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Person › Details

Kai Lamottke (Bicoll GmbH)

Lamottke, Kai (Bicoll 201308 Managing Director)

 

Organisation Organisation Bicoll GmbH
  Group Bicoll (Group)
Products Product Profiles™ technology (fractionated plant extracts library for drug discovery)
  Product 2 drug discovery technology
     

Bicoll GmbH. (8/29/13). "Press Release: Bicoll Announces a Fast Small Molecule Ligand Validation Method for Orphan Targets".

BICOLL Group announces today the successful application of its technology for the identification of ligands of a specific orphan target. As described in a new publication in the Journal of Biomolecular Screening (1), a class of potent and bioavailable RAR-related orphan receptor alpha (RORa) agonists has been identified in a plant extract library from BICOLL.

The findings were generated in collaboration with Genfit, a biopharmaceutical company at the forefront of drug discovery and development, focusing on the early diagnosis and preventive treatment of cardiometabolic and associated disorders. The successful joint program demonstrates the general effectiveness of BICOLL's small molecule approach on orphan targets as a case study. Indeed, the use of BICOLL's technology of fractionated plant extracts (Profiles™) has led to a timely identification of potent ligands and enabled target validation studies in vivo within a period of 9-months from the start of the initial screening.

BICOLL's plant Profiles™ is a fast-track validation tool for any small molecule screening program. It gives partners the opportunity to obtain essential target validation data in animal model(s) with an unprecedented rapidity. Classically, the identification of such ligands may take between 18 and 24 months or even longer. The disclosed plant ProfilesTM-approach brings together two important aspects that help to overcome usual drug discovery program difficulties, i.e. an enormous chemical diversity (up to 100.000 relevant, chemical entities in a typical screening campaign) and a relative ease of operations with respect to screening procedures, since the full set of this diversity can be leveraged without explicit purification.

"Any medicinal chemistry program will profit from employing plant Profiles™ in drug discovery - either as a jump starting point, benchmarking, or inspiration for chemists" stated Dr. Kai Lamottke, managing director of BICOLL and co-author of the publication. "Valid data from animal models can be quickly produced and "go" or "no-go" decisions can be done without any big investment or set-up of a compound library of highly pure and initially defined small molecules. Our partner Genfit is highly experienced in evaluating the suitability of difficult orphan targets for drug discovery programs. Genfit's drug discovery team led by Dr. Robert Walczak leveraged the whole set of information generated by our technology and translated the findings rapidly into animal studies. In principle, Profiles™ technology can be used in any classical drug discovery program, even on a difficult target, as a ready to go solution".


(1) Helleboid et al. (2013): The identification of naturally occurring neoruscogenin as a bioavailable, potent and high affinity agonist of the nuclear receptor RORa (NR1F1); J Biomol Screen 1087057113497095, first published on July 29, 2013

doi:10.1177/1087057113497095

   
Record changed: 2017-04-09

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