Project: PharmacEutical Applications of maRine naturaL products

This project has two goals, creating a collection of 1000 compounds produced by marine microorganisms, and a selection of bioactive products as drug candidates._x000D_Natural products continue to be an important source of drug candidates, and more than 70% of approved drugs are natural products or have been derived from natural products. Marine microorganisms and the compounds they produce have been clearly underrepresented in the search for new drugs, although the exponential increase in marine products entering clinical trials for different applications is a sign that this is changing. Nevertheless, there are not collections of marine compounds offered as libraries for screening projects, and the first goal of this project is to fill that gap in the market with the development of the collection PEARLS, made of secondary metabolites of marine isolated bacteria and fungi. In order to achieve this goal Analyticon and Biomar have joined forces, bringing together expertise and a long track record in marketting and supply of Natural Product libraries for screening (Analyticon) and in marine microbiology and natural product chemistry (Biomar). The steps to generate this new collection will be to determine the structure of compounds already isolated by Biomar, to ferment and isolate new compounds from Biomar´s collection of marine microorganisms, and to generate semisynthetic libraries from the most promising scaffolds. Biomar has a collection of more than 60.000 microbial strains isolated from marine samples collected all around the world, and information about their metabolic profiles, taxonomy and ecological and geographical origin that will be used to select those with higher potential to produce diverse and unique chemical compounds. Once the compounds have been isolated and characterized, the resulting library will be offered to third parties for screening projects as a specialized natural products library. Analyticon´s expertise in Natural product analogue synthesis, and Biomar´s capabilities for GMP-production of compounds by fermentation in volumes up to 3000L are complementary to the library and will help its commercialization._x000D_The second objective of the project is to select bioactive compounds from the collection based in screening results in anticancer and antiinfective activity assays. These assays will identify compounds active against specific molecular and cellular targets and in combination with the information regarding the structure of the compounds allow for the selection of those with a promising activity and strong intellectual property position. The drug-like properties of the active compounds will be improved through analogue synthesis, and the selected compounds will be evaluated in In vitro and In vivo models of the disease. Some of the properties that will be improved are solubility, stability, metabolism, pharmacokinetics and efficacy. Biomar and Analyticon will jointly seek licencing Ps for the resulting compounds as the CO commercial objective of this second goal. Both parties will also consider co-development of some of the drug candidates identified during this project._x000D_The consortium is made by the two companies, that will coordinate their efforts through a steering committee and workpackages coordinators. Biomar will be in charge of coordinating the workpackages related to strain fermentation, compound isolation and structure elucidation, and Analyticon will coordinate the workpackages related to activity screening and analogue synthesis. The steering committee will also be responsible of designing and executing the commercial strategy for the compound library and the drug candidates.

Acronym	PEARLS (Reference Number: 7024)
Duration	01/04/2012 - 31/12/2014
Project Topic	1000 compounds produced by marine microorganisms will be generated and screened against relevant targets for cancer and infectious disease therapy. Medicinal Chemistry programms will be run for bioactive compounds. The collection and drug candidates will be commercialized at the end of the project.
Project Results (after finalisation)	Biomar's library of marine derived natural products was significantly enlarged. Analyticon has established a screening plattform with proprietary high content anti cancer assays which was successfully used for the screening of natural products and synthetic analogues in the field of anticancer and antibiotic research. Hit evaluation together with optimisation by medicinal chemistry of several active compounds lead to advanced hit structures with interesting anticancer activities.
Network	Eurostars
Call	Eurostars Cut-Off 7

Project partner

Number	Name	Role	Country
2	ANALYTICON DISCOVERY GmbH	Partner	Germany
2	INSTITUTO BIOMAR S.A.	Coordinator	Spain