GP2A 2019 Workshop: The fundamentals of quantitative molecular pharmacology

Prof. Steven J Charlton
Excellerate Biosciences and University of Nottingham

Comparing the pharmacological characteristics of compounds across different systems (e.g. different assays and/or cell types) can be a complex task. More difficult still is the extrapolation of these in vitro data to in vivo systems through PK/PD modeling. In order to make these tasks as accurate as possible, it is critical to define quantitative, system independent measures of compound action. This workshop will introduce the concept of quantitative molecular pharmacology and detail the experimental and analytical methods used to determine key system-independent pharmacological descriptors of both drug binding and functional efficacy. It will culminate in a team-based exercise where you will put the knowledge and skills gained from the morning’s lectures into practice. You will play the role of the pharmacologist in a (fictitious) pharmaceutical company’s due diligence team, tasked with identifying the best compound to in-license for a respiratory indication. These deals can be very expensive – will you be confident enough in your analysis to make a recommendation to senior management…?

We are grateful to all the GP2A 2019 sponsors and exhibitors for their support of the conference.

Registration

To register for the conference, please use the registration portal: https://store.nottingham.ac.uk/conferences-and-events/conferences/schools-and-departments/pharmacy/27th-annual-gp2a-medicinal-chemistry-conference

Abstract Submission

Abstracts from conference registrants are invited for poster and oral presentation. Following review of all abstracts by the organising committee, a total of 6 abstracts will be selected for oral presentation.

To submit your abstract, please download complete the ‘abstract template and instructions file‘ below, and follow the instructions carefully. Completed abstracts should be sent (in MS Word format) to gp2a2019@gp2a.org, with the email subject as ‘GP2A2019 Abstract submission‘.

The abstract submission deadline is now extended to midnight (UK time) Friday 31st May 2019

Accommodation

The conference will be held at the East Midlands Conference Centre (EMCC), which is situated on University Park Campus (more information on the registration portal).

The most convenient accommodation is at the Orchard Hotel, which is adjacent to the EMCC.

There are a number of other accommodation options also available in the City Centre and Beeston, both of which are easy to travel to using Nottingham’s bus and tram network.

Prof. Stephen Husbands

Department of Pharmacy & Pharmacology, Centre for Therapeutic Innovation, University of Bath (UK)

A medicinal chemist primarily involved in the development of ligands that target the CNS. My main research interests relate to neuropsychological diseases and targets, in particular the development of low abuse liability analgesics and new treatment agents for drug abuse, depression and anxiety. Recent research has focussed on the development and therapeutic potential of ‘selectively promiscuous’ ligands and has been driven by the understanding that CNS disorders are rarely simple, requiring complex solutions. In closely related projects we are exploring the pro- and anti-inflammatory activities of opioids in the periphery and in the CNS with multiple potential applications, including improved analgesics and new anti-inflammatory agents, particularly for dermatology.
Prof. Paul Leeson

Paul Leeson Consulting. Honorary Prof. of Medicinal Chemistry, School of Pharmacy, University of Nottingham (UK)

 Dr Vania Moreira

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde (UK)



Dr. Moreira is a Chancellor’s Research Fellow (Lecturer in Medicinal Chemistry) at the Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), at the University of Strathclyde, UK. She carries the Title of “Docent” (Adjunct Professor) from the University of Helsinki in Finland, where she has been a Principal Investigator and group leader since 2015.
Dr. Moreiraholds a doctoral degree in Pharmaceutical Organic Chemistry from the University of Coimbra in Portugal, which she completed in 2008. In addition to Portugal, she has carried out research at the University of Maryland School of Medicine, Baltimore, USA (2006-2007), at the University of Ferrara, Italy (2011) and at the Faculty of Pharmacy, University of Helsinki, Finland (2012-present).
Her current research is devoted to exploring the medicinal chemistry of the diterpenoids, namely the resin acids and their derivatives, and has been funded by several international sources including the Finnish Funding Agency for Innovation (TEKES), the Academy of Finland, the Magnus Ehrnrooth Foundation, the Huonekalusäätiö, the Portuguese Science and Technology Foundation (FCT), the European Union (Seventh Framework Programme FP7) and Tenovus Scotland.
In 2016, she was highlighted as one of the “New talents- Europe”, by the European Federation of Medicinal Chemistry (EFMC).
More details can be found from https://tinyurl.com/y8skw9fn
 Dr Geoffrey Wells

School of Pharmacy, University College London (UK)

Geoff Wells is an Associate Professor in Medicinal Chemistry at UCL School of Pharmacy. He pursued a PhD in medicinal chemistry at the University of Nottingham under the supervision of Professor Malcolm Stevens FRS. He spent four years as a postdoctoral researcher in the CRUK Gene Targeted Drug Design Research Group at the School of Pharmacy, University of London, followed by two years working for Pharminox Ltd, an anticancer drug discovery company, as Drug Discovery Project Leader. In October 2007, Dr Wells took up the position of Lecturer in Medicinal Chemistry at The School of Pharmacy. His research work has focused on the design and synthesis of compound classes that affect redox homeostasis, interact with DNA in a sequence selective manner and that have selective cytotoxicity profiles. His current interests include the rational design of agents that modulate cytoprotective effects such as the Keap1-Nrf2 system that regulates antioxidant response element genes.
Prof. Mike Waring

Northern Institute for Cancer Research, Newcastle University (UK)

Dr Chris De Graaf
Director of Computational Chemistry, Sosei Heptares, Cambridge (UK)

Prof. Paul Wyatt
Wellcome Centre for Anti-Infectives Research, School of Life Sciences, University of Dundee (UK)

Prof. John F. Gilmer
School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin (Ireland)
John Gilmer is Professor in Pharmaceutical Chemistry in Trinity College Dublin (TCD). John holds a PhD in molecular recognition chemistry from TCD (1995). He held postdoc and visiting researcher positions in commercial pharmaceutical R&D at TCD and Queens University Belfast from 1995 to 1998 when he was appointed lecturer in the School of Pharmacy at TCD. He contributes to the TCD MPharm Programme and to a range of postgraduate courses related to pharmaceutical research and manufacturing, including MSc programs in Pharmaceutical Sciences and Pharmaceutical Manufacturing Technology (QP). He was Director of Teaching and Learning Postgraduate (2014-2018) and was recently elected Head of School, Pharmacy and Pharmaceutical Sciences. John has an active research group in varied fields of drug discovery and delivery. He is a co-founder of Solvotrin Therapeutics and its Director of Research.
Prof. Pierre Verhaeghe
Faculty of Pharmaceutical Sciences, Paul Sabatier University; CNRS, Toulouse (France)
Between 1997 & 2007, Pierre Verhaeghe studied Pharmacy and Organic Chemistry at the Universities of Caen, Rennes I and Aix-Marseille, where he was also pharmacy resident at the public teaching hospital (AP-HM). After a post-doc experience in the pharmaceutical industry at the J&J research center of Val de Reuil in 2008, PV joined academic research and is now, since 2013, professor of medicinal chemistry at the faculty of pharmaceutical sciences of Paul Sabatier university and team leader at the Laboratoire de Chimie de Coordination (UPR 8241) of the CNRS in Toulouse. The research activities of PV mainly focus on the design, synthesis and study of the mechanism of action of molecular or macromolecular anti-infective compounds targeting human pathogens such as intracellular protozoa (P. falciparum, Leishmania spp, Trypanosoma spp) or anaerobic bacteria (C. difficile).
Dr Nuria Cabedo
Instituto de Investigación Sanitaria INCLIVA (Spain)
I received my PhD in Pharmacy from the University of Valencia (2000), in the group of Prof. D. Cortes. From 2001-2004, I was a postdoctoral research fellow at several institutions (IRCOF, Rouen, CERMN, Caen, Chemistry Dept. of the University of Manchester). In 2005, I returned as postdoctoral researcher at the Centro de Ecología Química Agrícola of the Polytechnic University of Valencia. In 2015, I worked in the Biotechnology Company Biopolis of the Scientific Park of the University of Valencia.
Since 2016, I was hired by the Biomedical Research Institute INCLIVA of the Foundation for the Research of the Hospital Clínico Universitario of Valencia. I have participated in 5 regionally/nationally funded projects andam a member of the Research Strategy in Personalized Medicine and Development of Innovative Medicines within the RIS3 measures framework and the COST Action MuTaLig. Since 2011, I have taught at both graduate and postgraduate levels within the Pharmacology Department, University of Valencia as an associate/invited professor.
My research interests include the medicinal chemistry of natural products and synthetic analogues focused mainly on dopaminergic receptors, mitochondrial respiratory chain inhibitors, anti-inflammatory agents and PPARs, in order to treat cardiometabolic disorders and neurological diseases. 
Dr Sébastien Gouin
University of Nantes (France)
Dr Sébastien Gouin is a CNRS research director in the laboratory CEISAM of the University of Nantes (France). He was born in Le Mans in 1976 and studied organic chemistry at the University of Nantes where he received his PhD in 2003. After postdoctoral training with Prof. Paul V. Murphy at University College Dublin (Ireland), he was appointed as a CNRS researcher in the University of Amiens. The present research activities of his group in Nantes are focused on the development of mono- and multivalent glycoconjugates interfering with carbohydrate-binding and processing proteins (lectins and glycosidases) from pathogens.
Prof. Maart Saarma
University of Helsinki (Finland)

Mart Saarma is a Professor of Biotechnology and head of the Laboratory of Molecular Neuroscience at the Institute of Biotechnology, HiLIFE, University of Helsinki. His research group is investigating the signaling and biological functions of GDNF family ligands and endoplasmic reticulum located CDNF/MANF neurotrophic factor families, both within and outside of the nervous system. They are also interested in the therapeutic potential of these proteins in various diseases, so they are testing their efficacy in animal models of Parkinson’s disease, amyotrophic lateral sclerosis, stroke and diabetes mellitus. One of the highlights of their research has been, in 2017, the initiation of phase I-II clinical trials of CDNF protein in Parkinson’s disease patients by the Finnish company Herantis Pharma Plc.

Prof. Saarma was the Vice President of the European Research Council (2015-16) and a member of the EMBO Council (2011-16). He is a member of several academies, EMBO and Academia Europea. Prof. Saarma’s group has characterized several new GDNF family receptors, discovered a new neurotrophic factor CDNF and shown that it very efficiently protects and repairs dopamine neurons in animal models of Parkinson’s disease.

We are delighted to announce that the 27th Annual GP2A Medicinal Chemistry Conference will take place between 21st-23rd August 2019 at the University of Nottingham (UK).

The meeting will be hosted by the Division of Biomolecular Sciences and Medicinal Chemistry within the School of Pharmacy here at the University of Nottingham and will take place at the East Midlands Conference Centre which is situated on University Park Campus.

This year we will be running an exciting pre-meeting workshop aimed at PhD students and postdoctoral researchers on due diligence relating to quantitative pharmacological data. This workshop has been put together by Prof. Stephen Charlton (Professor of Molecular Pharmacology and Drug Discovery and Chief Scientific Officer of Excellerate Biosciences Ltd) and Prof. Stephen Hill (Professor of Molecular Pharmacology and current President of the British Pharmacological Society). The workshop is included in the conference registration fee, however spaces will be limited.

The meeting will include a range of invited speakers, in addition to a number of opportunities for PhD students and postdoctoral researchers to speak, industrial exhibitors and poster presentations. Registration and the call for abstracts for poster and oral presentations will be opened shortly – more details will appear here soon, and will also be disseminated by email. In the meantime any general enquiries can be directed to gp2a2019@gp2a.org.

We look forward to welcoming you to Nottingham with the aim of continuing on from what was an excellent and scientifically stimulating meeting earlier this year in Normandy. Please save the dates in your diaries!

Best wishes from the organising committee:

Dr. Shailesh Mistry & Prof. Barrie Kellam

Social Event

Conference dinner

The GP2A-JFB 2018 conference, organized by Prof. Patrick Dallemagne – Univ. Caen, Prof. Thierry Besson – Univ. Rouen and Prof. Christophe Rochais – Univ. Caen took place in Asnelles sur Mer (Normandy – F) from 13th to 15th June 2018.

Welcome

   
Prof. Raphaël Frédérick
University of Louvain (B)
JFB grouping
Prof. Pascal Marchand
University of Nantes (F)
Chair of GP2A
   
Welcome slide Welcome Team

Plenary lectures

     
Dr Louisa Barré – CEA
University of Caen (F)
Dr Thomas Cailly
University of Caen (F)
Dr Corinne Fruit
University of Rouen (F)
 
Prof. Raphaël Frédérick
University of Louvain (B)
Dr Niamh O’Boyle
University of of Dublin (IRL)
Dr Tatiana Besset
University of Rouen (F)
   
Prof. Maria Laura Bolognesi
University of Bologna (I)
Prof. Maria-João R. P. Queiroz
University of Minho, Braga (P)
Prof. Pascal Bonnet
University of Orléans (F)
     
Dr Shailesh Mistry
University of Nottingham (UK)
Prof. A. Ganesan
University of East Anglia, Norwich (UK)
Dr Cédric Logé
University of Nantes (F)
   
Prof. Johan Van der Eycken
University of Ghent (B)
Prof. Anne-Sophie Voisin-Chiret
University of Caen (F)

Early career researchers’ showcases

Dr Jade Fogha – ICOA
University of Orléans (F)
Dr Clément Fontenelle – LCMT
University of Caen (F)
Dr Marta Abellán-Flos ICMMO
University of Orsay (F)
Dr Charles Skarbek – ICMMO
University of Orsay (F)
Dr Julien Diharce – ICOA
University of Orléans (F)

Flash presentations of posters (PhD students)

   
Thomas Dal Maso
University of Namur (B)
Pauline Zipfel
University of Caen (F)
Yvain Gérard
University Clermont Auvergne (F)
     
Irène Pachon
University of Besançon (F)
Windbedema Ouedraogo
University of Caen (F)
Pauline Loupias
University of Picardie (F)
   
Sangheeta-Laura Thirumaran
University of Caen (F)
Fanny Danton
University Le Havre Normandie (F)
Viet Hung Dao
University of Nantes (F)
     
Reynald Mangeant
University of Caen (F)
Amanda Garrido
University of Tours (F)
Caroline Lanthier
University of Caen (F)
   
Gilles Degotte
University of Liège (B)
Agnieszka Zak
University of Orléans (F)
Bérénice Hatat
University of Caen & Montpellier (F)
     
Léo Faïon
University of Lille (F)
Martina de Pascale
University of Caen (F)
Alice Ameryckx
University of Louvain (B)
 
Christina Picken
University College London (UK)

Best Oral Presentations

Reynald Mangeant, University of Caen – France: Fluorinated indazole derivatives: promising structures for 5-HT4 receptors PET radiotracers
Dr Jade Fogha, University of Orléans – France: Crystallization additives, not so useless in in-silico kinase research

Best Posters

Florence Couly, University of Rouen – France: Promising DYRK1A inhibitor synthesized by late-stage C-H Arylation (right)
Birgit Gaiser, University of Copenhagen, Denmark: Targeting Metastable Binding Sites with Bitopic Ligands – A New Concept in GPCR Medicinal Chemistry (left)

Exhibitors at the GP2A-JFB2018 meeting :

Sponsors of the GP2A-JFB2018 meeting :

This year’s conference, GP2A-JFB 2018, organised by members from the Universities of Caen and Rouen will take place between 13th and 15th June at Asnelles sur Mer (Normandie).

Final program schedule is available HERE !!

Prizes will be given during the congress.
– 2 Best Poster Awards sponsored by ManRos Therapeutics
– 1 Best “PhD short communication” Award sponsored by MDPI
– 1 Best “Young researcher communication” Award sponsored by MDPI

As a joint meeting with the 32nd Journées Franco-Belges de Pharmacochimie, the 26th Annual GP2A Medicinal Chemistry Conference will provide a unique opportunity to engage with a wide group of European Chemists.

The “Journées Franco-Belges de Pharmacochimie” (JFB) is a widely recognized annual meeting on Medicinal Chemistry. This two-day symposium, whose first edition was held in 1986, aims to promote exchanges between medicinal chemists, mainly from France and Belgium. It is renowned for the advanced science presented, conviviality, and outstanding opportunities for senior and young scientists to exchange knowledge. An important part of the scientific program, besides plenary lectures given by internationally recognized scientists, is usually devoted to open lectures giving the opportunity for young scientists to present their research. The themes discussed during the meeting are those generally encountered by medicinal chemists: organic synthesis, bioinformatics and computer-aided drug design, pharmacological tests and molecular biology.

Registration fees

# Including 2 nights (Wednesday + Thursday) + 2 breakfasts (Thursday + Friday) + 3 lunches (Wednesday + Thursday + Friday) + 1 dinner (Wednesday) + 1 gala dinner (Thursday)

Academic: €300

PhD student: €200

Post-doctoral researcher: €200

Industrial: €350

# extra night (Tuesday) + 1 dinner (Tuesday) + 1 breakfast (Wednesday)

Academic: €365

PhD student: €265

Post-doctoral researcher: €265

Industrial: €450

Deadline for registration: 30th April 2018

Start of registration and abstract submission: 1st February 2018

PLEASE REGISTER HERE !!

Postdoctoral researchers and young Lecturers will be able to present their work as poster or as oral presentation (15 minutes + questions). Some abstracts will be selected by the Scientific Committee for oral presentation, the others will be presented as posters.

PhD students will be able to present their work as posters. Some abstracts will be selected for additional flash oral presentation (5 minutes w/o question).

PLEASE SUBMIT YOUR ABSTRACT HERE !! (abstract template)

For the venue to the site of congress, a shuttle will be available for free from Caen to Annelles sur Mer. More details will follow.

Most of the accommodation included in the registration are twin rooms. For single room booking, please contact the local organising committee.


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