H. pylori - Ace Therapeutics
Drug Development Targeting the Efflux Pumps of H. pylori
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Drug Development Targeting the Efflux Pumps of H. pylori

Efflux pumps are tightly related to the drug resistance of H. pylori and the balance of important metal ions in H. pylori. For example, cznABC transports zinc and nickel. Therefore, Ace Therapeutics provides small molecule drug development services for H. pylori efflux pumps.

Drug development services targeting H. pylori drug-related efflux pumps

Ace Therapeutics develops H. pylori drugs targeting the drug resistance mechanism of H. pylori. Although genetic mutations play a primary role in H. pylori antibiotic resistance. Efflux pumps are also tightly related to antibiotic resistance.

Efflux pumps are present in the bacterial membrane and are used to excrete exogenous biological components, including antibiotics, toxic substances, dyes, and neurotransmitters. Currently, Studies have found that H. pylori have primary active transporters (ABC superfamily) and three types of secondary active transporters (the major facilitator superfamily (MFS), the resistance nodulation cell division superfamily (RND), and the multidrug antimicrobial extrusion protein (MATE)). And we provide drug development services targeting those efflux pumps that have been clearly identified as effluxing drugs in H.pylori.

Plasma membrane view of multidrug efflux pumps in H. pyloriFig. 1 Plasma membrane view of multidrug efflux pumps in H. pylori (Raj et al., 2021).

More clearly, we offer drug development services for the following types of drug-related efflux pumps.

HP1181 and HP1165

HP1181 and HP1165 belong to MFS. They efflux antibiotics such as nitroimidazoles, tetracyclines, and fluoroquinolones. Thus, we offer drug development services targeting HP1181 and HP1165.

hefABC and cznABC

RND is the only efflux system that crosses the inner and outer membranes and it consists of three components. A very important characteristic of RND is that it extrudes drugs that are pumped by other smaller pumps to the periplasm to the exoplasm. Therefore, we provide drug development services with a focus on the RND of H. pylori, including hefABC consisting of HP0605-HP0607 and cznABC consisting of HP0969-HP0971.

HP1184

HP1184 belongs to MATE. We provide small molecule drug development services targeting HP1184 based on the substrate specificity of HP1184.

HP1082

HP1082 belongs to the ABC superfamily and it consumes ATP to exclude drugs such as ethidium bromide to the periplasm. And we provide drug development services for its ATP-consuming properties.

Drug development services targeting other important efflux pumps in H. pylori

Ace Therapeutics provides drug development services targeting other important efflux pumps for H. pylori including HP1561, HP0791, HP1072, and heflHG.

HP1561

We provide drug development services targeting HP1561. HP1561 is associated with the uptake of iron and the efflux of nickel and cadmium. Iron and nickel are important cofactors for many H. pylori proteins. For example, urease is a nickel-dependent enzyme that is important for the survival of H. pylori. Thus, the drug development service for HP1561 is also our focus service.

HP0791

Zinc is a cofactor for the H. pylori lipopolysaccharide-related synthase enzyme (3-Deoxy-D-mano-2-octulosonate-8-phosphate). HP0791 is associated with cadmium and zinc transport and we provide small molecule drug development services for HP0791.

HP1072

Copper is associated with the colonization of H. pylori. HP1072 can transport copper and we also offer drug development services targeting HP1072.

heflHG

heflHG consists of HP1329-HP1327 and is the third RND in H. pylori. We offer copper and zinc metal complex development services for heflHG.

Contact us

Ace Therapeutics provides small molecule drug development services for H. pylori efflux pumps. Please contact us for professional services.

References

  1. Raj, D. S.; et al. Efflux pumps potential drug targets to circumvent drug resistance – Multi drug efflux pumps of Helicobacter pylori. Materials Today: Proceedings. 2021, 45: 2976-81.
  2. Zanotti, G.; Cendron, L. Structural aspects of Helicobacter pylori antibiotic resistance. Helicobacter pylori in Human Diseases. 2019, 1149: 227-41.

※ All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.