T. Fukami

发表

Effect of P-glycoprotein-mediated efflux on cerebrospinal fluid/plasma concentration ratio.

Masahiko Sato, T. Ohe, Sachiko Tanaka, 2003, Drug metabolism and disposition: the biological fate of chemicals.

Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists.

H. Iwaasa, S. Sakuraba, A. Kanatani, 2009, Bioorganic & medicinal chemistry letters.

Role of the Y1 receptor in the regulation of neuropeptide Y-mediated feeding: comparison of wild-type, Y1 receptor-deficient, and Y5 receptor-deficient mice.

N. Morin, D. Macneil, Y. Saga, 2000, Endocrinology.

L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist.

D. Macneil, H. Iwaasa, L. V. D. van der Ploeg, 2000, Biochemical and biophysical research communications.

Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists.

M. Hirose, N. Fujino, A. Kanatani, 2003, Journal of medicinal chemistry.

Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788.

T. Nagase, S. Ozaki, T. Fukami, 1994, Proceedings of the National Academy of Sciences of the United States of America.

NPY-induced feeding involves the action of a Y1-like receptor in rodents

D. Macneil, H. Iwaasa, A. Kanatani, 1998, Regulatory Peptides.

The novel neuropeptide Y Y(1) receptor antagonist J-104870: a potent feeding suppressant with oral bioavailability.

T. Tanaka, M. Hata, A. Kanatani, 1999, Biochemical and biophysical research communications.

A typical Y1 receptor regulates feeding behaviors: effects of a potent and selective Y1 antagonist, J-115814.

T. Ohe, M. Hata, A. Kanatani, 2001, Molecular pharmacology.

Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor.

T. Fukami, M. Yano, T. Saeki, 1992, Life sciences.

Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors.

T. Umehara, M. Shirouzu, H. Seimiya, 2019, Journal of medicinal chemistry.

Novel tankyrase inhibitors suppress TDP-43 aggregate formation.

A. Kakita, H. Seimiya, K. Wakabayashi, 2020, Biochemical and biophysical research communications.

Neuropeptide Y receptors as targets of obesity treatment

D. Macneil, A. Kanatani, T. Fukami, 2006 .

(−)-Ternatin inhibits adipogenesis and lipid metabolism in 3T3-L1 cells

A. Kanatani, T. Fukami, D. Uemura, 2009, Peptides.

N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.

H. Iwaasa, M. Hirose, M. Hata, 2003, Bioorganic & medicinal chemistry letters.

A Pyrrolo-Pyrimidine Derivative Targets Human Primary AML Stem Cells in Vivo

Satoshi Tanaka, Shigeyuki Yokoyama, Hiroshi Kajita, 2013, Science Translational Medicine.

Carrier-mediated active transport of BQ-123, a peptidic endothelin antagonist, into rat hepatocytes.

T. Nakamura, Y. Sawasaki, A. Hisaka, 1996, The Journal of pharmacology and experimental therapeutics.

The ubiquinone synthesis pathway is a promising drug target for Chagas disease

M. Shirouzu, T. Honma, K. Kita, 2021, PloS one.

Synergistic interaction between neuropeptide Y1 and Y5 receptor pathways in regulation of energy homeostasis.

H. Iwaasa, H. Matsushita, A. Kanatani, 2009, European journal of pharmacology.

Characterization of neuropeptide Y (NPY) Y5 receptor-mediated obesity in mice: chronic intracerebroventricular infusion of D-Trp(34)NPY.

N. Morin, D. Macneil, H. Iwaasa, 2003, Endocrinology.

Analysis of responses to endothelins in isolated porcine blood vessels by using a novel endothelin antagonist, BQ-153.

T. Fukami, M. Yano, Y. Ohta, 1992, Life sciences.

Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.

H. Iwaasa, M. Ando, T. Ohe, 2009, Journal of medicinal chemistry.

Effects of a Novel Y5 Antagonist in Obese Mice: Combination With Food Restriction or Sibutramine

D. Macneil, H. Iwaasa, H. Matsushita, 2008, Obesity.

Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.

T. Hayama, T. Fukami, T. Saeki, 1995, Journal of medicinal chemistry.

A convenient synthetic method of a 5,7-diarylcyclopenteno-[1,2-b]pyridine-6-carboxylate: a key intermediate for potent endothelin receptor antagonists.

T. Hayama, T. Fukami, A. Naya, 2002, Bioorganic & Medicinal Chemistry.

Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity

T. Fukami, M. Yano, M. Ihara, 1995 .

Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon

T. Hayama, K. Matsuyama, T. Fukami, 1994 .

Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.

R. Yoshimoto, T. Fukami, Y. Mitobe, 2008, Journal of medicinal chemistry.

Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults.

Bengt Långström, Sandra M. Sanabria-Bohórquez, Steven B Heymsfield, 2006, Cell metabolism.

Discovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist.

H. Iwaasa, M. Ando, M. Ishikawa, 2009, Bioorganic & medicinal chemistry.

Identification of positron emission tomography ligands for NPY Y5 receptors in the brain.

H. Iwaasa, T. Ohe, A. Kanatani, 2009, Bioorganic & medicinal chemistry letters.

Discovery of pyridone-containing imidazolines as potent and selective inhibitors of neuropeptide Y Y5 receptor.

H. Iwaasa, H. Matsushita, M. Ando, 2009, Bioorganic & medicinal chemistry.

Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives.

H. Iwaasa, K. Matsuda, M. Ishikawa, 2008, Bioorganic & medicinal chemistry letters.

A Pair-Feeding Study Reveals That a Y5 Antagonist Causes Weight Loss in Diet-Induced Obese Mice by Modulating Food Intake and Energy Expenditure

D. Macneil, H. Iwaasa, L. V. D. van der Ploeg, 2007, Molecular Pharmacology.

A neuropeptide Y Y5 antagonist selectively ameliorates body weight gain and associated parameters in diet-induced obese mice.

D. Macneil, H. Iwaasa, L. V. D. van der Ploeg, 2006, Proceedings of the National Academy of Sciences of the United States of America.

[Development of anorectic NPY antagonists: possible roles of Y1 and Y5 receptors in feeding regulation].

D. Macneil, H. Iwaasa, A. Kanatani, 2006, Nihon yakurigaku zasshi. Folia pharmacologica Japonica.

Blockade of body weight gain and plasma corticosterone levels in Zucker fatty rats using an orally active neuropeptide Y Y1 antagonist

Keiko Watanabe, M. Hata, A. Kanatani, 2002, British journal of pharmacology.

A potent neuropeptide Y antagonist, 1229U91, suppressed spontaneous food intake in Zucker fatty rats.

T. Tanaka, A. Kanatani, T. Fukami, 1998, The American journal of physiology.

Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications.

T. Hayama, T. Fukami, M. Yano, 1992, Journal of medicinal chemistry.

Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.

S. Ozaki, T. Fukami, M. Yano, 1996, Journal of medicinal chemistry.

Endothelin antagonistic peptide derivatives with high selectivity for ETA receptors

T. Hayama, T. Fukami, M. Yano, 1993 .

Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.

H. Iwaasa, M. Ando, A. Kanatani, 2009, Bioorganic & medicinal chemistry letters.

(9S)-9-(2-hydroxy-4,4-dimethyl-6-oxo-1-cyclohexen-1-yl)-3,3-dimethyl-2,3,4,9-tetrahydro-1H-xanthen-1-one, a selective and orally active neuropeptide Y Y5 receptor antagonist.

H. Iwaasa, M. Ando, T. Ohe, 2008, Journal of medicinal chemistry.

Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.

H. Iwaasa, M. Ishikawa, A. Kanatani, 2009, Bioorganic & medicinal chemistry letters.

Endothelin Receptor Antagonists with Various Subtype-Specificity: Their Discovery and Use as Pharmacological Tools

T. Hayama, S. Ozaki, T. Fukami, 1995, European Journal of Medicinal Chemistry.

Practical synthesis of a cyclic pentapeptide in solution: large-scale preparation of a representative ETA-selective antagonist, BQ-123Na

T. Fukami, A. Naya, K. Ishikawa, 1994 .

Novel 4-substituted pyridine derivatives: Practical derivatization and biological profiles of reversible inhibitors

T. Fukami, K. Ishikawa, T. Nagase, 1997 .

Overcoming mutational complexity in acute myeloid leukemia by inhibition of critical pathways

A. Letai, O. Ohara, Kaori Sato, 2017, Science Translational Medicine.

Combined inhibition of XIAP and BCL2 drives maximal therapeutic efficacy in genetically diverse aggressive acute myeloid leukemia

Jordan A. Ramilowski, Y. Okazaki, P. Vyas, 2021, Nature Cancer.

Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R

Christopher P. Austin, Masahiko Ito, Alka Bansal, 2001, Proceedings of the National Academy of Sciences of the United States of America.

RK‐287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model

H. Seimiya, Minoru Yoshida, Yoko Yashiroda, 2018, Cancer science.

Design and Discovery of an Orally Efficacious Spiroindolinone-based Tankyrase Inhibitor for the Treatment of Colon Cancer.

T. Umehara, M. Shirouzu, H. Seimiya, 2020, Journal of medicinal chemistry.

Convenient synthesis of 2-alkylamino-6-carboxy-5,7-diarylcyclopenteno[1,2-b]pyridines via direct acylamination with imidoyl chlorides

T. Hayama, T. Fukami, T. Nishimura, 2005 .

Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.

Kouta Masutani, M. Kameda, H. Matsushita, 2009, Bioorganic & medicinal chemistry letters.

Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.

H. Iwaasa, S. Sakuraba, A. Kanatani, 2009, Bioorganic & medicinal chemistry letters.

Endothelin ETB receptors couple to two distinct signaling pathways in porcine kidney epithelial LLC-PK1 cells.

S. Ozaki, T. Fukami, M. Yano, 1994, The Journal of pharmacology and experimental therapeutics.

Aryl urea derivatives of spiropiperidines as NPY Y5 receptor antagonists.

H. Iwaasa, T. Ohe, A. Kanatani, 2009, Bioorganic & medicinal chemistry letters.

Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists.

D. Macneil, H. Iwaasa, A. Kanatani, 2009, Bioorganic & Medicinal Chemistry Letters.

Novel orally active NPY Y5 receptor antagonists: Synthesis and structure-activity relationship of spiroindoline class compounds.

H. Iwaasa, A. Kanatani, T. Fukami, 2009, Bioorganic & medicinal chemistry.

Syntheses and structure-activity relationships of novel, potent, and selective trans-2-[3-oxospiro[isobenzofuran-1(3H),1'-cyclohexan]-4'-yl]benzimidazole NPY Y5 receptor antagonists.

H. Iwaasa, K. Matsuda, M. Ishikawa, 2008, Bioorganic & medicinal chemistry letters.

Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives.

H. Iwaasa, M. Hirose, A. Kanatani, 2006, Bioorganic & medicinal chemistry.

Different binding sites for the neuropeptide Y Y1 antagonists 1229U91 and J-104870 on human Y1 receptors

H. Iwaasa, T. Iwama, A. Kanatani, 2001, Peptides.

In Vitro Biological Profile of a Highly Potent Novel Endothelin (ET) Antagonist BQ‐123 Selective for the ETA Receptor

T. Fukami, M. Yano, T. Saeki, 1992, Journal of cardiovascular pharmacology.

[3H]BQ-123, a highly specific and reversible radioligand for the endothelin ETA receptor subtype.

S. Ozaki, T. Fukami, M. Yano, 1995, European journal of pharmacology.

rapid communication A potent neuropeptide Y antagonist , 1229 U 91 , suppressed spontaneous food intake in Zucker fatty rats

A. Kanatani, T. Fukami, A. Ishihara, 1998 .

A potent neuropeptide Y antagonist, 1229U91, suppressed spontaneous food intake in Zucker fatty rats.

A. Kanatani, T. Fukami, A. Ishihara, 1998, American journal of physiology. Regulatory, integrative and comparative physiology.

Biochemical and pharmacological profile of a potent and selective endothelin

S. Ozaki, T. Fukami, M. Yano, 2022 .

Radioimmunoassay for clebopride, a new benzamide drug with antidopaminergic activity.

T. Fukami, M. Yano, K. Ishikawa, 1984, Chemical & pharmaceutical bulletin.

Effects of a Novel Y5 Antagonist in Obese Mice: Combination With Food Restriction

D. Macneil, A. Kanatani, T. Fukami, 2008 .

H. Iwaasa, M. Ando, T. Ohe, 2009, Journal of medicinal chemistry.

Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.

R. Yoshimoto, T. Fukami, Sayaka Ito, 2008, Journal of medicinal chemistry.