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Virtually all vital cellular processes are controlled by protein-protein interactions (PPIs), including gene expression, proliferation, intracellular communication and apoptosis. The understanding and manipulation of PPIs therefore plays an important role in fathoming the biology of healthy and diseased states. Achieving this goal will lead to new probes of cell signalling pathways or systems biology, and molecular therapeutics for addressing unmet medical need.
To date, only a few PPIs have been the subject of drug discovery initiatives by the pharmaceuticals industry. Given the potential opportunities around modulating more of the estimated >650,000 PPIs, this field continues to generate considerable scientific interest, which has stimulated significant academic and industrial innovation. This meeting will address recent advances in the area. Topics will include: inducing protein degradation using small molecules, protein engineering and synthetic biology, integration of computational and experimental methods to study PPIs, characterisation and identification of new PPI inhibitors and lead optimization challenges for molecules targeting PPIs from case studies in drug discovery.Speakers from both industry and academia will describe strategies for addressing these challenges whilst showcasing the opportunity for creativity and innovation.
Delegate Fees
GB£220 . . . . . . . . . . . . . . . . . SCI/RSC Member
GB£290.. . . . . . . . . . . . . . . . . Non-Member
GB£85 . . . . . . . . . . . . . . . . . . SCI/RSC Student Member
GB£135 . . . . . . . . . . . . . . . . . SCI Subsidised Member
PROGRAMME
Thursday 4 April
10.00 Registration
10.20 Introductory remarks
10.30 Plenary Talk: Structure based design of high affinity inhibitors of B-cell lymphoma 6 (BCL6) protein-protein interaction
Dr Graeme Robb, AstraZeneca
11.15 Preclinical validation of a therapeutic peptide targeting a protein/protein interaction
Dr Angelita Rebollo, Centre d’Immunologie et des Maladies Infectieuses
11.45 Designing and disrupting protein-protein interactions in test tubes and cells
Professor Dek Woolfson, University of Bristol
12.15 Lunch, exhibition and posters
13.30 Mimicking Protein-Protein Interactions in Persistent Bacteria
Dr Anna Barnard, Imperial College
13.45 Platforms for the generation and high-throughput screening of cyclic peptide libraries
Professor Ali Tavassoli, University of Southampton
14.15 Stabilising Protein-Protein Interactions: A Challenge for Ligand Discovery
Dr Richard Doveston, University of Leicester
14.45 A novel crosslinking method allows rapid and unbiased analysis of dynamic and tight protein-protein interaction interfaces in vitro
Jim Horne, University of Leeds
15.00 Ligand directed fragment ligation targeting protein-protein interactions
Dr Zsófia Hegedüs, University of Leeds
15.15 Peptide grafting into a repeat-protein scaffold can impart low nanomolar affinity for Keap1
Sarah Madden, University of Cambridge
15.30 Stabilization of Protein-Protein Interactions
Dr Pim J. de Vink, Eindhoven University of Technology
15.45 Refreshments
16.00 A new method to probe protein interactions in solution
Dr Maya Wright, Fluidic
16.15 Plenary talk: Fragment Based Drug Discovery for PPIs
Dr David Rees, Astex Pharmaceuticals
17.00 Poster session and wine mixer
Friday 5 April
9.00 Plenary talk: Navigating the landscape of Bcl-2-binding peptides
Professor Amy Keating, Massachusetts Institute of Technology
9.45 A new class of RAS-effector protein-protein interaction inhibitors derived using an intracellular antibody fragment
Dr Philip Fallon, Domainex
10.15 Nanobodies directed against Tau protein to modulate its protein interactions in Alzheimer’s disease
Professor Isabelle Landrieu, Universite de Lille
10.45 Refreshments
11.15 Discovery of Mcl-1-specific inhibitor AZD5991 and structure based design learnings from Mcl-1 PPI inhibition
Dr Elisabetta Chiarparin, AstraZeneca
11.45 Getting in to deep water: the discovery and optimisation of BCL6 inhibitors
Dr Ben Bellenie, ICR
12.15 Lunch, exhibition and posters
13.30 Development of a potent class of small molecule inhibitors of the MDM2-p53 protein-protein interaction
Dr Ian Hardcastle, University of Newcastle
14.00 Interaction of viral envelope proteins with host prohibitins
Dr Anja Winter, Keele University
14.30 The design and synthesis of selective CREBBP bromodomain ligands
Professor Stuart Conway, University of Oxford
15.00 Refreshments and poster prize presentation
15.15 Plenary talk: PROTAC-mediated Protein Degradation: A New Therapeutic Modality
Professor Craig Crews, Yale University
16.00 Closing remarks
16.15 Close
Virtually all vital cellular processes are controlled by protein-protein interactions (PPIs), including gene expression, proliferation, intracellular communication and apoptosis. The understanding and manipulation of PPIs therefore plays an important role in fathoming the biology of healthy and diseased states. Achieving this goal will lead to new probes of cell signalling pathways or systems biology, and molecular therapeutics for addressing unmet medical need.
To date, only a few PPIs have been the subject of drug discovery initiatives by the pharmaceuticals industry. Given the potential opportunities around modulating more of the estimated >650,000 PPIs, this field continues to generate considerable scientific interest, which has stimulated significant academic and industrial innovation. This meeting will address recent advances in the area. Topics will include: inducing protein degradation using small molecules, protein engineering and synthetic biology, integration of computational and experimental methods to study PPIs, characterisation and identification of new PPI inhibitors and lead optimization challenges for molecules targeting PPIs from case studies in drug discovery.Speakers from both industry and academia will describe strategies for addressing these challenges whilst showcasing the opportunity for creativity and innovation.
Delegate Fees
GB£220 . . . . . . . . . . . . . . . . . SCI/RSC Member
GB£290.. . . . . . . . . . . . . . . . . Non-Member
GB£85 . . . . . . . . . . . . . . . . . . SCI/RSC Student Member
GB£135 . . . . . . . . . . . . . . . . . SCI Subsidised Member
PROGRAMME
Thursday 4 April
10.00 Registration
10.20 Introductory remarks
10.30 Plenary Talk: Structure based design of high affinity inhibitors of B-cell lymphoma 6 (BCL6) protein-protein interaction
Dr Graeme Robb, AstraZeneca
11.15 Preclinical validation of a therapeutic peptide targeting a protein/protein interaction
Dr Angelita Rebollo, Centre d’Immunologie et des Maladies Infectieuses
11.45 Designing and disrupting protein-protein interactions in test tubes and cells
Professor Dek Woolfson, University of Bristol
12.15 Lunch, exhibition and posters
13.30 Mimicking Protein-Protein Interactions in Persistent Bacteria
Dr Anna Barnard, Imperial College
13.45 Platforms for the generation and high-throughput screening of cyclic peptide libraries
Professor Ali Tavassoli, University of Southampton
14.15 Stabilising Protein-Protein Interactions: A Challenge for Ligand Discovery
Dr Richard Doveston, University of Leicester
14.45 A novel crosslinking method allows rapid and unbiased analysis of dynamic and tight protein-protein interaction interfaces in vitro
Jim Horne, University of Leeds
15.00 Ligand directed fragment ligation targeting protein-protein interactions
Dr Zsófia Hegedüs, University of Leeds
15.15 Peptide grafting into a repeat-protein scaffold can impart low nanomolar affinity for Keap1
Sarah Madden, University of Cambridge
15.30 Stabilization of Protein-Protein Interactions
Dr Pim J. de Vink, Eindhoven University of Technology
15.45 Refreshments
16.00 A new method to probe protein interactions in solution
Dr Maya Wright, Fluidic
16.15 Plenary talk: Fragment Based Drug Discovery for PPIs
Dr David Rees, Astex Pharmaceuticals
17.00 Poster session and wine mixer
Friday 5 April
9.00 Plenary talk: Navigating the landscape of Bcl-2-binding peptides
Professor Amy Keating, Massachusetts Institute of Technology
9.45 A new class of RAS-effector protein-protein interaction inhibitors derived using an intracellular antibody fragment
Dr Philip Fallon, Domainex
10.15 Nanobodies directed against Tau protein to modulate its protein interactions in Alzheimer’s disease
Professor Isabelle Landrieu, Universite de Lille
10.45 Refreshments
11.15 Discovery of Mcl-1-specific inhibitor AZD5991 and structure based design learnings from Mcl-1 PPI inhibition
Dr Elisabetta Chiarparin, AstraZeneca
11.45 Getting in to deep water: the discovery and optimisation of BCL6 inhibitors
Dr Ben Bellenie, ICR
12.15 Lunch, exhibition and posters
13.30 Development of a potent class of small molecule inhibitors of the MDM2-p53 protein-protein interaction
Dr Ian Hardcastle, University of Newcastle
14.00 Interaction of viral envelope proteins with host prohibitins
Dr Anja Winter, Keele University
14.30 The design and synthesis of selective CREBBP bromodomain ligands
Professor Stuart Conway, University of Oxford
15.00 Refreshments and poster prize presentation
15.15 Plenary talk: PROTAC-mediated Protein Degradation: A New Therapeutic Modality
Professor Craig Crews, Yale University
16.00 Closing remarks
16.15 Close
