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Record W2763796604 · doi:10.1186/s40360-017-0170-5

Abstracts from the 8th International Conference on cGMP Generators, Effectors and Therapeutic Implications

2017· article· en· W2763796604 on OpenAlexaff
G. Todd Milne, Peter Sandner, Kathleen Lincoln, Paul C. Harrison, Hongxing Chen, Hong Wang, Holly D. Clifford, Hu Sheng Qian, Diane Wong, Chris Sarko, Ryan M. Fryer, Jeremy G. Richman, Glenn A. Reinhart, Carine Boustany, Steven S. Pullen, Henriette Andresen, Alessandro Cataliotti, Finn Olav Levy, Robert Łukowski, Sandra Frankenreiter, Timothy D. Calamaras, R. Baumgärtner, Angela McLaughlin, Mark Aronovitz, Wendy Baur, Guangrong Wang, Navin K. Kapur, Richard H. Karas, Robert M. Blanton, Stefan W. Hell, Scott A. Waldman, Jieru E. Lin, Francheska Colón‐González, Gilbert W. Kim, Erik Blomain, Dante J. Merlino, Adam E. Snook, Jeanette Erdmann, Jana Wobst, Thorsten Kessler, Heribert Schunkert, Ulrich Walter, Oliver Pagel, Elena Walter, Stepan Gambaryan, Albert Smolenski, Kerstin Jurk, René P. Zahedi, James R. Klinger, Raymond L. Benza, Paul A. Corris, David Langleben, Robert Naeije, Gérald Simonneau, Christian Meier, Pablo Colorado, Mi Kyung Chang, Dennis Busse, Marius M. Hoeper, Jaime L. Masferrer, Sarah Jacobson, Renee Sarno, Sylvie G. Bernier, Ping Zhang, Roger Flores‐Costa, Mark G. Currie, K. Hall, Dorit Möhrle, Katrin Reimann, Steffen Wolter, Markus Wolters, Evanthia Mergia, Nicole Eichert, H Geisler, Peter Ruth, Andreas Friebe, Robert Feil, Ulrike Zimmermann, Marlies Knipper, Lukas Rüttiger, Yasutake Tanaka, Atsuko Okamoto, Motofumi Kumazoe, Takeshi Tokudome, Koichi Miura, Jun Hino, Mikiya Miyazato, Kenji Kangawa, Vikas Kapil, Amrita Ahluwalia, Nazareno Paolocci, Philip Eaton, James C. Campbell, Philipp Henning, Eugen Franz, Banumathi Sankaran, Friedrich W. Herberg, Choel Kim, Matthias Wittwer, Luo Qi, Ville R. I. Kaila, Sonja A. Dames, Andrew B. Tobin, Mahmood M. Alam, Olena Rudyk, Susanne Krasemann, Kristin Hartmann, Oleksandra Prysyazhna, Min Zhang, Lan Zhao, Astrid Weiß, Ralph T. Schermuly, Amie J. Moyes, Sandy M. Chu, Reshma S. Baliga, Adrian J. Hobbs, Stylianos Michalakis, Regine Mühlfriedel, Christian Schön, Dominik Fischer, Barbara Wilhelm, Ditta Zobor, Susanne Kohl, Tobias Peters, Eberhart Zrenner, Karl Ulrich Bartz‐Schmidt, Marius Ueffing, Bernd Wissinger, Mathias W. Seeliger, Martin Biel, Mark J. Ranek, Kristen M. Kokkonen-Simon, Dong I. Lee, Ronald J. Holewinski, Vineet Agrawal, Cornelia Virus, Donté A. Stevens, Masayuki Sasaki, Huaqun Zhang, Mathew M. Mannion, Peter P. Rainer, Richard C. Page, Jonathan C. Schisler, Jennifer E. Van Eyk, Monte S. Willis, David A. Kass, Michael Russwurm, Jan Giesen, Corina Russwurm, Ernst‐Martin Füchtbauer, Nadja I. Bork, Luís Agulló, Martin Floor, Ornella Manfra, Gaia Calamera, Nicoletta C. Surdo, Silja Meier, Alexander Froese, Viacheslav O. Nikolaev, Kjetil Wessel Andressen, Annemarie Aue, Fabian Schwiering, Dieter Groneberg, Gzona Bajraktari‐Sylejmani, Jürgen Burhenne, Walter E. Haefeli, Johanna Weiß, Katharina Beck, Barbara Voußen, Alexander D. Vincent, Jan D. Huizinga, Fabíola Z. Mónica, Edward Seto, Ferid Murad, Ka Bian, Joseph R. Burgoyne, Daniel A. Richards, Marianne Bjørnerem, Andrea Hembre Ulsund, Jeong Joo Kim, Sonia Donzelli, Mara Göetz, Kjestine Schmidt, Κωνσταντίνα Σταθοπούλου, Jenna Scotcher, Christian Dees, Hariharan Subramanian, Elke Butt, Alisa Kamynina, S. Bruce King, Cor de Witt, Lars I. Leichert, Friederike Cuello, Hyazinth Dobrowinski, Moritz Lehners, Michael Paolillo Hannes Schmidt, Susanne Feil, Lai Wen, Martin Thunemann, Marcus Olbrich, Harald F. Langer, Meinrad Gawaz, Cor de Wit, Daniela Bertinetti, Friedrich Grimminger, Ekkehard Grünig, Yigao Huang, Pavel Jansa, Zhi‐Cheng Jing, D Kilpatrick, Stephan Rosenkranz, Flavia Menezes, Arno Fritsch, Sylvia Nikkho, Reiner Frey, Marc Humbert, Manuela Harloff, Jörg Reinders, Jens Schlossmann, Joon Jung, Jessica A. Wales, Cheng‐Yu Chen, Linda Breci, A. Weichsel, Robert Solinga, Paul A. Renhowe, W.R. Montfort, Liying Qin, Ying‐Ju Sung, Darren E. Casteel, Alexander Kollau, Andrea Neubauer, Astrid Schrammel, Bernd Mayer, Mika Takai, Chieri Takeuchi, Mai Kadomatsu, Shun Hiroi, Kanako Takamatsu, Hirofumi Tachibana, Marissa Opelt, Emrah Eroğlu, Markus Waldeck‐Weiermair, Doris Koesling, Roland Malli, Wolfgang F. Graier, John Fassett, Selene J. Sollie, Maria Hernandez-Valladares, Frode S. Berven, Takashi Nojiri, Miki Arai, Yutaka Suzuki, Meinoshin Okumura, Shinpei Kawaoka, Stefanie Peters, Hannes Schmidt, Selin Kenet, Sarah Helena Nies, Katharina Frank, Fritz G. Rathjen, Olga N. Petrova, Isabelle Lamarre, Michel Négrerie, Jerid W. Robinson, Jeremy R. Egbert, Julia Davydova, Laurinda A. Jaffe, Lincoln R. Potter, Nicholas Blixt, Leia C. Shuhaibar, Gordon L. Warren, Kim C. Mansky, Simone Romoli, T. Bauch, Karoline Dröbner, Frank Eitner, Mihály Ruppert, Tamás Radovits, Sevil Korkmaz‐Icöz, Shiliang Li, Péter Hegedűs, Sivakanan Loganathan, Balázs Tamás Németh, Attila Oláh, Csaba Mátyás, Kálmán Benke, Béla Merkely, Matthias Karck, Gábor Szabó, U. Scheib, Matthias Broser, Shatanik Mukherjee, Katja Stehfest, Christine E. Gee, Heinz G. Körschen, Thomas G. Oertner, Peter Hegemann, Deborah M. Dickey, Alexandre Dumoulin, Ralf Kühn, Sophie Schobesberger, Peter Wright, Claire Poulet, Catherine Mansfield, Siân E. Harding, Julia Gorelik, Gerald Wölkart, Antonius C.F. Gorren, Gerburg K. Schwaerzer, Nancy D. Dalton, Yusu Gu, Shunhui Zhuang, Dianna M. Milewicz, Kirk L. Peterson, Renate B. Pilz, Aikaterini I. Argyriou, Garyfalia Makrynitsa, Ioannis I. Alexandropoulos, Ανδριάνα Σταμοπούλου, Marina Bantzi, Athanassios Giannis, Stavros Topouzis, Andreas Papapetropoulos, Georgios A. Spyroulias, Dennis J. Stuehr, Arnab Ghosh, Yue Dai, Saurav Misra, Boris Tchernychev, Inmaculada Silos‐Santiago, Gerhard Hannig, Vu Thao-Vi Dao, Martin Deile, Pavel I. Nedvetsky, Andreas Güldner, César Ibarra‐Alvarado, Axel Gödecke, Harald Schmidt, Angelos Vachaviolos, Andrea Gerling, Stefan Lutz, Hans-Ulrich Häring, Marcel A. Krüger, Bernd J. Pichler, Michael J. Shipston, Sara Vandenwijngaert, Clara D. Ledsky, Obiajulu Agha, Dongjian Hu, Ibrahim J. Domian, Emmanuel S. Buys, Christopher Newton‐Cheh, Donald B. Bloch, Nadine Mauro, Jonas Keppler, Wilson A. Ferreira, Hanan Chweih, Pâmela L. Brito, Camila Bononi Almeida, Carla Fernanda Franco Penteado, Sara S. O. Saad, Fernando Ferreira Costa, Paul S. Frenette, Damian Brockschnieder, Johannes‐Peter Stasch, Nicola Conran, Daniel P. Zimmer, Jenny Tobin, Courtney Shea, Kimberly Long, Kim San Tang, Peter Germano, James Wakefield, Ali R. Banijamali, G-Yoon Jamie Im, Albert T. Profy

Bibliographic record

VenueBMC Pharmacology and Toxicology · 2017
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicPhosphodiesterase function and regulation
Canadian institutionsMcGill UniversityMcMaster UniversityPopulation Health Research InstituteJewish General Hospital
FundersDeutsches Zentrum für LungenforschungUniversité Paris-SaclayDeutsche ForschungsgemeinschaftBritish Heart Foundation
KeywordsEffectorComputer scienceBiologyCell biology

Abstract

fetched live from OpenAlex

The nitric oxide (NO)-soluble guanylate cyclase (sGC)-cyclic guanosine monophosphate (cGMP) signalling pathway plays a fundamental role in modulating diverse physiological processes including blood flow, fibrosis, inflammation, and metabolism. sGC stimulators are small-molecule, heme-dependent agonists of sGC that synergize with and enhance endogenous NO signaling. As such, sGC stimulators may provide therapeutic benefits both in diseases associated with impaired NO signaling and in diseases where stimulation of this pathway will restore functional homeostasis. Data from our recent preclinical studies add to the growing body of evidence that sGC stimulators have direct effects on systemic and vascular inflammation, fibrosis, and metabolism. Ironwood is developing IW-1973 and IW-1701 as oral, once-daily sGC stimulators for both cardiovascular and non-cardiovascular systemic disease indications. Phase 1 studies in healthy human subjects demonstrated clear evidence of target engagement, attractive pharmacokinetic properties, and predicted hemodynamic effects, at well-tolerated doses. Phase 2 studies are currently ongoing in patients with achalasia, an esophageal motility disorder, and in patients with diabetes and hypertension. Preclinical characterization of IW-1973 and IW-1701 support the broad therapeutic potential and multi-faceted pharmacology of these compounds. Based on preclinical studies, IW-1973 has extensive distribution into organs including liver, heart, kidney, and lung, which may maximize effects on target organs while limiting systemic hemodynamic effects. The pharmacokinetic profile of IW-1701 has a narrow peak-to-trough ratio, which may provide more consistent pharmacological effect throughout the dosing interval. Ironwood is also developing IW-6463, a novel, CNS-penetrant sGC stimulator that shows target engagement and effects on regional blood flow in the brain. Preclinical data suggest that IW-6463 may be useful in treating CNS disorders including vascular dementia and Alzheimer's disease. We believe that sGC stimulation, alone or in combination with other mechanisms, may afford therapeutic benefit in multiple diseases. Furthermore, there may be an opportunity to provide targeted treatments by selecting compounds that are well-suited for specific diseases based on pharmacological profile, tissue distribution, pharmacokinetics, and route of administration.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: none
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.806
Threshold uncertainty score0.337

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.039
GPT teacher head0.334
Teacher spread0.295 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations16
Published2017
Admission routes1
Has abstractyes

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Same venueBMC Pharmacology and ToxicologySame topicPhosphodiesterase function and regulationFrench-language works237,207