Plenary Keynotes 2019

Dan Erlanson

Dr. Daniel A. Erlanson is the VP of chemistry for Frontier Medicines, which is using covalent fragments, machine learning and chemoproteomics to drug previously undruggable targets. Prior to Frontier he co-founded Carmot Therapeutics, where he contributed to two clinical-stage molecules. Before Carmot, Dr. Erlanson spent a decade developing fragment-based discovery technologies and leading medicinal chemistry efforts in oncology and in metabolic and inflammatory diseases at Sunesis Pharmaceuticals, which he joined at the company’s inception. Dr. Erlanson was an NIH postdoctoral fellow with James A. Wells at Genentech, earned his PhD in chemistry from Harvard University in the laboratory of Gregory L. Verdine, and his BA in chemistry from Carleton College. As well as co-editing two books on fragment-based drug discovery, Dr. Erlanson is an inventor on more than a dozen issued patents and an author of more than forty scientific publications. He is also editor of a blog devoted to fragment-based drug discovery, Practical Fragments.

Alba Macias

Dr. Alba T. Macias is a Principal Scientist and project leader working in fragment-based drug discovery at Vernalis Ltd, a Ligand company. Vernalis combines fragment based approaches, structural biology, biophysics, assay technology, molecular modelling and medicinal chemistry in its drug discovery platform. Dr. Macias is a computational chemist with a particular interest in protein modelling, selectivity and design of covalent inhibitors. These approaches are used for detailed structure-based optimisation of fragments and lead compounds, as well as the design of compound libraries for off-rate-screening using surface plasmon resonance. Off-rate screening allows for rapid elaboration of fragments into leads. Since joining Vernalis in 2006, her contributions to internal projects and collaborations with external partners have resulted in numerous patents, publications, and clinical candidates. After completing a double-major in Chemistry and Mathematics, Dr. Macias pursued a PhD in chemistry under the supervision of Professor Jeffrey D. Evanseck at the University of Miami (USA). She then became an NIH postdoctoral fellow at the School of Pharmacy, University of Maryland at Baltimore, where she trained with Professor Alexander D. MacKerell.

Invited Speakers

Iwan de Esch

Prof. Iwan de Esch is professor at the Medicinal Chemistry division of VU University Amsterdam. His rsearch aims to understand and predict interactions between biologically active ligands and their molecular targets. The group makes extensive use of Computer-Aided Drug Design (CADD) and organic chemistry to design and synthesize new ligands. Hit finding and optimization efforts are guided by Fragment-Based Drug Design (FBDD) approaches. Various protein classes are being interrogated, including, GPCRs, PDEs, AChBP and LGICs, protein-protein interactions, kinases and others. Next to hit finding, the group has experience in hit and lead optimization, leading amongst others to clinical candidates for the histamine H4 receptor. In 2011, he received the Galenus Research Price for his work on Fragment-Based Drug Discovery and valorization activities. He is co-founder of three academic spin-out companies, i.e., De Novo Pharmaceuticals Ltd (a spin-out from the University of Cambridge, UK), IOTA Pharmaceuticals Ltd and Griffin Discoveries BV (spin-outs of VU University Amsterdam). Iwan de Esch is coordinator of FRAGNET, a European training network that focusses on developing FBDD.

Lorna Wilkinson-White

Dr Lorna Wilkinson-White is a Staff Scientist who runs the Fragment Based Drug Discovery (FBDD) platform at Sydney University, which is part of the Sydney Analytical Core Facility. Primarily using NMR spectroscopy and Surface Plasmon Resonance, Dr Wilkinson-White has worked with researchers across NSW on a variety of FBDD projects which aim to develop new anti-cancer, antibacterial and antifungal agents. Dr Wilkinson-White has a BSc (Hons I) and PhD from the University of Sydney. Following her PhD, she spent eight years working with Prof. Jacqui Matthews as a postdoctoral researcher in the field of protein structural biology. During this time, she used a range of techniques including Isothermal Titration Calorimetry, NMR spectroscopy, Small Angle X-ray Scattering and X-ray crystallography to characterise a variety of protein:protein and protein:nucleic acid complexes involved in leukemias.

Reto Horst

Dr. Reto Horst is a Principal Scientist in the Structural and Molecular Sciences group at Pfizer in Groton, CT, USA. He is developing and applying cutting edge NMR methods to identify and validate hits from various screening funnels and to characterize protein–ligand interactions. Dr. Horst has guided fragment-based drug discovery efforts in various disease areas and made key contributions to several discovery projects. Dr. Horst obtained a diploma (MSc) in Physics and a PhD in Biophysics under the supervision of Nobel Laureate Dr. Kurt Wuthrich at the ETH in Zurich, Switzerland. Before joining Pfizer in 2012, he was a Staff Scientist at Scripps Research in La Jolla, CA, where his research was focused on studying GPCR signaling pathways and chaperonin-assisted protein folding by solution state NMR spectroscopy, resulting in 25 peer-reviewed publications that appeared in Tier 1 journals including Cell, Science and PNAS.