Membrane Protein DNA-Encoded Library Screening Services

Creative Biolabs is a leading provider of membrane protein drug discovery. DNA-encoded library screening has several advantages over traditional high-throughput screening, including a substantially larger library size and more cost-effective affinity screenings.

DNA-encoded libraries (DELs) have gotten a lot of attention as a potential drug discovery tool for membrane proteins. Screening encoded libraries may have advantages over traditional hit discovery methods in pharmaceutical research, and it has the potential to complement such procedures. DELs are collections of combinatorial compounds in which each structure is tagged with a DNA identification barcode. DELs aims to combine the benefits of both chemical library screening and display technologies which would allow the interrogation of small-molecule libraries of unprecedented size rapidly and economically. Screening DELs typically involves affinity selection of libraries against an immobilized protein target, and therefore screening is rapid and inexpensive. Simultaneously, the synthetic methods used to prepare DELs to enable the encoding of diverse sets of compounds with potentially membrane protein drug characteristics.

Virtual drug screening. Fig.1. Conceptual representation of DELs. (Song, 2020)

DNA-encoded Library Design and Synthesis

Library design directly influences the chemical properties of encoded compounds. Important DELs design parameters are the number of diversity points and the assembly geometry. Moreover, the chemical reactions used to connect the diversity points and the building blocks themselves strongly influence the properties of the molecules. Possibly the most fundamental DELs design criterion is the number of diversity points (nBB). This number has an immediate effect on the chemical properties of the encoded compounds.

Representation of two virtual drug screening approaches. Fig.2. Combinatorial nature of DELs (nBB: number of diversity points in library). (Franzini, 2016)

Sample Requirements of Membrane Protein DNA-encoded Library Screening

>90% purity is required, as is a precise assessment of the multimeric state.
His, biotin, Strep tags, or dual/multiple tags are preferred.
The target membrane protein's activities and functionality should not be hampered by the tag.
The amount of protein required is determined by the selection group design. For example, 1 mg is sufficient for a normal 50 KD protein with 6 groups in the selection strategy.

Advantages of DNA-encoded Library Screening

Rapid and low-cost
High-throughput screening on a never-before-seen scale
Screening multiple related proteins
Structure information important to target specificity that has been deduced

Creative Biolabs has long-term devoted to developing and optimizing the effectiveness and the efficiency of membrane protein drug discovery. We are pleased to use our extensive experience and advanced platform to offer the best service and the most qualified products to satisfy each demand from our customers. Please contact us for more details about our membrane protein DNA-encoded library screening service. Our experts will help design an optimal solution for your project and trouble-shoot for you throughout the whole process.

References

Song, M., Hwang, G.T. DNA-encoded library screening as core platform technology in drug discovery: its synthetic method development and applications in DEL synthesis. Journal of medicinal chemistry. 2020; 63(13), 6578-6599.
Franzini, R.M., Randolph, C. Chemical space of DNA-encoded libraries: Miniperspective. Journal of medicinal chemistry. 2016; 59(14), 6629-6644.

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