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H. Hirai · SciRah

Researcher profile · Semantic Scholar

H. Hirai

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H. Hirai — researcher profile on SciRah

h-index: 22
Works: 73
Citations: 3,880

Most-cited papers

MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo
H. Hirai, H. Sootome, Y. Nakatsuru, Katsuyoshi Miyama +7 more
2010Molecular Cancer Therapeutics963 citations
Semantic Scholar
Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents
H. Hirai, Y. Iwasawa, Megumu Okada, Tsuyoshi Arai +19 more
2009Molecular Cancer Therapeutics463 citations Open access
Semantic Scholar
TAS-120 overcomes resistance to ATP-competitive FGFR inhibitors in patients with FGFR2 fusion-positive intrahepatic cholangiocarcinoma
L. Goyal, Lei Shi, Le-Ah Y. Liu, Ferran Fece de la Cruz +38 more
2019Cancer Discovery314 citations Open access
Semantic Scholar
MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts
N. Rajeshkumar, E. de Oliveira, Niki A. Ottenhof, J. Watters +7 more
2011Clinical Cancer Research276 citations Open access
Semantic Scholar
MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil
H. Hirai, Tsuyoshi Arai, Megumu Okada, T. Nishibata +9 more
2010Cancer Biology & Therapy266 citations Open access
Semantic Scholar
MK-1775, a Novel Wee1 Kinase Inhibitor, Radiosensitizes p53-defective Human Tumor Cells
K. Bridges, H. Hirai, C. Buser, Colin Brooks +5 more
2011Clinical Cancer Research239 citations Open access
Semantic Scholar
Futibatinib Is a Novel Irreversible FGFR 1–4 Inhibitor That Shows Selective Antitumor Activity against FGFR-Deregulated Tumors
H. Sootome, H. Fujita, Kenjiro Ito, H. Ochiiwa +12 more
2020Cancer Research164 citations Open access
Semantic Scholar
Tax protein of human T-cell leukemia virus type I binds to the ankyrin motifs of inhibitory factor kappa B and induces nuclear translocation of transcription factor NF-kappa B proteins for transcriptional activation.
H. Hirai, Takeshi Suzuki, J. Fujisawa, J. Inoue +1 more
1994Proceedings of the National Academy of Sciences of the United States of America158 citations Open access
Semantic Scholar
Successful Treatment of Animal Models of Rheumatoid Arthritis with Small-Molecule Cyclin-Dependent Kinase Inhibitors1
C. Sekine, T. Sugihara, S. Miyake, H. Hirai +3 more
2008Journal of Immunology102 citations
Semantic Scholar
Enforced cytokinesis without complete nuclear division in embryonic cells depleting the activity of DNA topoisomerase IIα
N. Akimitsu, N. Adachi, H. Hirai, Muktadir S. Hossain +5 more
2003Genes to Cells101 citations Open access
Semantic Scholar
Crystallographic Approach to Identification of Cyclin-dependent Kinase 4 (CDK4)-specific Inhibitors by Using CDK4 Mimic CDK2 Protein*
M. Ikuta, K. Kamata, K. Fukasawa, T. Honma +5 more
2001Journal of Biological Chemistry89 citations Open access
Semantic Scholar
Discovery of gene expression-based pharmacodynamic biomarker for a p53 context-specific anti-tumor drug Wee1 inhibitor
S. Mizuarai, Kazunori Yamanaka, H. Itadani, Tsuyoshi Arai +3 more
2009Molecular Cancer80 citations Open access
Semantic Scholar
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure.
Nobuhiko Kawanishi, T. Sugimoto, J. Shibata, Kaori Nakamura +3 more
2006Bioorganic & Medicinal Chemistry Letters77 citations Open access
Semantic Scholar
Recent advances in the development of selective small molecule inhibitors for cyclin-dependent kinases.
H. Hirai, Nobuhiko Kawanishi, Y. Iwasawa
2005Current Topics in Medicinal Chemistry67 citations
Semantic Scholar
Molecular cloning, expression pattern, and chromosomal localization of human CDKN2D/INK4d, an inhibitor of cyclin D-dependent kinases.
T. Okuda, H. Hirai, Virginia A. Valentine, S. Shurtleff +4 more
1995Genomics61 citations
Semantic Scholar
Preferences for phosphorylation sites in the retinoblastoma protein of D-type cyclin-dependent kinases, Cdk4 and Cdk6, in vitro.
T. Takaki, K. Fukasawa, I. Suzuki-Takahashi, K. Semba +3 more
2005Journal of Biochemistry (Tokyo)54 citations
Semantic Scholar
Discovery of Futibatinib: The First Covalent FGFR Kinase Inhibitor in Clinical Use.
S. Ito, S. Otsuki, Hirokazu Ohsawa, A. Hirano +14 more
2023ACS Medicinal Chemistry Letters38 citations Open access
Semantic Scholar
Abstract A270: TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities.
H. Ochiiwa, H. Fujita, K. Itoh, H. Sootome +7 more
201332 citations
Semantic Scholar
Identification of potent 5-pyrimidinyl-2-aminothiazole CDK4, 6 inhibitors with significant selectivity over CDK1, 2, 5, 7, and 9.
T. Shimamura, J. Shibata, H. Kurihara, Takashi Mita +4 more
2006Bioorganic & Medicinal Chemistry Letters31 citations Open access
Semantic Scholar
Cdk-mediated phosphorylation of pRB regulates HDAC binding in vitro.
T. Takaki, K. Fukasawa, I. Suzuki-Takahashi, H. Hirai
2004Biochemical and Biophysical Research Communications - BBRC31 citations
Semantic Scholar
Phase I study of the irreversible fibroblast growth factor receptor 1–4 inhibitor futibatinib in Japanese patients with advanced solid tumors
T. Doi, K. Shitara, T. Kojima, Y. Kuboki +8 more
2022Cancer Science29 citations Open access
Semantic Scholar
Early clinical efficacy of TAS-120, a covalently bound FGFR inhibitor, in patients with cholangiocarcinoma.
L. Goyal, H. Arkenau, B. Tran, J. Soria +9 more
2017Annals of Oncology23 citations Open access
Semantic Scholar
Expression levels of NF-Y target genes changed by CDKN1B correlate with clinical prognosis in multiple cancers.
Kazunori Yamanaka, S. Mizuarai, Tomohiro Eguchi, H. Itadani +2 more
2009Genomics22 citations Open access
Semantic Scholar
A first-in-human phase 1 and pharmacological study of TAS-119, a novel selective Aurora A kinase inhibitor in patients with advanced solid tumours
D. Robbrecht, Juanita Lopez, E. Calvo, Xiao-Min He +8 more
2020British Journal of Cancer21 citations Open access
Semantic Scholar
TAS-119, a novel selective Aurora A and TRK inhibitor, exhibits antitumor efficacy in preclinical models with deregulated activation of the Myc, β-Catenin, and TRK pathways
A. Miura, H. Sootome, N. Fujita, Takamasa Suzuki +10 more
2021Investigational new drugs19 citations
Semantic Scholar
Potent anti-tumor activity of a macrocycle-quinoxalinone class pan-Cdk inhibitor in vitro and in vivo
H. Hirai, Ikuko Takahashi-Suziki, T. Shimomura, K. Fukasawa +13 more
2011Investigational new drugs18 citations
Semantic Scholar
Aurora A Inhibitor TAS-119 Enhances Antitumor Efficacy of Taxanes In Vitro and In Vivo: Preclinical Studies as Guidance for Clinical Development and Trial Design
H. Sootome, A. Miura, N. Masuko, Takamasa Suzuki +2 more
2020Molecular Cancer Therapeutics14 citations
Semantic Scholar
Biological characterization of 2-aminothiazole-derived Cdk4/6 selective inhibitor in vitro and in vivo
H. Hirai, T. Shimomura, Makiko Kobayashi, Tomohiro Eguchi +14 more
2010Cell Cycle14 citations Open access
Semantic Scholar
Preclinical Evaluation of the FGFR-Family Inhibitor Futibatinib for Pediatric Rhabdomyosarcoma
Jerry T. Wu, A. Cheuk, Kristine A Isanogle, C. Robinson +23 more
2023Cancers13 citations Open access
Semantic Scholar
Expression levels of p18INK4C modify the cellular efficacy of cyclin-dependent kinase inhibitors via regulation of Mcl-1 expression in tumor cell lines
Tomohiro Eguchi, H. Itadani, T. Shimomura, Nobuhiko Kawanishi +2 more
2009Molecular Cancer Therapeutics13 citations Open access
Semantic Scholar
Abstract A271: TAS-120, an irreversible FGFR inhibitor, was effective in tumors harboring FGFR mutations, refractory or resistant to ATP competitive inhibitors .
H. Sootome, Y. Fujioka, A. Miura, H. Fujita +2 more
201312 citations
Semantic Scholar
ICRF‐193, a catalytic inhibitor of DNA topoisomerase II, inhibits re‐entry into the cell division cycle from quiescent state in mammalian cells
Muktadir S. Hossain, N. Akimitsu, T. Takaki, H. Hirai +1 more
2002Genes to Cells12 citations
Semantic Scholar
1241P Phase Ib study of futibatinib plus pembrolizumab in patients with advanced or metastatic solid tumors: Tolerability results and antitumor activity in esophageal carcinoma
K. Muro, K. Kato, K. Chin, K. Nishino +7 more
2022Annals of Oncology7 citations Open access
Semantic Scholar
372PDFirst-in-human (FIH) study of TAS-120, a highly selective covalent oral fibroblast growth factor receptor (FGFR) inhibitor, in patients (pts) with advanced solid tumors
Y. Kuboki, N. Matsubara, H. Bando, K. Shitara +9 more
20177 citations Open access
Semantic Scholar
Abstract 1117: Acquired resistance to ATP-competitive and irreversible FGFR inhibitors (FGFRi's): A library-based approach
H. Sootome, Suzuko Kato, Masanori Kato, H. Hirai
2021Experimental and Molecular Therapeutics6 citations
Semantic Scholar
Abstract LB-092: TAS120, a covalently-binding FGFR inhibitor (FGFRi), overcomes resistance to BGJ398 in patients with FGFR2 fusion positive cholangiocarcinoma
L. Goyal, Le-Ah Y. Liu, J. Lennerz, J. Harding +8 more
2018Experimental and Molecular Therapeutics6 citations
Semantic Scholar
438 Identification of Gene Expression Signature to Predict Anti-tumor Efficacy of MET/VEGFR Inhibitor, TAS-115
H. Itadani, S. Hasako, K. Yonekura, A. Ooyama +5 more
20124 citations
Semantic Scholar
1383P Phase I study of the irreversible FGFR inhibitor futibatinib in Japanese patients with advanced solid tumors: Updated dose expansion results and activity in gastric cancer
Y. Kuboki, K. Shitara, C. Morizane, T. Kojima +7 more
2021Annals of Oncology3 citations Open access
Semantic Scholar
First-in-human phase I and pharmacological study of TAS-119, a selective Aurora A (AurA) kinase inhibitor, in patients (pts) with advanced solid tumors.
D. Robbrecht, F. Eskens, E. Calvo, Xiao-Min He +7 more
2019Journal of Clinical Oncology3 citations Open access
Semantic Scholar
Phase I study of the Aurora A kinase (AurA) inhibitor TAS-119 with paclitaxel (P) in advanced solid tumors.
D. Cardin, Haeseong Park, J. Diamond, A. Drilon +5 more
2019Journal of Clinical Oncology3 citations
Semantic Scholar
380 Identification & Biological Characterization of a Highly Potent, Irreversible Inhibitor of FGFR, TAS-2985
H. Sootome, H. Fujita, H. Ochiiwa, K. Ito +5 more
20123 citations
Semantic Scholar
Cell death induction in resting lymphocytes by pan-Cdk inhibitor, but not by Cdk4/6 selective inhibitor
Makiko Kobayashi, Ikuko Takahashi-Suzuki, T. Shimomura, Y. Iwasawa +1 more
2011Investigational new drugs3 citations
Semantic Scholar
544P Phase I study of the irreversible FGFR inhibitor (i) futibatinib (FBN; TAS-120) in Japanese patients (pts) with advanced (adv) solid tumours
C. Morizane, T. Kojima, Y. Kuboki, H. Bando +6 more
20202 citations Open access
Semantic Scholar
398 TAS-119 a selective inhibitor of Aurora A kinase, potentiates taxane therapy in breast and lung cancer models
Y. Nakatsuru, A. Hashimoto, H. Sootome, K. Ito +5 more
20142 citations
Semantic Scholar
Abstract A272: Intermittent treatment with TAS-120, an irreversible FGFR inhibitor, is effective in tumors harboring a FGFR gene abnormality.
Y. Nakatsuru, H. Ochiiwa, H. Sootome, H. Fujita +7 more
20132 citations
Semantic Scholar
252 TAS-2104, a Highly Potent and Selective Aurora A Inhibitor, Enhanced Antitumor Activity of Taxanes in Vivo
K. Ishihara, N. Masuko, H. Sootome, Takamasa Suzuki +3 more
20122 citations
Semantic Scholar
Abstract A251: MK‐1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions in pancreatic tumor xenografts
N. Rajeshkumar, E. de Oliveira, Niki A. Ottenhof, I. Garrido-Laguna +8 more
20092 citations
Semantic Scholar
Expression levels of p 18 INK 4 C modify the cellular efficacy of cyclin-dependent kinase inhibitors via regulation of Mcl-1 expression in tumor cell lines
Tomohiro Eguchi, H. Itadani, T. Shimomura, Nobuhiko Kawanishi +2 more
20092 citations
Semantic Scholar
Expression levels of p18 INK4C modify the cellular efficacy of cyclin-dependent kinase inhibitors via regulation of Mcl-1 expression in tumor cell lines
Tomohiro Eguchi, H. Itadani, T. Shimomura, Nobuhiko Kawanishi +2 more
20092 citations
Semantic Scholar
Abstract 661: Synergistic antitumor activity of futibatinib, an FGFR1-4 inhibitor, and TAS-117, a selective AKT inhibitor, inFGFR-deregulated cancer models
Junya Iwasaki, T. Kuramoto, Toshiharu Komori, H. Saito +1 more
2020Experimental and Molecular Therapeutics1 citations
Semantic Scholar

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H. Sootome×12
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H. Sootome — researcher profile on SciRah
Hidehito Kotani×10
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Hidehito Kotani — researcher profile on SciRah
Y. Iwasawa×8
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Y. Iwasawa — researcher profile on SciRah
S. Mizuarai×8
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S. Mizuarai — researcher profile on SciRah

Nobuhiko Kawanishi

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Y. Nakatsuru×6

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H. Itadani — researcher profile on SciRah

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K. Fukasawa — researcher profile on SciRah

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T. Sagara — researcher profile on SciRah

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H. Fujita — researcher profile on SciRah

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Tomohiro Eguchi — researcher profile on SciRah