• Discovery of a novel series of medium-sized cyclic enteropeptidase inhibitors.

    Kikuchi, F., Ikeda, Z., Kakegawa, K., Nishikawa, Y., Sasaki, S., Fukuda, K., Takami, K., Banno, Y., Nishikawa, H., Taya, N. and Nakahata, T. Bioorganic & Medicinal Chemistry 93 (2023): 117462.

    • Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan
    • Pharmaceutical Sciences, Takeda Pharmaceutical Company Ltd., 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan

    5FAM-Abu-Gly-Asp-Asp-Asp-Lys-Ile-Val-Gly-Gly-Lys(CPQ2)-Lys-Lys-NH2 (purity: 97.2%, CPC Scientific, Inc.) was diluted with an assay buffer to prepare a 5.4 μM substrate solution.

    Published On: August 29th, 2023Categories: Citations, Dye-Labeled, FRET Substrates
  • Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity.

    Ikeda, Z., Kakegawa, K., Kikuchi, F., Itono, S., Oki, H., Yashiro, H., Hiyoshi, H., Tsuchimori, K., Hamagami, K., Watanabe, M. and Sasaki, M. Journal of Medicinal Chemistry 65, no. 12 (2022): 8456-8477.

    • Research, Takeda Pharmaceutical Company Limited, 26-1, Muraokahigashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan

    Subsequently, 5FAM–Abu–Gly–Asp–Asp–Asp–Lys–Ile–Val–Gly–Gly–Lys(CPQ2)–Lys–Lys–NH2 (purity: 97.2%, CPC Scientific, Inc.) was diluted with an assay buffer to prepare a 2.1 μM substrate solution.

    Published On: June 10th, 2022Categories: Citations, Dye-Labeled, FRET Substrates, Unnatural Amino Acids
  • Discovery and characterization of a small‐molecule enteropeptidase inhibitor, SCO‐792.

    Sasaki, Masako, Ken‐ichi Hamagami et al. Pharmacology Research & Perspectives 7, no. 5 (2019): e00517.

    • Research, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan

    The substrates QSY21‐Gly‐Asp‐Asp‐Asp‐Lys‐Ile‐Val‐Gly‐Gly‐Lys(Cy5) and 5FAM‐Abu‐Gly‐Asp‐Asp‐Asp‐Lys‐Ile‐Val‐Gly‐Gly‐Lys(CPQ2)‐Lys‐Lys‐NH2 were purchased from CPC Scientific (Sunnyvale, CA).

    Published On: February 7th, 2019Categories: Citations, Dye-Labeled, FRET Substrates
  • Time-dependent inhibition of PHD2.

    Tcholakov, I., Grimshaw, C.E., Shi, L., Kiryanov, A., Murphy, S.T., Larson, C.J., Plonowski, A. and Ermolieff, J. Bioscience Reports 37, no. 3 (2017): BSR20170275.

    • Departments of In Vitro Pharmacology, Immunology, Enzymology and Biophysical Chemistry, Medicinal Chemistry, External Innovation, Metabolic Disease, In Vitro Pharmacology, and Gastrointestinal and Enterology Discovery Unit, Takeda California, Inc., 10410 Science Center Drive, San Diego, CA 92121, U.S.A

    The substrate used for our PHD2 kinetic study was a 17-mer peptide mimicking the sequence of HIF-1a surrounding the Pro564 residue hydroxylated by the PHD enzymes (Biotin-DLEMLAPYIPMDDDFQL). The substrate used for FIH1 was a 34-mer peptide mimicking the sequence of HIF-1α surrounding residue Asn803 (DESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRAL). Both peptides were synthesized by CPC Scientific Inc.

    Published On: June 30th, 2017Categories: Citations
  • Residence time and kinetic efficiency analysis of extracellular signal-regulated kinase 2 inhibitors.

    Vanderpool, D., Grimshaw, C.E., Lawson, J.D. and Ermolieff, J. Analytical Biochemistry 473 (2015): 46-52.

    • Enzymology and Biophysical Chemistry Group, Takeda California, San Diego, CA 92121, USA
    • Computational Sciences and Crystallography Group, Takeda California, San Diego, CA 92121, USA

    The mobility shift assay substrate (5-FAM-IPTSPITTTYFFFKKK) was purchased from CPC Scientific (Sunnyvale, CA, USA).

    Published On: December 20th, 2014Categories: Citations, Dye-Labeled