FAQS:

• How quickly can VENENUM Biodesign run a UHTS for ECLIPS compound collection?

  In general, from assay validation to confirmed hits it takes six months. We generate a full report of the data for the customer.

• Who does the assay development / miniaturization for the UHTS?

  VENENUM Biodesign can do this for you from start to finish or we can take your assay and convert it to 1536-well format.

• Can VENENUM Biodesign run 1536 UHTS in whole cells?

  Yes.

• Can other plate formats than 1536-well be used?

  For UHTS we strongly prefer 1536 as the reagent as the time and overall costs for running 384-well screens tend to be prohibitive.

• What type of quality control is used for the ECLiPS libraries?

  ECLiPS libraries are constructed after comprehensive optimization of reaction conditions to ensure the success of each R-group addition. The quality of the completed library is analyzed by Library QA, an LC/MS method conducted at the single bead level. Further detailed information on the Library QA protocol for ECLiPS analysis can be found in Journal of Combinatorial Chemistry (2000), 2, 716-731.

• Does VENENUM Biodesign have a license to use radiolabeled materials?

  Yes. Radioactive assays are used for HTS when needed, and radiolabeled material can be used for secondary, lower-throughput assays in 96- or 384-well microplate formats.

• Does VENENUM Biodesign screen the ECLiPS libraries on beads?

  No, the linker covalently linking the ECLiPS compound to the bead is cleaved and the compound is tested free from the bead.

• Can you improve solubility of my target protein?

  Yes. To achieve an enhanced solubility we optimize a combination of parameters including vector, expression conditions and host cells. Additionally, for difficult targets we employ an extensive bioinformatic analysis to derive functional domains and/or to engineer potentially beneficial alterations. Fusion tags can also be added to improve folding and purification efficiency.

• What are your quality standards for recombinant proteins?

  Because at VENENUM Biodesign we conduct crystallographic studies of our own target proteins, we keep the purity and homogeneity requirements at the highest crystallization grade.

• How useful is X-ray crystallography for lead optimization?

  X-ray crystallography allows to take an atomic level snap-shot of a drug candidate bound to your target protein. This provides an important feedback for the next round of computational and chemical optimization by showing the exact binding mode and specific network of interatomic contacts between the drug and its target.

• I am interested in your computational optimization service, however, a 3D structure of my target protein is not available. What are my options?

  Availability of experimentally determined 3D structure is highly desirable for computer-aided drug optimization. Upon agreement we can proceed with crystallographic studies of your target protein in order to obtain its 3D structure. Alternatively, in many cases a homology model can be built based on the existing structural information of closely related family members.