Publications by authors named "BiChing Sang"

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Structure-Based Design, Synthesis, and Biological Evaluation of Imidazo[4,5-b]Pyridin-2-one-Based p38 MAP Kinase Inhibitors: Part 2.
Akira Kaieda, Masashi Takahashi, Hiromi Fukuda, Rei Okamoto, Shinji Morimoto, Bi-Ching Sang

ChemMedChem· December 2019

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Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists.
Ayumu Sato, Yoshiyuki Fukase, Mitsunori Kono, Atsuko Ochida, Tsuneo Oda, Bi-Ching Sang

ChemMedChem· November 2019

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Cholesterol Unbound RORγt Protein Enables a Sensitive Inverse Agonist Screening.
Ryokichi Koyama, Yasunori Fukuda, Yusuke Kamada, Hideyuki Nakagawa, Darbi Witmer, Bi-Ching Sang

Assay Drug Dev Technol· October 2019

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Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
Jun Fujimoto, Osamu Kurasawa, Terufumi Takagi, Xin Liu, Hiroshi Banno, Bi-Ching Sang

ACS Med Chem Lett· October 2019

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Structure-Based Design, Synthesis, and Biological Evaluation of Imidazo[4,5-b]pyridin-2-one-Based p38 MAP Kinase Inhibitors: Part 1.
Akira Kaieda, Masashi Takahashi, Hiromi Fukuda, Rei Okamoto, Shinji Morimoto, Bi-Ching Sang

ChemMedChem· May 2019

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Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Tomoya Yukawa, Yoshi Nara, Mitsunori Kono, Ayumu Sato, Tsuneo Oda, BiChing Sang

J Med Chem· February 2019

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Biochemical Properties of TAK-828F, a Potent and Selective Retinoid-Related Orphan Receptor Gamma t Inverse Agonist.
Hideyuki Nakagawa, Ryoukichi Koyama, Yusuke Kamada, Atsuko Ochida, Mitsunori Kono, Bi-Ching Sang

Pharmacology· December 2018

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Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Mitsunori Kono, Atsuko Ochida, Tsuneo Oda, Takashi Imada, Yoshihiro Banno, Bi-Ching Sang

J Med Chem· April 2018

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Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors.
Akira Kaieda, Masashi Takahashi, Takafumi Takai, Masayuki Goto, Takahiro Miyazaki, Bi-Ching Sang

Bioorg Med Chem· February 2018

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Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Yoshiyuki Fukase, Ayumu Sato, Yoshihide Tomata, Atsuko Ochida, Mitsunori Kono, Bi-Ching Sang

Bioorg Med Chem· February 2018

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Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Junya Shirai, Yoshihide Tomata, Mitsunori Kono, Atsuko Ochida, Yoshiyuki Fukase, BiChing Sang

Bioorg Med Chem· January 2018

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Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
Tomohiro Okawa, Yoshio Aramaki, Mitsuo Yamamoto, Toshitake Kobayashi, Shoji Fukumoto, Bi-Ching Sang

J Med Chem· August 2017

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Structure of Human GIVD Cytosolic Phospholipase A2 Reveals Insights into Substrate Recognition.
Hui Wang, Michael G Klein, Gyorgy Snell, Weston Lane, Hua Zou, Bi-Ching Sang

J Mol Biol· July 2016

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Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKCθ inhibitors.
Taisuke Katoh, Takafumi Takai, Takafumi Yukawa, Tetsuya Tsukamoto, Etsurou Watanabe, Bi-Ching Sang

Bioorg Med Chem· June 2016

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Crystal structure of human stearoyl-coenzyme A desaturase in complex with substrate.
Hui Wang, Michael G Klein, Hua Zou, Weston Lane, Gyorgy Snell, Bi-Ching Sang

Nat Struct Mol Biol· July 2015

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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, Bi-Ching Sang

J Med Chem· August 2013

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Biological characterization of TAK-901, an investigational, novel, multitargeted Aurora B kinase inhibitor.
Pamela Farrell, Lihong Shi, Jennifer Matuszkiewicz, Deepika Balakrishna, Takashi Hoshino, BiChing Sang

Mol Cancer Ther· April 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, Bi-Ching Sang

Bioorg Med Chem· September 2012

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Structure-activity relationships and key structural feature of pyridyloxybenzene-acylsulfonamides as new, potent, and selective peroxisome proliferator-activated receptor (PPAR) γ Agonists.
Kentaro Rikimaru, Takeshi Wakabayashi, Hidenori Abe, Taisuke Tawaraishi, Hiroshi Imoto, Bi-Ching Sang

Bioorg Med Chem· May 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, Bi-Ching Sang

J Med Chem· April 2012

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A new class of non-thiazolidinedione, non-carboxylic-acid-based highly selective peroxisome proliferator-activated receptor (PPAR) γ agonists: design and synthesis of benzylpyrazole acylsulfonamides.
Kentaro Rikimaru, Takeshi Wakabayashi, Hidenori Abe, Hiroshi Imoto, Tsuyoshi Maekawa, Bi-Ching Sang

Bioorg Med Chem· January 2012

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Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors.
Tohru Yamashita, Makoto Kamata, Satoshi Endo, Mitsuo Yamamoto, Keiko Kakegawa, Biching Sang

Bioorg Med Chem Lett· November 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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Cell-based assay for screening 11beta-hydroxysteroid dehydrogenase inhibitors using liquid chromatography/tandem mass spectrometry detection.
Rongda Xu, Bi-Ching Sang, Marc Navre, Daniel B Kassel

Rapid Commun Mass Spectrom· August 2007

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Characterization of the two catalytic domains in histone deacetylase 6.
Hua Zou, Yiqin Wu, Marc Navre, Bi-Ching Sang

Biochem Biophys Res Commun· March 2006

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