Effects of MTX-23, a Novel PROTAC of Androgen Receptor Splice Variant-7 and Androgen Receptor, on CRPC Resistant to Second-Line Antiandrogen Therapy.

Autor: Lee GT; Section of Urologic Oncology, Rutgers Cancer Institute of New Jersey, and Division of Urology, Rutgers Robert Wood Johnson Medical School, Rutgers, The State University of New Jersey, New Brunswick, New Jersey., Nagaya N; Section of Urologic Oncology, Rutgers Cancer Institute of New Jersey, and Division of Urology, Rutgers Robert Wood Johnson Medical School, Rutgers, The State University of New Jersey, New Brunswick, New Jersey., Desantis J; Department of Chemistry, Biology and Biotechnology, University of Perugia, Perugia, Italy., Madura K; Department of Pharmacology, Rutgers Robert Wood Johnson Medical School, Rutgers, The State University of New Jersey, Piscataway, New Jersey., Sabaawy HE; Department of Pharmacology, Rutgers Robert Wood Johnson Medical School, Rutgers, The State University of New Jersey, Piscataway, New Jersey.; Division of Medical Oncology, Rutgers Cancer Institute of New Jersey, and Departments of Medicine and Pharmacology, Rutgers Robert Wood Johnson Medical School, Rutgers, The State University of New Jersey, New Brunswick, New Jersey., Kim WJ; Department of Urology, Chungbuk National University College of Medicine, Cheongju, Korea., Vaz RJ; Montelino Therapeutics, LLC, Southborough, Massachusetts., Cruciani G; Department of Chemistry, Biology and Biotechnology, University of Perugia, Perugia, Italy., Kim IY; Section of Urologic Oncology, Rutgers Cancer Institute of New Jersey, and Division of Urology, Rutgers Robert Wood Johnson Medical School, Rutgers, The State University of New Jersey, New Brunswick, New Jersey. kimiy@cinj.rutgers.edu.

Publikováno v: Molecular cancer therapeutics [Mol Cancer Ther] 2021 Mar; Vol. 20 (3), pp. 490-499. Date of Electronic Publication: 2020 Dec 04.

Discovery of 4-Piperazine Isoquinoline Derivatives as Potent and Brain-Permeable Tau Prion Inhibitors with CDK8 Activity.

Autor: Grandjean JM; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Jiu AY; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., West JW; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Aoyagi A; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Droege DG; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Elepano M; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Hirasawa M; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Hirouchi M; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Murakami R; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Lee J; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Sasaki K; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Hirano S; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Ohyama T; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Tang BC; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Vaz RJ; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Inoue M; R&D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan., Olson SH; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Prusiner SB; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Conrad J; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States., Paras NA; Institute for Neurodegenerative Diseases (IND), UCSF Weill Institute for Neurosciences, University of California, San Francisco, San Francisco, California 94518, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2020 Jan 30; Vol. 11 (2), pp. 127-132. Date of Electronic Publication: 2020 Jan 30 (Print Publication: 2020).

Amelioration of PXR-mediated CYP3A4 induction by mGluR2 modulators.

Autor: Vaz RJ; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA. Electronic address: roy.vaz@sanofi.com., Li Y; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Chellaraj V; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Reiling S; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Kuntzweiler T; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Yang D; Pre-Development Sciences, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Shen H; Pre-Development Sciences, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Batchelor JD; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Zhang Y; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Chen X; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., McLean LR; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Kosley R Jr; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Oct 15; Vol. 28 (19), pp. 3194-3196. Date of Electronic Publication: 2018 Aug 20.

Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K ⁺ channel.

Autor: Vaz RJ; Integrated Drug Discovery, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA. Electronic address: roy.vaz@sanofi.com., Kang J; Prelinical Safety, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Luo Y; Drug Metabolism & PK, Sanofi US, 153-2nd Ave., Waltham, MA 02451, USA., Rampe D; Preclinical Safety, Sanofi US, 55 Corporate Blvd, Bridgewater, NJ 08807, USA.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Feb 01; Vol. 28 (3), pp. 446-451. Date of Electronic Publication: 2017 Dec 15.

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