplexan parasite Toxoplasma gondii damages fetuses in utero and threatens immunocompromised individuals. The toxicity associated with standard antitoxoplasmal therapies, which target the folate pathway, underscores the importance of examining alternative pharmacological strategies. Parasitic protozoa cannot synthesize purines de novo; consequently, targeting purine salvage enzymes is a plausible pharmacological strategy. Several enzymes critical to purine metabolism have been studied in T. gondii, but IMP dehydrogenase (IMPDH), which catalyzes the conversion of IMP to XMP, has yet to be characterized. Thus, we have cloned the gene encoding this enzyme in T. gondii. Northern blot analysis shows that two IMPDH transcripts are present in T. gondii tachyzoites. The larger transcript contains an open reading frame of 1,656 nucleotides whose deduced protein sequence consists of 551 amino acids (TgIMPDH). The shorter transcript is an alternative splice product that generates a 371-amino-acid protein lacking the active-site flap (TgIMPDH-S). When TgIMPDH is expressed as a recombinant protein fused to a FLAG tag, the fusion protein localizes to the parasite cytoplasm. Immunoprecipitation with anti-FLAG was employed to purify recombinant TgIMPDH, which converts IMP to XMP as expected. Mycophenolic acid is an uncompetitive inhibitor relative to NAD+, with a intercept inhibition constant (Kii ) of 0.03 ± 0.004 μM. Tiazofurin and its seleno analog were not inhibitory to the purified enzyme, but adenine dinucleotide analogs such as TAD and the nonhydrolyzable β-methylene derivatives of TAD or SAD were inhibitory, with Kii values 13- to 60-fold higher than that of mycophenolic acid.

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