Delving into the Latest Updates on PaTx-II with Synapse

Overview

Basic Info

Drug Type

Protein drugs

Synonyms-

Target-

Mechanism-

Therapeutic Areas

Infectious DiseasesOther Diseases

Active Indication

Gram-Positive Bacterial InfectionsWounds and Injuries

Inactive Indication-

Originator Organization

National University of Singapore

Active Organization

National University of Singapore

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Alternariol monomethyl ether (AME), a dibenzopyrone derivative, was isolated from Alternaria brassicae along with altertoxin II (ATX-II). The compounds were tested for the inhibitory activity of monoamine oxidase (MAO), which catalyzes neurotransmitting monoamines. AME was found to be a highly potent and selective inhibitor of human MAO-A with an IC₅₀ value of 1.71 µM; however, it was found to be ineffective for MAO-B inhibition. ATX-II was not effective for the inhibition of either MAO-A or MAO-B. The inhibition of MAO-A using AME was apparently instantaneous. MAO-A activity was almost completely recovered after the dilution of the inhibited enzyme with an excess amount of AME, suggesting AME is a reversible inhibitor. AME showed mixed inhibition for MAO-A in Lineweaver-Burk plots with a K_i value of 0.34 µM. The findings of this study suggest that microbial metabolites and dibenzopyrone could be potent MAO inhibitors. In addition, AME could be a useful lead compound for developing reversible MAO-A inhibitors to treat depression, Parkinson's disease, and Alzheimer's disease.

100 Deals associated with PaTx-II

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gram-Positive Bacterial Infections	Preclinical	-	National University of Singapore	22 Feb 2023
Wounds and Injuries	Preclinical	-	National University of Singapore	22 Feb 2023