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      1. Home
      2. Tag:
      3. Merck

      Merck 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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      • 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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      • Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists.

        Chandramohan, A., Josien, H., Yuen, T.Y., Duggal, R., Spiegelberg, D., Yan, L., Juang, Y.C.A., Ge, L., Aronica, P.G., Kaan, H.Y.K. and Lim, Y.H. Nature Communications 15, no. 1 (2024): 489.

        1. Merck & Co., Inc., Kenilworth, NJ 07033, USA.
        2. Merck & Co., Inc., Boston, MA 02115, USA
        3. Merck & Co., Inc., West Point, PA 19486, USA
        4. Genentech, South San Francisco, CA 94080, USA

        We thank Evans (Chen) Ge, Mike (Dixin) Xue, and Simon (Junhua) Li at Chinese Peptide Company (CPC) for peptide synthesis support.

        Published On: January 12th, 2024Categories: Citations, Click Peptides, Stapled Peptides, Unnatural Amino Acids
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      • Longitudinal CSF proteomics identifies NPTX2 as a prognostic biomarker of Alzheimer’s disease.

        Libiger, O., Shaw, L.M., Watson, M.H., Nairn, A.C., Umaña, K.L., Biarnes, M.C., Canet‐Avilés, R.M., Jack Jr, C.R., Breton, Y.A., Cortes, L. and Chelsky, D. Alzheimer's & Dementia 17, no. 12 (2021): 1976-1987.

        1. Janssen Research and Development, 3210 Merryfield Row, San Diego, CA 92121, USA.
        2. Foundation for the National Institutes of Health, North Bethesda, Maryland, USA
        3. Department of Radiology, Mayo Clinic, Rochester, Minnesota, USA
        4. Merck & Co., Inc., West Point, Pennsylvania, USA

        Purified synthetic stable isotope (15N and 13C) labeled (SIL) peptides were from CPC Scientific (EDSLEAGLPLQVR [CMGA]; SLGVGFATR [FABPH]; VLEYLNQEK [SCG2]; and THLGEALAPLSK [VGF]); and JPT Peptide Technologies (TNYLYGK [NPTX2]).

        Published On: March 13th, 2021Categories: Citations, Isotope-Labeled Peptides
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      • Inhibition of factor XIa reduces the frequency of cerebral microembolic signals derived from carotid arterial thrombosis in rabbits.

        Wang, X., Kurowski, S., Wu, W., Castriota, G.A., Zhou, X., Chu, L., Ellsworth, K.P., Chu, D., Edmondson, S., Ali, A. and Andre, P. Journal of Pharmacology and Experimental Therapeutics 360, no. 3 (2017): 476-483.

        1. Departments of Cardiometabolic Disease Biology, Discovery Pharmaceutical Sciences, In Vitro Pharmacology, and Discovery Chemistry, Merck Research Laboratories, Kenilworth, New Jersey.
        2. Lead Optimization Chemistry, Merck Research Laboratories, Rahway, New Jersey.

        The 7-amido-4-thifluoromethylcoumarin (AFC) containing fluorescence substrate, CH3SO2-cyclohexyl-Gly-Gly-Arg-AFC (cyclohexyl-G-G-R-AFC) was custom synthesized by CPC Scientific (Sunnyvale, CA, USA)..

        Published On: March 1st, 2017Categories: Citations, Dye-Labeled, Unnatural Amino Acids
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      • Factor XIIa as a novel target for thrombosis: target engagement requirement and efficacy in a rabbit model of microembolic signals.

        Barbieri, Christopher M., et al. Journal of Pharmacology and Experimental Therapeutics 360.3 (2017): 466-475.

        • In Vitro Pharmacology and Cardiometabolic Diseases, Merck & Co., Inc., Kenilworth, New Jersey

        "The 7-amido-4-thifluoromethylcoumarin (AFC) containing fluorescence substrate, CH3SO2-cyclohexyl-Gly-Gly-Arg-AFC (cyclohexylG-G-R-AFC) was custom synthesized by CPC Scientific (Sunnyvale, CA, USA)"

        Published On: February 10th, 2017Categories: Citations, Dye-Labeled, Unnatural Amino Acids
        Learn More
      • Development and validation of an IA-LC/MS method to quantitate active and total B-type natriuretic peptide in human plasma.

        Chappell, D.L., Lee, A.Y., Bernstein, H.S., Lassman, M.E. and Laterza, O.F. Bioanalysis 8, no. 22 (2016): 2341-2349.

        • Merck & Co., Inc. Rahway, NJ07065, USA
        Published On: July 15th, 2016Categories: Citations
        Learn More
      • Multiplexed quantification of proglucagon-derived peptides by immunoaffinity enrichment and tandem mass spectrometry after a meal tolerance test.

        Lopez, A., Reyna, D.E., Gitego, N. et al. Co-targeting of BAX and BCL-XL proteins broadly overcomes resistance to apoptosis in cancer. Nat Commun 13, 1199 (2022).

        • Cardio-metabolic Disease Biomarkers, Merck Research Laboratories, Kenilworth, NJ., Merck & Co., Inc.

        "Glucagon synthetic peptide and heavy isotope–labeled internal standards (ISs) of oxyntomodulin and glucagon containing 2 [ 13 C 6 - 15 N]-labeled leucines and 1 [ 13 C 9 - 15 N]-labeled phenylalanine were synthesized by CPC Scientific.."

        Published On: December 10th, 2015Categories: Citations, Isotope-Labeled Peptides
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      • Acute hemodynamic and renal effects of glucagon-like peptide 1 analog and dipeptidyl peptidase-4 inhibitor in rats.

        Zhou, X., Huang, C.H., Lao, J., Pocai, A., Forrest, G., Price, O., Roy, S., Kelley, D.E., Sullivan, K.A. and Forrest, M.J. Cardiovascular Diabetology 14 (2015): 1-10.

        • Departments of Cardiometabolic Diseases and In Vivo Pharmacology, Merck Research Laboratories, 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA

        GLP-1 was purchased from CPC Scientific (San Jose, California). MK-0626 was synthesized by Merck & Co., Inc.

        Published On: March 7th, 2015Categories: Citations
        Learn More
      • Use of high-throughput mass spectrometry to reduce false positives in protease uHTS screens.

        Adam, G.C., Meng, J., Rizzo, J.M., Amoss, A., Lusen, J.W., Patel, A., Riley, D., Hunt, R., Zuck, P., Johnson, E.N. and Uebele, V.N. Journal of Biomolecular Screening 20, no. 2 (2015): 212-222.

        • Screening and Protein Sciences, Merck Research Labs, North Wales, PA, USA

        Plates were incubated for 210 min at 25 °C followed by quenching with 25 uL water with 2% formic acid containing 600 nM of the internal standard with the sequence KTEEISEVN[L-U7]-OH (CPC Scientific).

        Published On: October 21st, 2014Categories: Citations, Isotope-Labeled Peptides
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