As a leading CRO company, Creative Biolabs is devoted to helping global clients to explore and identify the potential and well-recognized targets for antifungal drug development. Here we describe the attractive antifungal targets involved in the phospholipid biosynthesis.

Introduction of Phospholipid

Fungi cell membrane is rich in a variety of lipids belonging to the class glycerophospholipids, sphingolipids, and sterols. Glycerophospholipids consist of glyc-erol-3-phosphate that contains two fatty acyl chains along with various substituents like choline, serine, and ethano-lamine. Various phospholipids have been detected including phosphatidic acid, phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylserine (PS), phosphatidylglycerol (PG), phosphatidylinositol (PI), cardiolipin and sphingolipids such as inositol phosphateceramide, mannosyl-inositolphosphate-ceramide, and mannosyl-diinositolphosphate-ceramide in the cell membrane of Saccharomyces cerevisiae.

Phospholipid Biosynthesis

Phospholipid biosynthesis pathways in fungi include endogenous and exogenous pathways. In almost all endogenous pathways, all membrane phospholipids are synthesized via a common liponucleotide precursor called CDP-diacylglycerol (GDP-DAG). PS is synthesized via PS synthase by catalyzing the reaction between CDP-DAG and serine, whereas PE and serine are converted to PS by the enzyme PS synthase II in other organisms. Therefore targeting fungal PS synthase would be a promising approach for antifungal drug development. Besides, some key enzymes specific to fungi in phospholipid biosynthesis also become the targets of antifungal drug development, such as PS decarboxylase and PE N-methyl-transferase.

Enzymes and respective inhibitors for phospholipid biosynthesis. Fig.1 Enzymes and respective inhibitors for phospholipid biosynthesis. (Sant, 2016)

What Can We Provide?

Creative Biolabs has an outstanding professional team and diverse advanced technology platforms to provide customers worldwide with a full range of antifungal drug discovery services including target identification and validation, Hit identification, Hit to lead, Lead optimization, and IND enabling. Our services not only enable you to obtain a final result but also provide a whole-process technical support service so that you can keep abreast of the progress of the project and obtain our technical guidance in a timely manner.

Advantages of our Services

  • Advanced technology platforms-diverse technology platforms including whole genome sequencing (WGS), gene manipulation, phage display and so on.
  • An experienced team of experts-our specialists with years of experience in drug target discovery provide a full range of technical support services from taking over the project to the end of the project.
  • Extensive repertoires of pharmacological targets
  • Rapid and accurate screening protocols
  • Low cost and high quality

If you are interested in our antifungal drug discovery package services, please do not hesitate to contact us for more details or a detailed quote.

Reference

  1. Sant, D.G.; et al. Fungal cell membrane-promising drug target for antifungal therapy. Journal of Applied Microbiology. 2016, 121(6):1498-1510.

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