BERLIN With a focus on rapid preclinical development of novel therapeutic leads, Jerini Bio Tools GmbH has developed tools for rapid and simple synthesis and screening of substance libraries. The company has established technologies unmatched in reliability of library synthesis and speed and has attracted an impressive customer list during the last three years.
If Ulrich Reineke, project manager of Jerini Bio Tools, had to choose a symbol for his company, he would take a standard office file: ¿That¿s how we store our small-molecule libraries. We can store millions of different peptides or other small-molecule libraries in a simple file, as they are spotted on standard filter paper. You can file them, locate them very easily, and you can even store them at room temperature.¿
In Jerini¿s bright and shiny facilities at the new East-West Center in the heart of Berlin, a robot synthesizes libraries of peptides and other small molecules by spotting the activated building blocks directly onto the paper. With this technique, 25 spots per square centimeter can be plotted. For some applications, Jerini uses polypropylene sheets and sprays the libraries. That way a density of 400 spots per square centimeter can be reached.
¿We have several standard libraries in store,¿ Reineke told BioWorld International, ¿but for rational screening we can build them according to the special needs of customers.¿ In addition, other intelligent screening methods are possible, e.g., by a positional scanning library to locate key residues within a target molecule.
The screening itself is simple, too. Compounds do not have to be transferred, as the binding assay is performed on the paper directly. So there is no need for complex robotics, and one technician can screen up to 1 million compounds per month.
¿A positional scanning library comprising 68,590 defined peptide mixtures takes us as little as three weeks to synthesize,¿ Reineke said. ¿To screen the resulting 8 x 1017 <8 x 10 to the power of 17> different peptides with a customer¿s target molecule takes us two days.¿
Cell-based assays are possible using a soft agar screening system in which a conventional Petri dish is overlaid with a membrane-bound compound library, which in turn is overlaid with soft agar containing reporter microorganisms.
Jerini the name is composed of the initials of the founders¿ names was established in 1994 with money from a research cooperation that German pharmaceutical giant Schering AG, of Berlin, entered with Jens Schneider-Mergener, one of Jerini Bio Tool¿s founders, then working at the famous Charit Clinic in Berlin. The Schering cooperation, which is still running, led to a jointly held patent on a lead structure inhibiting angiogenesis.
Meanwhile, Jerini Bio Tools has developed into a company specialized in tools for the intelligent search for novel therapeutic and diagnostic leads. Its customer list ranges from more than half a dozen German and U.S. pharmaceutical companies to U.S. agribiotech giant Monsanto and Procter & Gamble.
¿We enhance our customers¿ and collaborators¿ research and accelerate lead-finding processes,¿ Volker Thomd, CEO and director of finance, told BioWorld International. ¿Catalogue products such as peptides, assays and compound libraries account for one-third of our business activities. The other two-thirds fall to project contracts, half of them with aims set by the customer and the other half with aims defined and worked out together with Jerini Bio Tools. In this case, usually we demand royalties.¿ Thomd added that the company was planning to search for its own leads in the near future and was negotiating with investors for an expansion of its own research activities.
The company is expanding its technology platform fast. Together with AnalytiCon AG, of Potsdam-Hermannswerder, Germany, Jerini Bio Tools developed a novel approach for the generation of structurally diverse derivatives of selected natural products. Up to 50,000 molecular hybrids of natural substances like alcohols, primary amines or carboxylic acids can be produced for screening. That way, the orientation of functional groups, the polarity of the molecule, the stability of side chains and other parameters can be modified. Besides, the derivatives are patentable.
With ChemotopiX GmbH, of Berlin, Jerini Bio Tools is developing peptidomimetics and other small-molecule libraries. ¿Peptide libraries can render important biological information,¿ Reineke said, ¿but pharma companies don¿t like them, as they are difficult therapeutics. So we are concentrating on peptoids peptide-like molecules with side chains linked with the nitrogen atom and other small molecules, such as triacins. These are much more interesting from a pharmacological point of view, and we have the technology to synthesize and screen them very fast, cheap and reliable.¿
The company employs a staff of 40 and has just opened a U.S. subsidiary in Wilmington, N.C. n