9th GPCRs in Medicinal Chemistry
Event
9th RSC-BMCS/RSC-SCI Symposium on GPCRs in Medicinal Chemistry
Dates
Wednesday 2nd – Friday 4th October 2024
Place
Evotec Campus Levi-Montalcini, Verona, Italy
Downloads and Links
Twitter hashtag – #GPCRs24
To register for the meeting, click here
To download the venue guide, click here
To download the first announcement poster, click here
To download the second announcement poster, click here
To download the third announcement poster, click here
To book accommodation, click here
Synopsis
The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine. We are pleased to hold this 9th meeting in the series on GPCR drug discovery, which combines cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.
The meeting will consist of:
• Case studies in GPCR drug discovery and development
• Structural biology advances and impact on drug design
• Showcasing multiple modalities and drug discovery approaches to modulating GPCRs
Also: poster session – trade exhibition opportunities – two evening dinners and vineyard visit – accommodation agency booking service.
Call for Abstracts
Abstract submission is now closed.
Want to become a member?
To join the RSC and qualify for discounted registration fees at all RSC, please click here.
Registration
Registration open! To register click here.
Early Bird Rate (until 5th July 2024)
RSC/SCI Member- £575
Non-Member- £800
RSC/SCI Student** Member*- £230
Student** Non-Member- £345
Standard Rate (from 6th July 2024)
RSC/SCI Member- £675
Non-Member- £900
RSC/SCI Student** Member*- £280
Student** Non-Member- £395
* Member is a paid-up member of the RSC or SCI
** Student rates apply to undergraduate and post-graduate students only, but not post-doctoral students or students in full-time employment.
Registration fees include:
– coach transport between Verona city centre and the Evotec campus at the start and end of each day
– dinner on Wednesday evening at Spiller Restaurant
– vineyard visit and dinner on Thursday evening at Rocca Sveva.
Networking Social Activities and Accommodation
The informal dinner on the first evening will be a great time to come together to enjoy a traditional three-course meal. The dinner will take place on Wednesday, 2nd October at Spiller Restaurant, located within a few minutes walk of the venue, and is included in the registration package.
A vineyard visit and informal dinner will be held on Thursday, 3rd October. The visit to Rocca Sveva will consist of a guided tour of the underground cellars of Cantina Soave, an explanation of the wines to be served at dinner, an aperitivo outside the restaurant, an opportunity to use the wine shop, and a fantastic dinner with wine-sampling in the Locanda del Borgo. (Coach transport will be provided.)
Venue and Travel
Detailed travel information may be found in this Venue Guide.
A coach service will be provided by the conference between Verona city centre (Giardini Pradaval) and Evotec at the beginning and end of each day, and on a daily basis. On Thursday evening, the coach service will travel to the vineyard and later back to Verona city centre.
Accommodation
A selection of accommodation options in the area has been put together for attendees of the conference. To visit the website and book, please click here.
Exhibitor Opportunity
The Exhibitor Package (£1,500) includes:
– stand space measuring 3 metres wide x 2 metres deep
– table measuring 160 cm wide x 80 cm deep and chair
– electrical and wi-fi access
– your logo and full promotional page in the delegate handbook
– your web-linked company name on this page
– your logo in the rolling slides, shown during the breaks
– full attendance at the technical programme, poster sessions, Wednesday evening dinner, and Thursday evening vineyard visit and dinner.
Important further information about Evotec’s requirements for advance deliveries may be found here.
Exhibitor Packages include full participation in the social activities.
Confirmed Exhibitors
Confirmed sponsors
Programme
Wednesday 2nd October 2024
| 08.30 | Registration and Refreshments |
| Session Chair: Adrian Hall | |
| 09.20 - 09.35 | Welcome and Opening Remarks: Adrian Hall and Maria Pilla |
| 09.35 - 10.25 | KEYNOTE: Nicola Smith (UNSW) – Pitfalls and caveats with orphan G protein-coupled receptor pairings |
| 10.25 - 10.55 | Andrew Stott (Cerevance) - The Discovery of Potent, Selective, CNS-penetrant GPR55 agonists |
| 10.55 - 11.25 | Refreshments, exhibition and posters |
| 11.25 - 11.55 | Daniel Meibom (Bayer AG) - BAY-6096: A Potent, Selective, and Highly Water-Soluble Adrenergic α2B Antagonist |
| 11.55 - 12.25 | Daniele Andreotti (Evotec) - A Structure Based Drug Discovery approach towards a novel Orexin 2 Receptor antagonist |
| 12.25 - 14.00 | Lunch, Exhibition, Evotec Site Tour and Posters |
| Session Chair: Daniel Jones | |
| 14.00 - 14.20 | Rachel Johnson (Sygnature Discovery) - Revisiting the serotonin-bound state of 5-HT2AR with cryo-EM |
| 14.20 - 14.40 | Sonja Peter (University of Urbino/Nxera Pharma) - Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential |
| 14.40 - 15.10 | Malliga R Iyer (NIH) - Discovery of Potent, Peripherally Restricted CB1R (Cannabinoid Receptor-1) Antagonists: Studies Leading to a Clinical Candidate |
| 15.10 - 15.40 | Refreshments, exhibition and posters |
| 15.40 - 16.10 | Noureldin Saleh (Schrödinger) - Accurate Modelling of Receptor Functional Response: GPCRs and Beyond |
| 16.10 - 16.40 | Nigel Swain (Nxera Pharma) – Discovery of HTL0039732: A Potent and Selective EP4 Receptor Antagonist for Cancer Immunotherapy |
| 16.40 - 18.00 | Poster session and flash poster presentations with drinks reception FO1: Eszter Szanti-Pinter (Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences) “Identification of cholesterol binding sites on muscarinic acetylcholine receptors by rationally designed steroid-dark quencher probes” FO2: Pulkit Kumar Gupta (Indian Institute of Technology Bhubaneswar) “Structural Modeling of the Ternary Complexes of C5a Receptors” FO3: Olivier Corminboeuf (Idorsia Pharmaceuticals ltd) “Discovery of CCR8 antagonist IDOR-1136-5177 for the treatment of cancer” FO4: Szabolcs Dvoracsko (HUN-REN Biological Research Centre) “In vivo evaluation of novel allosteric/ dualsteric cannabinoid receptor 1 ligands in alcohol and cannabinoid use disorders” |
| 18.30 onwards | Dinner – Spiller Pizza Restaurant – kindly sponsored by Nxera Pharma |
Thursday 3rd October 2024
| 09.00 | Registration |
| Session Chair: Daniele Andreotti | |
| 09.30 - 10.20 | KEYNOTE: Peter Kolb (Phillips-Universitat Marburg) - GPCR Ligands Going Places |
| 10.20 - 10.50 | Graeme Semple (Eurofins) - Discovery of LP-352 (bexicaserin): A 5-HT2CR agonist with unprecedented receptor selectivity |
| 10.50 - 11.20 | Refreshments, exhibition and posters |
| 11.20 - 11.50 | Lubos Remen (LeadXPro) - Enabling structure-based drug discovery on challenging GPCR drug targets |
| 11.50 - 12.20 | James Errey (Evotec) - GPCR Biophysical and Structure Based Drug Design |
| 12.20 - 13.40 | Lunch, exhibition, Evotec Site Tour and posters |
| Session Chair: Thomas Clohessy | |
| 13.40 - 14.10 | Luc VanHijfte (Symeres) - A New Dual Mode of Action to Treat Pain - From Scratch to Pre-Clinical Candidate |
| 14.10 - 14.30 | Iulia Bodnariuc (Utrecht University) - Methodology to study GPCRs in Native Membrane Environment: An In-Cell Solid-State NMR Approach |
| 14.30 - 15.00 | Seungil Han (Pfizer) - Structural Characterization of an Orphan GPCR Reveals a Novel Mechanism of Inverse Agonism |
| 15.00 - 15.30 | Refreshments, exhibition and posters |
| 15.30 - 16.00 | Uwe Grether (Roche) - Deep Dive on Cannabinoid Receptor Type-2: Leveraging the Power of Chemical Probes and Assays to Deliver a Clinical Candidate |
| 16.00 - 16.50 | KEYNOTE: Angela Russell (University of Oxford) - Structural and functional insights into biased signalling at GPR84 |
| 16.50 - 17.00 | Close |
| 17.00 | Coaches depart for Vineyard tour and dinner |
| 19.00 onwards | Dinner |
Friday 4th October 2024
| 09.00 | Registration |
| Session Chair: Barbara Bertani | |
| 09.30 - 10.00 | Robin Löving (Salipro) - Unlocking New Possibilities in Drug Discovery with Wildtype GPCRs and Native Lipids |
| 10.00 - 10.30 | Marta Giuliani (Chiesi) – LPA Receptor Inhibitors: A Promising Therapeutic Approach for Idiopathic Pulmonary Fibrosis |
| 10.30 - 10.35 | Poster prize-giving |
| 10.35 - 11.05 | Refreshments, exhibition and posters |
| 11.05 - 11.55 | KEYNOTE: Patrick Sexton (Monash University) - Understanding the structural basis for selective and non-selective amylin and calcitonin receptor agonists |
| 11.55 - 12.25 | Chris de Graaf (Structure Therapeutics) - GPCR Structure-Based Drug Discovery: From Peptides to Small Molecules |
| 12.25 - 13.20 | Lunch, exhibition and posters |
| Session Chair: Caroline Low | |
| 13.20 - 13.40 | Sidra Faryal (University of Edinburgh) - Pituitary Adenylate Cyclase-Activating Polypeptide analogues as PAC-1 receptor antagonists |
| 13.40 - 14.00 | Giovanna Tedesco (Cresset) - Accurate predictions of binding free energy for G protein-coupled receptors (GPCRs): capturing lipid exposed binding interactions in P2Y1 |
| 14.00 - 14.20 | Adam Schofield (University of Edinburgh) - Peptide-Based Drug Discovery for Migraine Treatment |
| 14.20 | Closing Remarks |
| 14.25 | Close |
| 14.30 | Coaches depart |
Organising Committee
Daniele Andreotti, Evotec
Adrian Hall (co-chairman), UCB
Daniel Jones, Nxera Pharma
Caroline Low (co-chairman), Isomorphic Labs
Lampros Milanos, Charles River Laboratories
Secretariat Contact and Further Information
Hg3 Conferences Ltd
+44 (0)1423 529333
E-mail
