Eric Jnoff
UCB
13 Papers
90 Citations
Eric Jnoff is an academic researcher from UCB. The author has contributed to research in topics: SV2A & Computer science. The author has an hindex of 6, co-authored 13 publications.
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Papers
Binding Mode and Structure-Activity Relationships around Direct Inhibitors of the Nrf2-Keap1 Complex.
Eric Jnoff,Claudia Albrecht,John J. Barker,Oliver Barker,Edward Beaumont,Steven Bromidge,Frederick Arthur Brookfield,Mark A. Brooks,Christian Bubert,Tom Ceska,Vincent Anthony Corden,Graham Dawson,Stephanie Duclos,Tara Fryatt,Christophe Genicot,Emilie Jigorel,Jason Kwong,Rosemary Maghames,Innocent Mushi,Richard Pike,Zara A. Sands,Myron A. Smith,Christopher C. Stimson,Jean-Philippe Courade +23 more
TL;DR: This X‐ray crystal structure provides breakthrough experimental evidence for the true binding mode of the hit compound (S,R,S)‐1 a, as the ligand orientation was found to differ from that of the initial docking model, which was available at the start of the project.
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Open Science Discovery of Oral Non-Covalent SARS-CoV-2 Main Protease Inhibitor Therapeutics
Hagit Achdout,A. Aimon,Elad Bar-David,Haim Barr,Amir Ben-Shmuel,Jim Bennett,Boby Ml,Borden B,Gregory R. Bowman,Juliane Brun,Bvnbs S,Mark Daniel Calmiano,Anna Carbery,Emma Cattermole,Chernyshenko E,John D. Chodera,Austin Clyde,Joseph E. Coffland,Galit Cohen,Jason C. Cole,Alessandro Contini,Cox L,Cvitkovic M,Alexandre Dias,Kim Donckers,Dotson Dl,Alice Douangamath,Shirly Duberstein,Dudgeon T,Louise Dunnett,Peter Eastman,Noam Erez,Eyermann Cj,Michael Fairhead,Fate G,D. Fearon,Oleg Fedorov,Matteo P. Ferla,R.S. Fernandes,Ferrins L,Richard Foster,Holly Foster,Ronen Gabizon,Adolfo García-Sastre,V.O. Gawriljuk,P. Gehrtz,Carina Gileadi,Charline Giroud,William G. Glass,Robert C. Glen,Itai Glinert,Andre S. Godoy,Marian V. Gorichko,T.J. Gorrie-Stone,Griffen Ej,Hart Sh,Jag Paul Heer,Henry M,Mark A. Hill,Horrell S,Matthew F. D. Hurley,Tomer Israely,Jajack A,Eric Jnoff,Dirk Jochmans,Tobias John,Steven De Jonghe,Anastassia L. Kantsadi,Peter W. Kenny,J. L. Kiappes,Koekemoer L,Kovar B,T. Krojer,Alpha A. Lee,Lefker Ba,Haim Levy,Nir London,Petra Lukacik,Hannah E. Bruce Macdonald,MacLean B,Tika R. Malla,Matviiuk T,William McCorkindale,McGovern Bl,Sharon Melamed,Oleg M. Michurin,Mikolajek H,Milne Bf,Morris A,Garrett M. Morris,Morwitzer Mj,Moustakas D,A.M. Nakamura,Jose Brandao Neto,Johan Neyts,Nguyen L,G.D. Noske,Oleinikovas,Glaucius Oliva,Gijs J. Overheul,David R. Owen,Psenak,Pai R,Pan J,Nir Paran,Benjamin Ian Perry,Pingle M,Pinjari J,Boaz Politi,A.J. Powell,Puni R,Victor L. Rangel,Rambabu N. Reddi,Reid Sp,Efrat Resnick,Ripka Eg,Matthew C. Robinson,Robinson Rp,Rodriguez-Guerra J,Rosales R,Rufa D,Christopher J. Schofield,Shafeev M,Shaikh A,Jiye Shi,Khriesto A. Shurrush,Sukrit Singh,Assa Sittner,R. Skyner,Adam Smalley,Smilova,Solmesky Lj,John Spencer,Claire Strain-Damerell,Swamy,Hadas Tamir,Tennant R,Thompson W,Andrew Thompson,Tomasio S,Anthony Tumber,Ioannis Vakonakis,van Rij Rp,Laura Vangeel,Finny S. Varghese,Vaschetto M,Einat B. Vitner,Voelz,Andrea Volkamer,von Delft F,von Delft A,Martin A. Walsh,Ward W,Charlie Weatherall,Shay Weiss,White Km,Wild Cf,Wittmann M,Nicholas A. Wright,Yfat Yahalom-Ronen,Zaidmann D,Zidane H,Nicole Zitzmann +162 more
TL;DR: The COVID Moonshot as discussed by the authors was a fully open-science structure-enabled drug discovery campaign targeting the SARS-CoV-2 main protease, which leveraged crowdsourcing, high throughput structural biology, machine learning, and exascale molecular simulations.
Discovery of Heterocyclic Nonacetamide Synaptic Vesicle Protein 2A (SV2A) Ligands with Single‐Digit Nanomolar Potency: Opening Avenues towards the First SV2A Positron Emission Tomography (PET) Ligands
Joël Mercier,Laurence Archen,Véronique Bollu,Stephane Carre,Yves Evrard,Eric Jnoff,Benoit Kenda,Bénédicte Lallemand,Philippe Michel,Florian Montel,Florence Moureau,Nathalie Price,Yannick Quesnel,Xavier Sauvage,Anne Valade,Laurent Provins +15 more
TL;DR: Using a 3D pharmacophore model based on close analogues of levetiracetam, the rationale design of three heterocyclic non‐acetamide lead compounds are reported, the first single‐digit nanomolar SV2A ligands with suitable properties for development as PET tracers.
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Reversible inhibition of the glycine transporter GlyT2 circumvents acute toxicity while preserving efficacy in the treatment of pain
A Mingorance-Le Meur,P Ghisdal,B Mullier,P De Ron,Patrick Downey,C Van Der Perren,V Declercq,S Cornelis,Michel Famelart,J. van Asperen,Eric Jnoff,Jean-Philippe Courade +11 more
TL;DR: There is a need for novel molecular targets to develop new therapeutics with improved efficacy and tolerability for chronic pain, and encouraging efficacy data in rodents with inhibitors of the neuronal glycine transporter‐2 (GlyT2) is encouraging.
COVID Moonshot: Open Science Discovery of SARS-CoV-2 Main Protease Inhibitors by Combining Crowdsourcing, High-Throughput Experiments, Computational Simulations, and Machine Learning
Hagit Achdout,A. Aimon,Elad Bar-David,Haim Barr,Amir Ben-Shmuel,Jim Bennett,Melissa L Bobby,Juliane Brun,Sarma Bvnbs,Mark Daniel Calmiano,Anna Carbery,Emma Cattermole,John D. Chodera,Austin Clyde,Joseph E. Coffland,Galit Cohen,Jason C. Cole,Alessandro Contini,Lisa Cox,Milan Cvitkovic,Alex Dias,Alice Douangamath,Shirly Duberstein,Tim Dudgeon,Louise Dunnett,Peter K. Eastman,Noam Erez,Michael Fairhead,D. Fearon,Oleg Fedorov,Matteo P. Ferla,Holly Foster,Richard Foster,Ronen Gabizon,P. Gehrtz,Carina Gileadi,Charline Giroud,William G. Glass,Robert C. Glen,Itai Glinert,Marian V. Gorichko,T.J. Gorrie-Stone,Edward J Griffen,Jag Paul Heer,Michelle L. Hill,Sam Horrell,Matthew F. D. Hurley,Tomer Israely,Andrew Jajack,Eric Jnoff,Tobias John,Anastassia L. Kantsadi,Peter W. Kenny,J. L. Kiappes,Lizbe Koekemoer,Boris Kovar,T. Krojer,Alpha A. Lee,Bruce A. Lefker,Haim Levy,Nir London,Petra Lukacik,Hannah E. Bruce Macdonald,Beth MacLean,Tika R. Malla,Tatiana Matviiuk,Willam McCorkindale,Sharon Melamed,Oleg M. Michurin,Halina Mikolajek,Aaron Morris,Garrett M. Morris,Melody Jane Morwitzer,Demetri Moustakas,Jose Brandao Neto,Vladas Oleinikovas,Gijs J. Overheul,David Owen,Ruby Pai,Jin Pan,Nir Paran,Benjamin Ian Perry,Maneesh Pingle,Jakir Pinjari,Boaz Politi,Ailsa Powell,Vladimir Psenak,Reut Puni,Victor L. Rangel,Rambabu N. Reddi,St Patrick Reid,Efrat Resnick,Matthew C. Robinson,Ralph P. Robinson,Dominic Rufa,Christopher J. Schofield,Aarif Shaikh,Jiye Shi,Khriesto A. Shurrush,Assa Sittner,R. Skyner,Adam Smalley,Mihaela D. Smilova,John Spencer,Claire Strain-Damerell,Vishwanath Swamy,Hadas Tamir,Rachael Tennant,Andrew Thompson,Warren Thompson,Susana Tomasio,Anthony Tumber,Ioannis Vakonakis,Ronald P. van Rij,Finny S. Varghese,Mariana Vaschetto,Einat B. Vitner,Vincent A. Voelz,Annette von Delft,Frank von Delft,Martin Walsh,Walter Ward,Charlie Weatherall,Shay Weiss,Conor Francis Wild,Matthew Wittmann,Nathan Wright,Yfat Yahalom-Ronen,Daniel Zaidmann,Hadeer Zidane,Nicole Zitzmann +130 more
TL;DR: This manuscript describes the methodologies leading to both covalent and non-covalent inhibitors displaying protease IC50 values under 150 nM and viral inhibition under 5 uM in multiple different viral replication assays.