Project Goal: Lead discovery
Partnership with: European inter-governmental research organization
Key Funding: Partner’s service payment
Project Objectives: Protein kinases are validated intervention points for contemporary drug discovery approaches. However active site similarities often lead to a lack of selectivity and unwanted side effects in the clinic. Our client identified a specific kinase receptor that would provide the desired selectivity. The goal was to find a cost- and resource-efficient way to expand their chemical structural variety through natural products. Discovering selective inhibitors as potential drug candidates was envisioned.
Our Contributions: Bicoll provided 1,000 Bicoll Plant Profiles™ from its proprietary small molecule natural product library BILOBAC N™ to the client’s screening program. The result was: 18 hit clusters showing specific kinase activity. Because of the high hit rate of 1.8%, the client elected to focus on 4 hit clusters for isolation and structure elucidation. Within three months Bicoll identified and structurally elucidated two pure compounds with promising structural motifs for the client’s further development programs. Subsequent comparison to Bicoll’s pure natural compound database, using the newly found structural motifs, led to the testing of additional compounds.
Time duration: 3-Months
Key benefits: cost- and resource-efficient screening
Key results: Identified a specific kinase inhibitor as potential drug candidate
Time duration: 2 years
Key benefits: Lead discovery with cost- and resource-efficient screening
Key results: Identified and delivered novel compounds as ligands
Project Goal: The search for novel ligands of a well-characterized class of orphan nuclear receptors.
Partnership with: European biopharmaceutical company
Key Funding: 50% European Union, 50% each project partner
Project Objectives: Our research partner, the biopharmaceutical company, has identified a specific nuclear receptor as a relevant target in inflammatory processes. However, any natural or synthetic ligand of this receptor still remains unknown. The main challenge was to de-orphanize the receptor by screening a very high number of compounds with the broadest structure diversity.
Our Contributions: Bicoll was approached for a joint research project based on the screening of its highly diversified library of plant metabolites BILOBAC N™. With the delivery of an extensive number of selected Plant Profiles™ from its fractionated natural product compound database BILOBAC N™, the project was able to identify several novel compounds. Bicoll’s unique Plant Profiles™ technology has demonstrated its ability to be successfully integrated into screening systems for modern drug discovery.
Project Goal: Lead optimization
Partnership with: North American biotech company and US-partner Ricerca Biosciences
Key Funding: Flexible FTE service contract (from 2 to 10 FTE’s)
Project Objectives: Our research client needed a target-focused molecular library preparation following a thorough lead optimization process. The client requested a target-focused synthetic library within a tight timeline. This project had to include the follow-up compounds for the subsequent biological tests at a scale of up to 100 g.
Our Contributions: We tackled this project with Bicoll’s US-partner Ricerca Biosciences. Together with the client and our partner Ricerca, Bicoll had set up efficient project management through its headquarters in Europe including synthetic strategies, workflow management, communication, and reporting between the US, Europe, and China locations. The setup guaranteed the client a convenient overlap in working hours for teleconferences and weekly reporting: an essential requirement for patent filing and IP protection. Bicoll’s MedChem team provided high-quality synthetic strategy support and ensured the achievement of the desired timelines with its manpower. The successful finish of the project sped up the acquisition of Bicoll’s biotech partner by a larger pharmaceutical company for several US$ Mio.
Time duration: 12 months
Key benefits: Lead optimization with cost- and resource-efficient molecular library preparation
Key results: Patent filing of the prepared target-focused molecular library.