Delving into the Latest Updates on AIC-499 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

β-lactamase

Mechanism

β-lactamase inhibitors(Beta Lactamase inhibitors)

Therapeutic Areas

Infectious DiseasesUrogenital Diseases

Active Indication

Intraabdominal InfectionsUrinary Tract Infections

Inactive Indication

Gram-Negative Bacterial Infections

Originator Organization

AiCuris GmbH & Co. KG

Active Organization

AiCuris GmbH & Co. KG

Inactive Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Novel antimicrobial strategies are urgently required because of the rising threat of multi drug resistant bacterial strains and the infections caused by them. Among the available target structures, the so-called penicillin binding proteins are of particular interest, owing to their good accessibility in the periplasmic space, and the lack of homologous proteins in humans, reducing the risk of side effects of potential drugs. In this report, we focus on the interaction of the innovative β-lactam antibiotic AIC499 with penicillin binding protein 3 (PBP3) from Escherichia coli and Pseudomonas aeruginosa. This recently developed monobactam displays broad antimicrobial activity, against Gram-negative strains, and improved resistance to most classes of β-lactamases. By analyzing crystal structures of the respective complexes, we were able to explore the binding mode of AIC499 to its target proteins. In addition, the apo structures determined for PBP3, from P. aeruginosa and the catalytic transpeptidase domain of the E. coli orthologue, provide new insights into the dynamics of these proteins and the impact of drug binding.

100 Deals associated with AIC-499

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Intraabdominal Infections	Phase 1	-	AiCuris GmbH & Co. KG	-
Urinary Tract Infections	Phase 1	-	AiCuris GmbH & Co. KG	-
Gram-Negative Bacterial Infections	Preclinical	AT	AiCuris GmbH & Co. KG	-