Scientific Programme

The scientific programme will include plenary lectures, oral communications and poster sessions.
You can download the final programme as a pdf
The program and abstract booklet is also available online as a pdf


Sunday May 13th, NH Carlton Hotel
17.00 - 19.00
 Reception at NH Carlton (near Mint Tower and Flower Market) for all participants & speakers

Monday May 14 th, Royal Tropical Institute
8.30 - 17.00 Registration


Opening
9.00 - 9.05 Henk Timmerman, symposium chair


Forum on the MedChem 2020 arena (chairs Henk Timmerman & Dave Swinney)
9.05 – 9.15 Introduction by Dave Swinney (iRND3, USA)
9.15 – 9.45 Gerhard Mόller (Mercachem, NL) Medicinal Chemistry Services within 'small pharma': from molecular understanding to complex chemistry
9.45 – 10.15 Anthony Wood (Pfizer, US) Challenges and Opportunities for Medicinal Chemistry
10.15 – 10.30 Gyφrgy Keseru (Gideon Richter, Hungary)Finding the sweet spot: the role of nature and nurture in Medicinal Chemistry
10.30 – 11.00 Discussion with Gerhard Mόller, Anthony Wood, Mike Hann, Gyφrgy Keseru and the audience - moderated by Henk Timmerman & Dave Swinney


Session 1: New synthetic technologies for medicinal chemistry (chair: F. Rutjes, NL)
11.30 – 11.35 Introduction by Floris Rutjes (Radboud University Nijmegen, NL)
11.35 – 12.15 Keynote lecture: Thomas Franch (Nuevolution, Danmark) Billion member DNA-tagged screening libraries. From theory to practical application in medicinal chemistry
12.15 – 12.45 Floris Rutjes (Radboud University Nijmegen, NL) Recent advances in flow chemistry
12.45 – 13.15 Daniel Obrecht (Polyphor, Switserland) Medium-sized macro cyclic PEM molecules: synthetic challenges and evaluation for targeting challenging and therapeutically relevant GPCRs


Lunch break & Poster viewing

Session 2: Fragment-based drug discovery (chairs D. Rees, UK, I. De Esch, NL)
14.15 – 14.55 Keynote lecture: David Rees (Astex, UK) The Rise of Fragment Based Drug Discovery
14.55 – 15.25 Mike Hann (GSK, UK) Molecular Obesity, potency and other addictions in medicinal chemistry
15.25 – 15.55 Herbert Nar (Boehringer Ingelheim, Germany) Linking HTS-based and fragment-based approaches to a productive lead identification process using structural biology and biophysics
15.55 – 16.10 Carol Austin (Selcia, UK) Fragment screening using capillary electrophoresis
16.10 – 16.25 Gregg Siegal (Leiden University, NL) Effective structure determination of protein-fragment complexes using NMR


Social program – Concert (ticket required) in Royal Concert Hall

Tuesday May 15th, Royal Tropical Institute
9.00 - 17.00 Registration
9.15 - 9.55 Special lecture: Anette Beck-Sickinger, (Univ. Leipzig, Germany) Peptide Drugs – State of the Art and Innovative Applications


Session 3: Structural biology of membrane proteins (chair: Fiona Marshall, UK)
9.55 – 10.35 Keynote lecture: Fiona Marshall (Heptares, UK)Structure and fragment based drug discovery applied to G-protein coupled receptors
10.35 – 11.05 So Iwata(UCL, UK) Structural studies on G-protein coupled receptors
11.30 – 12.00 Gebhard Schertler (Paul Scherrer Institute, Switzerland) Structures of constitutively active G-Protein Coupled Receptors
12.00 – 12.30 Chris de Graaf (VU University Amsterdam, NL) Fragments, Fits, Fingerprints: Structure-based virtual screening for fragment-like GPCR ligands
12.30 – 13.00 Marijn Sanders (Radboud University Nijmegen, NL) Snooker: Multiple sequence alignment derived pharmacophores and its application in drug design
14.00– 14.30 Werner Sieghardt (University of Vienna, Austria) GABAA receptor subtypes – exciting targets for the development of clinically important drugs
14.30 – 15.00 Chris Ulens (University of Leuven, Belgium) Structural principles of agonist and modulator recognition in a bacterial GABA-gated ion channel
15.00 – 15.15 Rogier Smits (Griffin Discoveries, NL) Long receptor residence time and H4R antagonism
15.15 – 15.30 Fabio Del Bello (University of Camerino, Italy) Might Allyphenyline and cyclomethyline become profitable multifunctional tools in the opioid addiction management?
15.30 – 15.45 Maikel Wijtmans (VU University Amsterdam, NL) Bisaryl-type Ligands: a Thin Line Between Antagonism and Agonism at Chemokine Receptor CXCR3


Drinks & poster discussions with presenters

(please be present at your poster!!)


Wednesday May 16th, Royal Tropical Institute
9.00 - 17.00 Registration
9.15 – 9.55 Special lecture: Martine Smit, (VU University Amsterdam) Therapeutic targeting of chemokine receptors with Nanobodies (VHH immunoglobulin-based single variable domains)


Session 4: Target tumor therapy via antibody-drug conjugates (chair: R. Jautelat, Ger)

9.55 – 10.00 Introduction by chair Rolf Jautelat (Bayer, Germany)
10.00 – 10.40 Keynote lecture: Hans-Georg Lerchen (Bayer, Germany) Antibody Drug Conjugates: Challenges in the interface between proteins and small molecules
11.15 – 11.45 Vincent de Groot (Synthon, NL) Preclinical Development Progress of ADCs based on Novel Potent Payload Linker-Drug Technology
11.45 – 12.15 David Satijn (Genmab, Denmark) Development of antibody drug conjugates against Tissue Factor for the treatment of solid tumors.


Late breaking topics

13.15 – 13.45 EelcoRuijter (AIMMS, VU University Amsterdam, NL) Multicomponent reactions – opportunities for medicinal chemistry
13.45 – 14.15 Thiery Langer (Prestwick, Chemical SAS France) 3D Chemical Feature-based Pharmacophores: Efficient Tools In Lead Optimization and Profiling
14.15 – 14.30 Kristina Orrling (TI Pharma consortium T4-302 Swe) From fragments to trypanocidals – PDE inhibitors as potential new treatment of African Sleeping Sickness


Session 5: Epigenetics: from chemical biology to new therapeutics (chair: M. Hann, UK)
15.00 – 15.05 Introduction by chair Mike Hann (GSK, UK)
15.05 – 15.45 Keynote lecture: John Trzupek (Pfizer, USA) Chemical Probes for Epigenetics
15.45 – 16.15 Jian Jin (University of North Carolina, USA) Discovery of Chemical Probes for Methyl Writers of the Histone Code
16.15 – 16.45 Chun-wa Chung (GSK, USA) Hedging your BETs: from phenotypic screening to fragment based drug discovery


Social program – Symposium diner at Felix Meritis, Keizersgracht 324 (ticket required)


Thursday, May 17th Royal Tropical Institute
9.00 - 17.00 Registration


Session 6: The drug resistance issue (chair: J. Moll, Germany)
9.15 – 9.20 Introduction by chair Jόrgen Moll (Boehringer Ingelheim, Germany)
9.20 – 10.00 Keynote lecture: Doriano Fabbro (Novartis Pharma AG, Switzerland) Drug resistance mechanisms for kinase inhibitors
10.00 – 10.30 Ivana Scovassi (IGM-CNR, Italy) Search for anticancer drugs: A look to apoptosis but also to autophagy!
10.30 – 11.00 Anne Gougeon (University of Rennes, France) Antibiotics and bacteria in biofilms: a daily fight


Session 7: Kinetic and thermodynamic aspects of ligand binding (chair G. Keseru, Hungary)
11.30 – 11.35 Introduction by chair György Keseru (Gedeon Richter, Hungary)
11.35 – 12.15 Keynote lecture: Dave Swinney (iRDN3, USA) The value of understanding and applying binding kinetics to drug discovery
12.15 – 12.45 Glyn Williams (Astex, UK) Mapping the Thermodynamic Landscape of Fragment-Based Drug Discovery
13.45 – 14.15 Ron Dror (DE Shaw Research, USA) How drugs bind and control their targets: characterizing GPCR signalling through long-timescale simulation
14.15 – 14.45 Xavier Barril (University of Barcelona, Spain) Water-shielded hydrogen bonds as structural determinants of binding kinetics
14.45 – 15.15 Peter Brandt (Beactica, Sweden) Importance of binding kinetics and Quantitative Structure-kinetics modelling
15.15 – 15.45 Iwan de Esch (VU University Amsterdam, NL) Fragment screening and growing in acetylcholine binding protein, structural insights and thermodynamic considerations
15.45 – 16.15 Anna Tigerstrφm (AstraZeneca R&D, Sweden) Competitive single injection ITC, a tool for thermodynamic profiling of fragments


Closing of the symposium