Protease inhibitors from a water bloom of the cyanobacterium Microcystis aeruginosa
摘要:
Five new protease inhibitors, micropeptins SD944 (1), SD979 (2), SD999 (3) and SD1002 (4) and microginin SD755 (5) were isolated along with two known inhibitors, micropeptin SF995 (6) and microcin SF608 (7), from the hydrophilic extract of Microcystis aeruginosa. The planar structure of compounds 1-5 was determined by homonuclear and inverse-heteronuclear 2D-NMR techniques as well as high-resolution mass spectrometry. The absolute configuration of the asymmetric centers was studied using Marfey's method for HPLC. Compounds 1-4, 6 and 7 are serine-protease inhibitors while compound 5 was found to inhibit amino-proteases. (C) 2001 Elsevier Science Ltd. All rights reserved.
IDO1 INHIBITOR AND PREPARATION METHOD AND APPLICATION THEREOF
申请人:SHANDONG LUYE PHARMACEUTICAL CO., LTD.
公开号:US20190169140A1
公开(公告)日:2019-06-06
A compound as an indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, and an application thereof in the field of IDO1-related diseases, and in particular a compound as shown in formula (I) and a pharmaceutically acceptable salts thereof.
Isotopic methods for measurement of tryptophan and metabolites thereof
申请人:ELECTROPHORETICS LIMITED
公开号:US11320438B2
公开(公告)日:2022-05-03
Tryptophan degradation is a key metabolic pathway controlling immune reactions and evidence suggests that during cancer progression generation of tryptophan metabolites may be fundamental for immune escape promoting the malignant phenotype of cancer cells in an autocrine fashion. The present invention relates to methods of measuring mass tag labelled tryptophan and metabolites thereof and methods using the labelled molecules for monitoring in a subject the effectiveness of a treatment and of disease recurrence after treatment, for stratifying patients and for diagnosing suppression of an immune response in a subject.
ISOTOPIC METHODS FOR MEASUREMENT OF TRYPTOPHAN AND METABOLITES THEREOF
申请人:Electrophoretics Limited
公开号:EP3368905A1
公开(公告)日:2018-09-05
[EN] ISOTOPIC METHODS FOR MEASUREMENT OF TRYPTOPHAN AND METABOLITES THEREOF<br/>[FR] PROCÉDÉS ISOTOPIQUES POUR MESURE DE TRYPTOPHANE ET DE SES MÉTABOLITES
申请人:ELECTROPHORETICS LTD
公开号:WO2017072368A1
公开(公告)日:2017-05-04
Tryptophan degradation is a key metabolic pathway controlling immune reactions and evidence suggests that during cancer progression generation of tryptophan metabolites may be fundamental for immune escape promoting the malignant phenotype of cancer cells in an autocrine fashion. The present invention relates to methods of measuring mass tag labelled tryptophan and metabolites thereof and methods using the labelled molecules for monitoring in a subject the effectiveness of a treatment and of disease recurrence after treatment, for stratifying patients and for diagnosing suppression of an immune response in a subject.
Cyclic lipopeptides having one or more modifications relative to daptomycin, and methods of making them are provided. The cyclic lipopeptides can be used as antibacterial agents. The daptomycin analogues are generated by chemical synthesis, which makes introduction of an unnatural amino acid and any modification into daptomycin possible. Pharmaceutical compositions and method of use thereof for the disclosed daptomycin analogues are also provided.