42362-08-3Relevant articles and documents
LIVER X RECEPTOR AGONISTS AND USES THEREOF
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Paragraph 0130; 0131, (2016/11/28)
Disclosed herein are antibody drug conjugates having an antibody or antibody fragment that binds a cell surface molecule on a target cell, wherein the target cell is a lymphocyte and a therapeutic agent that has a therapeutic effect in a subject in need t
Vinyl sulfone-based peptidomimetics as anti-trypanosomal agents: Design, synthesis, biological and computational evaluation
Dunny, Elizabeth,Doherty, William,Evans, Paul,Malthouse, J. Paul G.,Nolan, Derek,Knox, Andrew J.S.
, p. 6638 - 6650 (2013/10/01)
A series of vinyl sulfone-containing peptidomimetics were rationally designed, synthesized, and evaluated against Trypanosoma brucei brucei. These electrophilic compounds are likely to exert their antitrypanosomal activity via inhibition of trypanosomal cysteine proteases, TbCatB and rhodesain, through alkylation of a key cysteine residue within the protease active site. The series was designed to present complementary groups to naturally recognized peptide substrates while probing tolerance to a range of substitutions at the P1, P1′, and P2 positions. The most potent compound, 29 (EC50 = 70 nM, T. b. brucei whole cell assay), displayed minimal toxicity (>785 times selectivity) when assayed for cytotoxicity against the human promyelocytic leukemia (HL-60) cell line. Cells treated with compound 29, as with K777 (2), exhibited an increase in both the number of multinucleated cells and cells with swollen flagellar pockets. Computational analysis revealed a strong correlation between the hypothetical binding mode in TbCatB/rhodesain and trypanocidal activity in vitro.
Conventional Synthesis of a Selective Peptide Substrate for Measurements of Protein Kinase C
Spencker, Torsten,Goppelt-Struebe, Margarete,Keese, Wolfgang,Resch, Klaus,Rimpler, Manfred
, p. 237 - 240 (2007/10/02)
Protein kinase C (PKC), a family of serin/threonin kinases, plays a key role in signal transduction.We have prepared the PKC-selective peptide substrate H-Phe-Lys-Lys-Ser-Phe-Lys-Leu-NH2 (7) by classical solution synthesis. 7 allows PKC-measurements in cr