Publications by authors named "Jason Yano"

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Structure-based design of a novel series of cholesterol 24-hydroxylase (CH24H) inhibitors bearing 1,3-oxazole as a heme-iron binding group.
Yoshiteru Ito, Tomoaki Hasui, Eiji Kimura, Izumi Nomura, Hiromi Fukuda, Jason Yano

Bioorg Med Chem· October 2025

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Correction: Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Jingjing Jiang, Lingyan Jiang, Benjamin J Maldonato, Yingyun Wang, Matthew Holderfield, Jason K Yano

Cancer Discov· October 2025

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Design and identification of brain-penetrant, potent, and selective 1,3-oxazole-based cholesterol 24-hydroxylase (CH24H) inhibitors.
Yoshiteru Ito, Eiji Kimura, Izumi Nomura, Etsurou Watanabe, Jason Yano

Bioorg Med Chem· July 2025

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The "three body solution": Structural insights into molecular glues.
Aidan C A Tomlinson, John E Knox, Luc Brunsveld, Christian Ottmann, Jason K Yano

Curr Opin Struct Biol· April 2025

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Analysis of Burkholderia pseudomallei IspF in complex with sulfapyridine, sulfamonomethoxine, ethoxzolamide and acetazolamide.
Dakota Grote, Christopher G Stewart, Drashti G Daraji, Parisa Enayati, Kristina N Braverman, Jason K Yano

Acta Crystallogr F Struct Biol Commun· April 2025

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Discovery of Elironrasib (RMC-6291), a Potent and Orally Bioavailable, RAS(ON) G12C-Selective, Covalent Tricomplex Inhibitor for the Treatment of Patients with RAS G12C-Addicted Cancers.
James Cregg, Kristof Pota, Aidan C A Tomlinson, Jason Yano, Abby Marquez

J Med Chem· March 2025

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Genomic Discovery and Structure-Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors.
Jack R Davison, Michalis Hadjithomas, Stuart P Romeril, Yoon Jong Choi, Keith W Bentley, Jason Yano

J Med Chem· August 2024

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Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Jingjing Jiang, Lingyan Jiang, Benjamin J Maldonato, Yingyun Wang, Matthew Holderfield, Jason K Yano

Cancer Discov· June 2024

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Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
Adrian Hall, Jan Abendroth, Madison J Bolejack, Tom Ceska, Sylvie Dell'Aiera, Jason Yano

ACS Med Chem Lett· July 2022

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Discovery of Novel 3-Piperidinyl Pyridine Derivatives as Highly Potent and Selective Cholesterol 24-Hydroxylase (CH24H) Inhibitors.
Yuichi Kajita, Shuhei Ikeda, Masato Yoshikawa, Hiromi Fukuda, Etsurou Watanabe, Jason Yano

J Med Chem· February 2022

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Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H).
Tatsuki Koike, Masato Yoshikawa, Haruhi Kamisaki Ando, William Farnaby, Toshiya Nishi, Jason Yano

J Med Chem· August 2021

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Soticlestat, a novel cholesterol 24-hydroxylase inhibitor shows a therapeutic potential for neural hyperexcitation in mice.
Toshiya Nishi, Shinichi Kondo, Maki Miyamoto, Sayuri Watanabe, Shigeo Hasegawa, Jason Yano

Sci Rep· October 2020

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Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
Katsuji Aikawa, Moriteru Asano, Koji Ono, Noriyuki Habuka, Jason Yano

Bioorg Med Chem· July 2017

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Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.
Moriteru Asano, Takenori Hitaka, Takashi Imada, Masami Yamada, Megumi Morimoto, Jason Yano

Bioorg Med Chem Lett· May 2017

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Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).
Betty Lam, Yasuyoshi Arikawa, Joshua Cramlett, Qing Dong, Ron de Jong, Jason Yano

Bioorg Med Chem Lett· December 2016

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High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
Ankita Srivastava, Jason Yano, Yoshihiko Hirozane, Georgia Kefala, Franz Gruswitz

Nature· September 2014

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Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Masanori Okaniwa, Masaaki Hirose, Takeo Arita, Masato Yabuki, Akito Nakamura, Jason Yano

J Med Chem· August 2013

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Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Masaaki Hirose, Masanori Okaniwa, Tohru Miyazaki, Takashi Imada, Tomohiro Ohashi, Jason Yano

Bioorg Med Chem· September 2012

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Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.
Masanori Okaniwa, Masaaki Hirose, Takashi Imada, Tomohiro Ohashi, Youko Hayashi, Jason Yano

J Med Chem· April 2012

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Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Tomoyasu Ishikawa, Masaki Seto, Hiroshi Banno, Youichi Kawakita, Mami Oorui, Jason Yano

J Med Chem· December 2011

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Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.
Hironobu Maezaki, Yoshihiro Banno, Yasufumi Miyamoto, Yusuke Moritoh, Tomoko Asakawa, Jason Yano

Bioorg Med Chem· August 2011

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Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.
Yoshihiro Banno, Yasufumi Miyamoto, Mitsuru Sasaki, Satoru Oi, Tomoko Asakawa, Jason Yano

Bioorg Med Chem· August 2011

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Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.
Kathleen Aertgeerts, Robert Skene, Jason Yano, Bi-Ching Sang, Hua Zou

J Biol Chem· May 2011

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Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Alexandra E Gould, Ruth Adams, Sharmila Adhikari, Kathleen Aertgeerts, Roushan Afroze, Jason Yano

J Med Chem· March 2011

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Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor.
Yasufumi Miyamoto, Yoshihiro Banno, Tohru Yamashita, Tatsuhiko Fujimoto, Satoru Oi, Jason Yano

J Med Chem· February 2011

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