Drug intelligence / Profile preview

aeruginosin 98-b

Development stage
Unknown
Modality
Peptides, Small Molecules
01

Overview

Aeruginosin 98-B is a bioactive small molecule natural product belonging to the aeruginosin family of oligopeptides produced by cyanobacteria such as Microcystis aeruginosa. It is characterized structurally as a dipeptide with unique moieties including Choi and guanidinobutyl groups. Aeruginosins are notable for their potent inhibition of serine proteases—particularly trypsin and thrombin—by binding to their active sites. Aeruginosin 98-B has demonstrated antitumor[3], anti-inflammatory[3], and antimicrobial activities[3]. Its absolute configuration was determined by X-ray crystallography in complex with thrombin and hirudin[8]. The compound is considered experimental; it has not been approved for clinical use or entered advanced clinical trials.

Other names
(2S,3aS,6R,7aS)-2-[4-(diaminomethylideneamino)butylcarbamoyl]-1-[(2R,3R)-2-[[(2R)-2-hydroxy-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]-2,3,3a,4,5,6,7,7a-octahydroindol-6-yl) hydrogen sulfate((2S,3aS,6R,7aS)-2-(4-(diaminomethylideneamino)butylcarbamoyl)-1-((2R,3R)-2-( ( ( 2 R ) - 2 - hydroxy - 3 - ( 4 - hydroxyphenyl ) propanamido ) - 3-methylpentanoyl ) octahydro -1H-indol–6–yl)oxidanesulfonic acid((2S , 3 a S , 6 R ,7 a S ) – ...hydrogen sulfate
02

Targets

PLG (Plasminogen)F2 (Thrombin)PRSS1 (Trypsin family)

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