Delving into the Latest Updates on RM-032 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

KRAS G12C x NRAS G12C

Mechanism

KRAS G12C inhibitors(GTPase KRas G12C inhibitors), NRAS G12C inhibitors(GTPase NRas G12C inhibitors)

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

Revolution Medicines, Inc.

Active Organization

Revolution Medicines, Inc.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

AbstractPyoverdines, a group of peptide siderophores produced by Pseudomonas species, function not only in iron acquisition, but also in their virulence in hosts. Thus, chemical inhibition of pyoverdine production may be an effective strategy to control Pseudomonas virulence. In the plant pathogen Pseudomonas cichorii SPC9018 (SPC9018), pyoverdine production is required for virulence on eggplant. We screened microbial culture extracts in a pyoverdine-production inhibition assay of SPC9018 and found Streptomyces sp. RM-32 as a candidate-producer. We isolated two active compounds from RM-32 cultures, and elucidated their structures to be actinomycins X2 and D. Actinomycins X2 and D inhibited pyoverdine production by SPC9018 with IC50 values of 17.6 and 29.6 μM, respectively. Furthermore, pyoverdine production in other Pseudomonas bacteria, such as the mushroom pathogen P. tolaasii, was inhibited by the actinomycins. Therefore, these actinomycins may be useful as chemical tools to examine pyoverdine functions and as seed compounds for anti-Pseudomonas virulence agents.

100 Deals associated with RM-032

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