Final programme - Oral sessions
Programme and abstracts for oral session - download HERE
Sunday 9 September 2018 |
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| 18.00 - 19.30 19.00 | S01 |
Plenary lectures Chair: Patrick Masson, Kamil Kuca |
| 18.00 - 18.45 | S01-1 | Chronic illness from organophosphorus toxicant exposure Oksana Lockridge |
| 18.45 - 19.30 | S01-2 | The Catalytic Power of Phosphotriesterases for the Hydrolysis and Destruction of Organophosphorus Nerve Agents Frank Raushel |
| 19.30 - 21.00 | Welcome party | |
Monday 10 September 2018 |
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| 08.15 - 08.30 | Opening ceremony | |
| 08.30 - 11.30 | S02 | Structure and dynamics of cholinesterases and OP hydrolases Chair: Yuan-Ping Pang, Joel Sussman |
| 08.30 - 08.50 | S02-1 | Recent Breakthroughs in the Structure/Function Studies of Acetylcholinesterase Joel Sussman |
| 08.50 - 09.10 | S02-2 | Coupling of Acetylcholinesterase to the Interfacial Phase State Israel Silman |
| 09.10 - 09.30 | S02-3 | The other side of AChE: Allosteric sites and modulators Nuria E. Campillo |
| 09.30 - 09.50 | S02-4 | Partial unfolding of insect acetylcholinesterase: Steps toward cysteine-targeting insecticides Yuan-Ping Pang |
| 09.50 - 10.10 | Coffee break | |
| 10.10 - 10.30 | S02-5 | The protonation state of Glu197 and its important role in stabilizing catalytic triad of butyrylcholinesterase Junjun Liu |
| 10.30 - 10.50 | S02-6 | Recipes to design specific ligands of human butyrylcholinesterase Florian Nachon |
| 10.50 - 11.10 | S02-7 | Exploring the evolutionary potential of the αE7 carboxylesterase Galen Correy |
| 11.10 - 11.30 | S02-8 | Protein dynamics of phosphotriesterase: Two cations required for enzyme catalysis Yuan-Ping Pang |
| 11.30 - 12.30 | Lunch and posters | |
| 12.30 - 15.15 | S03 |
Interaction of cholinesterases with substrates, inhibitors and reactivators
Chair: Terrone Rosenberry, Franz Worek |
| 12.30 - 12.50 | S03-1 | New Progress in Drug Design, Discovery and Development Involving Cholinesterases Chang-Guo Zhan |
| 12.50 - 13.10 | S03-2 | In searching for the mechanism of butyrylcholinesterase activators Jure Stojan |
| 13.10 - 13.30 | S03-3 | Computational analysis of reaction mechanisms for optimization of butyrylcholinesterase-based catalytic bioscavengers against organophosphorus agents Sofya Lushchekina |
| 13.30 - 13.50 | S03-4 | Enhancement in pyridinium oxime-assisted reactivation of tabun-inhibited acetylcholinesterase achieved by active site mutations Zrinka Kovarik |
| 13.50 - 14.10 | S03-5 | The search for resistance-breaking and species-selective mosquitocidal inhibitors of Anopheles gambiae AChE Paul Carlier |
| 14.10 - 14.30 | S03-6 | Steric Effects in the Decarbamoylation of Carbamoylated Acetylcholinesterase Terrone Rosenberry |
| 14.30 - 14.45 | S03-7 | Assessment of scoring functions for AChE-ligand interactions Goran Šinko |
| 14.45 - 15.00 | S03-8 | Phenyl valerate esterase activity of human cholinesterases Jorge Estévez |
| 15.00 - 15.15 | S03-9 | Effects of memantine and its metabolite Mrz 2/373 on soman-induced inhibition of bovine erythrocyte acetylcholinesterase in vitro Miloš Stojiljković |
| 15.15 - 15.40 | Coffee break | |
| 15.40 - 18.10 | S04 | Reactivators of AChE, OP inhibitors - mechanism of toxicity, detection and analytical methods, diagnosis of exposure, detoxification and therapy; counter-terrorism strategies Chair: Franz Worek, Terrone Rosenberry |
| 15.40 - 16.00 | S04-1 | Oximes with ortho-positioned chlorine moiety exhibit improved physical-chemical properties, efficient reactivation of inhibited human acetylcholinesterase and reduced in vivo toxicity Kamil Musilek |
| 16.00 - 16.20 | S04-2 | Design and synthesis of bifunctional fluoropyridinaldoxime reactivators for nerve agent-inhibited human acetylcholinesterase Jagadeesh Yerri |
| 16.20 - 16.40 | S04-3 | Combination of oximes with overlapping reactivation spectra: obidoxime and HI-6 Timo Wille |
| 16.40 - 17.00 | S04-4 | Design of broad spectrum antidotes Fredrik Ekström |
| 17.00 - 17.15 | S04-5 | Demonstration of the First Small Molecule Therapeutics for Resurrection of the Aged form of Acetylcholinesterase after Exposure to Organophosphorus Chemical Nerve Agents and Pesticides Andrew Franjesevic |
| 17.15 - 17.30 | S04-6 | Nanotechnology strategies using oximes-loaded lipid nanoparticles for brain protection against organophosphorus poisoning Tatiana Pashirova |
| 17.30 - 17.50 | S04-7 | Utilizing Structure-Activity Relationships and Mechanistic Insights to Design Non-Oxime Reactivators Linn Cadieux |
| 17.50 - 18.10 | S04-8 | New Non-Oxime Reactivators of Organophosphate Inhibited Acetylcholinesterase with Promising Reactivation Potency Martijn de Koning |
Tuesday 11 September 2018 |
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| 08.00 - 09.40 | S05 | Enzymes and proteins other than ChEs interacting with OP Chair: Oksana Lockridge, Patrick Masson |
| 08.00 - 08.20 | S05-1 | Identifying axonal transport-related targets for reversing the adverse effects of organophosphate exposure Alvin Terry |
| 08.20 - 08.40 | S05-2 | Diagnosis of Poisoning with О-Isobutyl-S-[2-(diethylamino)ethyl]methylphosphonothioate (VR) under Antidotal Therapy with Carboxim Nadezhda Koryagina |
| 08.40 - 09.00 | S05-3 | Copper-dependent hydrolysis of trichloronate by turkey serum and albumin Damianys Almenares López |
| 09.00 - 09.20 | S05-4 | Mass spectral detection of diethoxyphospho-tyrosine adducts on proteins from HEK293 cells using monoclonal antibody depY for enrichment Seda Onder |
| 09.20 - 09.40 | S05-5 | Innovative Biocatalysts as Tools to Detect and Inactivate Nerve Agents Giuseppe Manco |
| 09.40 - 10.00 | Coffee break | |
| 10.00 - 12.10 | S06 | Stoichiometric bioscavanger, biotechnology and therapeutical aspects Chair: Palmer Taylor |
| 10.00 - 10.10 | Commemoration of John Casida Palmer Taylor |
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| 10.10 - 10.30 | S06-1 | Ionizable, Zwitterionic Oximes as Countermeasures to Volatile Organophosphate (OP) Exposure Palmer Taylor |
| 10.30 - 10.50 | S06-2 | Development of pre- and post-countermeasures against OP toxins in macaques Yvonne Rosenberg |
| 10.50 - 11.10 | S06-3 | Human Plasma-Derived Butyrylcholinesterase Is Behaviorally Safe and Effective in Cynomolgus Macaques (Macaca fascicularis) Challenged with Soman Todd Myers |
| 11.10 - 11.30 | S06-4 | Design of a combined aptamer for paraoxon and acetylcholinesterase by in silico approach Daria Belinskaia |
| 11.30 - 11.50 | S06-5 | Prokaryotic expression of human butyrylcholinesterase as a tool for catalytic bioscavenger development Xavier Brazzolotto |
| 11.50 - 12.10 | S06-6 | Bioscavengers and the medical management chain Tom Mann |
| 12.10 - 13.40 | Lunch and posters | |
| 13.40 - 16.00 | S07 | Catalytical Bioscavangers - PON and PTE Chair: Eugenio Vilanova, Florian Nachon |
| 13.40 - 13.50 | Commemoration of Doug Cerasoli Tamara C. Otto |
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| 13.50 - 14.00 | S07-1 | Borderline between catalytic and non-catalytical bioscavengers: the example of albumin and reversible B-esterases Eugenio Vilanova |
| 14.00 - 14.20 | S07-2 | Catalytic Scavengers Provide Broad-Spectrum Protection against Organophosphorus Nerve Agents Tamara Otto |
| 14.20 - 14.40 | S07-3 | Paraoxonase 1 variant I-F11 gene therapy using adeno-associated virus8 (AAV8) offers long-term protection against G-type chemical warfare nerve agents Nageswararao Chilukuri |
| 14.40 - 15.00 | S07-4 | Phosphotriesterase (PTE) Designed as a Tethered Monomer Stephen Kirby |
| 15.00 - 15.20 | S07-5 | A new animal model to investigate organophosphorus poisoning and enzymatic decontamination Laetitia Poirier |
| 15.20 - 15.40 | S07-6 | Paraoxonase-2 dependent redox control of platelet physiology Victoria Petermann |
| 15.40 - 16.00 | S07-7 | Copper with chicken serum albumin show stereoselective hydrolysis of chiral phosphoramidates Antonio Monroy |
| 18.00 | Walking tour around the city | |
| 20.00 | Concert in the Cathedral of the Holy Spirit | |
Wednesday 12 September 2018 |
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| 08.30 - 11.30 | S08 |
3D section - structure and dynamics of α/β hydrolases and OP hydrolases, |
| 08.30 - 08.55 | S08-1 | Insights into the Yin and the Yang of Acetylcholinesterase Inhibition by Mechanistic X-Ray Crystallography Doriano Lamba |
| 08.55 - 09.20 | S08-2 | Photo-induced release of an acetylcholinesterase inhibitor Eugenio de la Mora |
| 09.20 - 09.45 | S08-3 | Structural studies of Anopheles gambiae acetylcholinesterase provide insight towards improved insecticides for malaria vector control Jonah Cheung |
| 09.45 - 10.05 | Coffee break | |
| 10.05 - 10.30 | S08-4 | Room-temperature crystallography and neutron scattering studies of human acetylcholinesterase to inform the design of oxime reactivators Andrey Kovalevsky |
| 10.30 - 10.55 | S08-5 | Crystal structures of human cholinesterases in complex with supramolecular ligands José Dias |
| 10.55 - 11.20 | S08-6 | Modifications of Cholinesterase Structure and Function in Covalent Organophosphate Conjugates Visualized in 2D, 3D and VR Zoran Radić |
| 11.20 - 11.30 | Concluding sentence Zoran Radić |
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| 11.30 - 13.00 | Lunch and posters | |
| 13.00 | Trips | |
Thursday 13 September 2018 |
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| 08.00 - 11.30 | S09 | Biological functions, development and non-cholinergic function of cholinesterases Chair: Shani Shenhar-Tsarfaty, Israel Silman |
| 08.00 - 08.15 | Commemoration of Eric Barnard Israel Silman, Karl Tsim |
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| 08.15 - 08.35 | S09-1 | Cholinergic mechanisms at the core of skeletal and retinal histogenesis Paul Layer |
| 08.35 - 08.55 | S09-2 | Butyrylcholinesterase as a ghrelin modulator impacting anxiety, stress, obesity, and drug cravings Stephen Brimijoin |
| 08.55 - 09.15 | S09-3 | Assembly of PRiMA-linked form of acetylcholinesterase in neurons: the role of enzyme inhibitor acting as chemical chaperon Karl Tsim |
| 09.15 - 09.35 | S09-4 | Evolution of the first disulfide bond in the cholinesterase-carboxylesterase (COesterase) family: Possible consequences for cholinesterase expression in prokaryotes Arnaud Chatonnet |
| 09.35 - 09.55 | Coffee break | |
| 09.55 - 10.15 | S09-5 | Acetylcholinesterase in neuromuscular synaptic clefts of vertebrates Lili Anglister |
| 10.15 - 10.35 | S09-6 | Respiration during organophosphate and carbamate intoxication when acetylcholinesterase is not anchored at cholinergic synapses Eric Krejci |
| 10.35 - 10.55 | S09-7 | Single nucleotide polymorphisms in the genes encoding AChE and its miR-608 regulator co-modulate anxiety and blood pressure Alon Simchovitz |
| 10.55 - 11.15 | S09-8 | Dioxin suppresses AChE expression in neuron and muscle Heidi Xie |
| 11.15 - 11.30 | S09-9 | Wnt3a induces the transcription of acetylcholinesterase: an enzyme playing a role in osteoblastic differentiation Miranda Xu |
| 11.30 - 12.30 | Lunch and posters | |
| 12.30 - 14.45 | S10 | Alzheimer's disease and diseases related to cholinesterases Chair: Ana Martinez, Maria-Laura Bolognesi |
| 12.30 - 12.50 | S10-1 | Restoring mitochondria dysfunction and acetylcholine levels as a prospective therapeutic strategy for Alzheimer’s disease Fernanda Borges |
| 12.50 - 13.10 | S10-2 | From dual binding site AChE inhibitors to chameleon molecules: discovery of potent BuChE inhibitors Ana Martinez |
| 13.10 - 13.30 | S10-3 | Discovery and development of neuroprotective and disease-modifying anti-AD drug leads from the Chinese medicine Yifan Han |
| 13.30 - 13.50 | S10-4 | Fifty shades of cholinesterase immobilization and their application to drug discovery Manuela Bartolini |
| 13.50 - 14.10 | S10-5 | Serum cholinesterase activity and Alzheimer disease comorbidities - can bariatric surgery change your sympathetic prone state? Shani Shenhar-Tsarfaty |
| 14.10 - 14.30 | S10-6 | Indazolylketones: hit to lead optimization of a multitarget drugs Nuria E. Campillo |
| 14.30 - 14.45 | S10-7 | Butyrylcholinesterase genetic polymorphism and neuroimaging biomarkers in Alzheimer’s disease Drew DeBay |
| 14.45 - 15.10 | Coffee break | |
| 15.10 - 17.40 | S11 | Multi-target-directed ligands in Alzheimer's disease primarily targeting cholinesterases Chair: Maria-Laura Bolognesi, Ana Martinez |
| 15.10 - 15.30 | S11-1 | Case studies for successful combination of ChE inhibitors and GPCR ligands (cannabinoid 2 and histamine 3 receptors) Michael Decker |
| 15.30 - 15.50 | S11-2 | From acetylcholinesterase inhibitors to multi-target-directed ligands (MTDLs): a step forward in Alzheimer's disease drug discovery Maria-Laura Bolognesi |
| 15.50 - 16.10 | S11-3 | From selective butyrylcholinesterase inhibitors to multi-target-directed ligands as lead compounds for Alzheimer’s disease Stanislav Gobec |
| 16.10 - 16.30 | S11-4 | Discovery and characterization of tacrine/huprine-tryptophan heterodimers as novel multipotent compounds against Alzheimer's disease Jan Korabecny |
| 16.30 - 16.50 | S11-5 | Novel conjugates based on γ-carbolines, carbazoles, phenothiazines, and aminoadamantanes as multifunctional agents for Alzheimer’s disease treatment Galina Makhaeva |
| 16.50 - 17.10 | S11-6 | Pleiotropic prodrugs: a novel polypharmacology approach to treat neurodegenerative diseases Christophe Rochais |
| 17.10 - 17.25 | S11-7 | Toward an innovative treatment of Alzheimer’s disease: Design of multi-target directed ligands (MTDLs) targeting acetylcholinesterase (AChE) and alpha-7 nicotinic receptors (alpha-7 nAChRs) Mégane Pons |
| 17.25 - 17.40 | S11-8 | Molecular modeling in search of new, multi-target ligands against Alzheimer´s disease Jakub Jonzcyk |
| 20.00 | Gala dinner | |
Friday 14 September 2018 |
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| 08.00 - 09.20 | S12 | Varia Chair: Kamil Kuca, Ondrej Soukup |
| 08.00 - 08.20 | S12-1 | Design of a butyrylcholinesterase mutant for detoxifying cocaine and its toxic metabolites in concurrent use of cocaine and alcohol Fang Zheng |
| 08.20 - 08.40 | S12-2 | 7-Methoxyderivative of tacrine is a ‘foot-in-the-door’ blocker of GluN1/GluN2 and GluN1/GluN3 NMDA receptors Martin Horak |
| 08.40 - 09.00 | S12-3 | The Caenorhabditis elegans pharynx as a model system to investigate and mitigate against the effects of anti-cholinesterase drugs Patricia Gonzalez |
| 09.00 - 09.20 | S12-4 | Pharmacokinetics of bis-pyridinium mono-aldoximes Huba Kalasz |
| 09.20 - 09.30 | Concluding remarks | |
| 10.00 | Shuttle bus to Prague Airport | |