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      1. Home
      2. Posts
      3. FRET Substrates

      FRET Substrates Archive

      • Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Biological and Pharmacological Profiling.

        Alvarez, N., Adam, G.C., Howe, J.A., Sharma, V., Zimmerman, M.D., Dolgov, E., Rasheed, R., Nizar, F., Sahay, K., Nelson, A.M. and Park, S. Viruses 16, no. 7 (2024): 1158.

        1. Center for Discovery and Innovation, Hackensack Meridian Health, 111 Ideation Way, Nutley, NJ 07110, USA
        2. Merck & Co., Inc., Rahway, NJ 07065, USA

        The enzymatic activity of recombinantly expressed 3CLPro enzymes from different coronaviruses was measured using the following synthetic quenched FRET peptide: CP488-ESATLQSGLRKAK- (CPQ2)-NH2 (CPC Scientific, San Jose, CA, USA).

        Published On: July 18th, 2024Categories: Citations, Dye-Labeled, FRET Substrates
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      • The Potential of Usnic-Acid-Based Thiazolo-Thiophenes as Inhibitors of the Main Protease of SARS-CoV-2 Viruses.

        Yarovaya, Olga I., Aleksandr S. Filimonov, Dmitriy S. Baev, Sophia S. Borisevich, Anna V. Zaykovskaya, Varvara Yu Chirkova, Mariya K. Marenina et al. " Viruses 16, no. 2 (2024): 215.

        Fluorescence was observed by an assay involving a synthetic fluorescently labeled peptide substrate of the type DabcylKTSAVLQ↓SGFRKME(Edans)NH2 (more than 95% purity, CPC Scientific Inc., Hangzhou, China) containing the site digested by the main protease of coronavirus. The fluorescent dye attached to the peptide substrate allows the FRET effect to be implemented [..]

        Published On: March 8th, 2024Categories: Citations, Dye-Labeled, FRET Substrates
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      • Invention of MK-7845, a SARS-CoV-2 3CL Protease Inhibitor Employing a Novel Difluorinated Glutamine Mimic.

        Shurtleff, V.W., Layton, M.E., Parish, C.A., Perkins, J.J., Schreier, J.D., Wang, Y., Adam, G.C., Alvarez, N., Bahmanjah, S., Bahnck-Teets, C.M. and Boyce, C.W. Journal of Medicinal Chemistry 67, no. 5 (2024): 3935-3958.

        1. Center for Discovery and Innovation, Hackensack Meridian Health. 111 Ideation Way. Nutley, New Jersey 07110, United States.
        2. Merck & Co., Inc., Rahway, New Jersey 07065, United States.

        The enzymatic activity of recombinantly expressed 3CLPro enzymes from different coronaviruses was measured using the following synthetic quenched FRET peptide: CP488-ESATLQSGLRKAK- (CPQ2)-NH2 (CPC Scientific, San Jose, CA.

        Published On: February 16th, 2024Categories: Citations, COVID-19, Dye-Labeled, FRET Substrates
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      • 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
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      • 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
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      • Ionic liquid-mediated transdermal delivery of thrombosis-detecting nanosensors.

        Bekdemir, Ahmet, Eden EL Tanner, Jesse Kirkpatrick, Ava P. Soleimany, Samir Mitragotri, and Sangeeta N. Bhatia Advanced Healthcare Materials (2022): 2102685.

        Peptides [TDN-qFAM, C-(PEG)2-K(CPQ2)-GGGSRPfGG-5FAM] were obtained from Tufts University Peptide Core Facility or CPC Scientific, Inc (USA)

        Published On: March 14th, 2022Categories: Citations, D-Amino Acids, Dye-Labeled, FRET Substrates, PEGylation
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      • Urinary detection of early responses to checkpoint blockade and of resistance to it via protease-cleaved antibody-conjugated sensors.

        Mac, Quoc D., Anirudh Sivakumar, Hathaichanok Phuengkham, Congmin Xu, James R. Bowen, Fang-Yi Su, Samuel Z. Stentz et al. Nature Biomedical Engineering (2022): 1-15.

        "FITC-labelled GzmB substrate peptides with internal quencher ((5FAM)aIEFDSG(K-CPQ2)kkc) were synthesized by CPC Scientific and used for all in vitro activity assays. [..] Quenched fluorescent peptides for screening candidate substrates ((5FAM)-{substrate}-(K-DABCYL)-amide"

        Published On: March 8th, 2022Categories: Citations, Dye-Labeled, FRET Substrates
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      • Activatable zymography probes enable in situ localization of protease dysregulation in cancer.

        Soleimany, Ava P., [..] Sangeeta N. Bhatia. Cancer Research 81, no. 1 (2021): 213-224.

        All peptides were synthesized by CPC Scientific (Sunnyvale, CA) and reconstituted in dimethylformamide (DMF) unless otherwise specified. Sequences are provided in Supplementary Table S1.

        Published On: October 26th, 2021Categories: Dye-Labeled, FRET Substrates, PEGylation, Unnatural Amino Acids
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      • Peptide-based urinary monitoring of fibrotic nonalcoholic steatohepatitis by mass-barcoded activity-based sensors.

        Cazanave, S.C., Warren, A.D., Pacula, M., Touti, F., Zagorska, A., Gural, N., Huang, E.K., Sherman, S., Cheema, M., Ibarra, S. and Bates, J. Science Translational Medicine 13, no. 616 (2021): eabe8939.

        All peptides were synthesized by CPC Scientific Inc. For fluorogenic assays, peptides were flanked with the fluorophore-quencher pair 5-FAM-CPQ2. For in vivo urine experiments, peptides were barcoded with Glu-Fib–derived and heavy isotope–labeled peptides. PEGylated peptides were pooled prepared before in vivo experiments and stored at 4°C in phosphate-buffered saline.

        Published On: October 20th, 2021Categories: Citations, Dye-Labeled, FRET Substrates
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      • Multiplexed Single-Cell Leukocyte Enzymatic Secretion Profiling from Whole Blood Reveals Patient-Specific Immune Signature.

        Zeming, K. K.; Lu, R.; Woo, K. L.; Sun, G.; Quek, K. Y.; Cheow, L. F.; Chen, C.-H.; Han, J.; Lim, S. L. Analytical Chemistry 2021.

        The FRET substrates used in this project are: neutrophil elastase substrate ((Z-AAAA)2Rh110 Abs/Em:497/520 nm, Anaspec), Granzyme B substrate (5TAMRA-VGPDFGR-K(QSY7)-NH2 Abs/Em: 546/580, CPC scientific), and metalloproteinase substrate (QSY21-HGDQMAQKSK(Cy5)-NH2 Abs/Em:649/666 nm, CPC Scientific).

        Published On: February 18th, 2021Categories: Citations, Dye-Labeled, FRET Substrates
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      12Next
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