1381868-47-8Relevant articles and documents
SYNTHETIC INNATE IMMUNE RECEPTOR LIGANDS AND USES THEREOF
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Paragraph 0052; 0081, (2020/06/10)
An adjuvant formulation includes a monophosphoryl Lipid A (MPLA) analogue, a Pam3CSK4 analogue, or a muramyldipeptide (MDP) analogue, or combinations thereof. The adjuvant may be formulated in soluble form or in a nanoparticle, such as polylactic glycolic acid nanoparticles. A vaccine formulation comprises the adjuvant formulation and an immunogen. Methods of vaccinating an animal include delivering the vaccine formulation to the animal.
Design and synthesis of potent, selective inhibitors of matriptase
Colombo, Eloic,Desilets, Antoine,Duchene, Dominic,Chagnon, Felix,Najmanovich, Rafael,Leduc, Richard,Marsault, Eric
supporting information; experimental part, p. 530 - 534 (2012/08/29)
Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a potential target for cancer therapy. We report herein a new series of slow, tight-binding inhibitors of matriptase, which mimic the P1-P4 substrate recognition sequence of the enzyme. Preliminary structure-activity relationships indicate that this benzothiazole-containing RQAR-peptidomimetic is a very potent inhibitor and possesses a good selectivity for matriptase versus other serine proteases. A molecular model was generated to elucidate the key contacts between inhibitor 1 and matriptase.
