R&D Initiatives

We have several ongoing R&D projects at Red Glead Discovery (RGD).

Project Nile aims at developing novel compounds for an epigenetic target in the treatment of cancer. This project is a collaboration between RGD, SARomics Biostructures (SBX) and a research group led by Professor Jonas Nilsson at Sahlgrenska Hospital (Gothenburg, Sweden). Candidate drug development activities are supported by a research grant from Vinnova (the Swedish innovation agency).

Project Ganges, a collaboration between SARomcs Biostructures and RGD, is built on the foundation of a successful fragment screen, where hits for this bromodomain-class target were identified using our exclusive WAC technology. Further validation led to X-ray co-crystal structures revealing a possibility for developing a PPI inhibitor-type molecule. The project is currently in the hit expansion phase and entering hit-to-lead.

A previous project has been spun out into a separate company, Apoglyx, where RGD is a co-owner. Apoglyx research is based on aquaporins, a group of structures in cell membranes discovered in 1991 by Peter Agre and awarded with the Nobel Prize in Chemistry 2003. Aquaporins have been recognized as potential drug targets and may have roles for development of autoimmune diseases, cancer, diabetes, malaria, inflammation and sepsis. The lead compound – RG100204, has shown promising effects against sepsis when evaluated in vivo.

Pipeline

We currently have several ongoing internal drug discovery projects in our pipeline.

Science

Red Glead Discovery (RGD) invests heavily in remaining at the forefront of research and innovation. Ninety-five percent of our staff currently work in lab- or other science-based positions. In addition to actively producing peer-reviewed research papers, we have contributed to several patents for both clients and internal RGD projects. A number of our scientists are appointed lecturers at Lund University and Lund Technical University and serve in advisory roles shaping the teaching curriculum in chemistry / biomedicine and chemical engineering programs respectively. RGD actively engages in collaboration with academia to address societal challenges, welcoming diploma workers to participate in projects from all of our scientific disciplines.

An area of focus for RGD is on green chemistry. Organic solvents are used to facilitate chemical reactions, but they do not add any value to the final product and in most cases, they originate from petroleum and end up as waste. We have initiated a collaboration with researchers at the Centre for Analysis and Synthesis at Lund University. The project aims to develop methods for organic synthesis in water.  Our approach is to recycle water and the catalyst used, so the created waste is close to zero. The long-term goal is to be able to synthesize pharmaceuticals with low environmental impact.

Diploma Work

Tomas Laszlo Szakacs 2019, Lund University

Peptide fragment screening towards a new inhibitor of neutrophil elastase

Sofi Gummeson 2020, Lund University

Synthesis of a 13C-labeled tool compound for diagnostic applications

Artur Sahakjan 2020, Lund University

Fragment screening using WAC towards new SMARCA4 inhibitors

Kajsa Andréasson Dahlgren 2021, Lund University

Validation of a 3D culture model for toxicity studies in malignant and non-cancerous cells

Publications

Molecular Dynamics Studies of Therapeutic Liquid Mixtures and Their Binding to Mycobacteria

Monteiro, H.; Santos, F.; Paiva A.; Duarte, A. R. C.; Ferreira, R. J.
Front. Pharmacol. 2021,12:626735

Evolution of Nitrogen-Based Alkylating Anticancer Agents

Lehmann, F.; Wennerberg, J.
Processes 2021, 9, 377

An Aldehyde Responsive, Cleavable Linker for Glucose Responsive Insulins

Mannerstedt, K.; Mishra, N. M.; Engholm, E.; Lundh, M.; Madsen, C. S.; Pedersen, P. J.; Le-Huu, P.; Pedersen, S. L.; Buch-Månson, N.; Borgström, B.; Brimert, T.; Fink, L. N.; Fosgerau, K.; Vrang, N.; Jensen, K. J.
Chemistry, 2021, 1-12

Melflufen: A Journey from Discovery to Multi-Kilogram Production

Lehmann, F.; Wennerberg, J.
Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 3, Chapter 5 pp 157-177, 2020

NMR Study of the Secondary Structure and Biopharmaceutical Formulation of an Active Branched Antimicrobial Peptide

Castiglia, F.; Zevolini, F.; Riolo, G.; Brunetti J, De Lazzari, A:, Moretto, A.; Manetto, G.; Fragai, M.; Algotsson, J.; Evenäs, J.; Bracci, L.; Pini, A.; Falciani, C.
Molecules 2019, 24(23), 4290-4302

Monosaccharide Derivatives with Low Nanomolecular Lectin Affinity and High Selectivity Based on Combined Fluorine-Amide, Phenyl-Arginine, Sulfur-π, and Halogen Bond Interactions

Zetterberg, F.; Peterson, K.; Johnsson, R.; Brimert, T.; Håkansson, M.; Logan. D.; Leffler, H.; Nilsson, U.
ChemMedChem. 2018;13(2):133–137

Structural Insights into the Calcium-Mediated Allosteric Transition in the C-Terminal Domain of Calmodulin from Nuclear Magnetic Resonance Measurement

Kukic, P.; Lundström, P.; Camilloni, C.; Evenäs, J.; Akke, M.; Vendruscolo, M.
Biochemistry 2016 Jan 12;55(1):19-28

Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS)

Edfeldt, F.; Evenäs, J.; Lepistö, M.; Ward, A.; Petersen, J.; Wissler, L.; Rohman, M.; Sivars, U.; Svensson, K:, Perry, M.; Feierberg, I:, Zhou, X.; Hansson, T.; Narjes, F.
Bioorg Med Chem Lett. 2015 15;25(12):2496-2500

HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase

Evenäs, J.; Edfeldt, F.; Lepistö, M.; Svitacheva, N.; Synnergren, A.; Lundquist, B.; Gränse, M.; Rönnholm, A.; Varga, M.; Wright, J.; Wei, M.; Yue, S.; Wang, J.; Li, C,; Li, X.; Chen, G:, Liao, Y.; Lv, G.; Tjörnebo, A.; Narjes, F.
Bioorg & Med Chem Lett. 2014, 24(5), 1315–1321