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Discovery of Gut-Restricted PRMT5 Inhibitors to Intercept Colorectal Cancer in Patients with Genetic Loss of Tumor Suppressor Adenomatous Polyposis Coli Hulpia, F.; Schepens, W.; Lepri, S.; Nicolai, J.; Jiang, Z.; Boj, S.F.; Bush, T.L.; Carvalho, M.A.; Chen, F.; Chu, G.; 等. 发现肠道特异性的PRMT5抑制剂,以阻断具有腺瘤性息肉病 coli基因缺失的肿瘤抑制基因患者的结直肠癌。J. Med. Chem. 2025. [Google Scholar] [CrossRef] [PubMed] Hulpia, Fabian; Schepens, Wim; Lepri, Susan; Nicolai, Johan; Jiang, Zhengyu; Boj, Sylvia F.; Bush, Tammy L.; Carvalho, Mary-ambre; Chen, Falian; Chu, Gerald; Clancy, Kathleen W.; Etwebi, Zienab; Everaerts, Melissa; Fan, Yi; Fernandez Candelaria, Froylan Omar; Francis, Albi; Hixon, Mark S.; Jardi, Ferran; Jin, Shuai; Larin, Egor M.; Last, Stefaan; Leenaerts, Joseph E.; Li, Siyu; Liddane, Alexandra G.; Lutter, Ferdinand H.; Lv, Dan; Mattson, Bethany; Milligan, Cynthia M.; Patrick, Aaron N.; Patwardhan, Gauri Anand; Perez-Benito, Laura; Pieters, Serge; Renders, Evelien; Retzbach, Ed; Smith-Monroy, Constance; Silva, Jose; Silva, Mariana; Sterckx, Hans; ten Hag, Gerben; Thate, Claudia; Van Brandt, Sven; Verissimo, Carla S.; Verniest, Guido; Vesely, Eileen; Vetrano, Irene; Vinken, Petra; Wang, Yufei; Wong, Victoria; Yao, Xuemei; Yang, Jie; Zijlmans, Remco; Bachman, Kurtis E.; Pocalyko, David; Jimenez, Juan-Miguel; Gaffney, Dana; Thuring, Jan Willem 分享 收藏
PET clinical study of novel antipsychotic LB-102 demonstrates unexpectedly prolonged dopamine receptor target engagement Wong, Dean F.; Chand, Ganesh B.; Caito, Nicole; Eramo, Anna; Grattan, Vincent T.; Hixon, Mark S.; Nicol, Ginger; Lessie, Erin; Prensky, Zachary; Kuwabara, Hiroto; Tian, Lucy; Valenta, Ines; Schindler, Thomas H.; Gruender, Gerhard; Vaino, Andrew R. 分享 收藏
A randomized, double-blind, placebo controlled, phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of LB-102, a selective dopamine D2/3/5-HT7 inhibitor Biernat, Lukasz; Grattan, Vincent T.; Hixon, Mark S.; Prensky, Zachary; Vaino, Andrew R. 分享 收藏
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LB-102 displays superior dopamine receptor occupancy compared to amisulpride in mouse and human PET studies Vaino, A.; Mintz, A.; Eramo, A.; Caito, N.; Chand, G.; Nicol, G.; Hixon, M.; Grattan, V.; Prensky, Z.; Molotkov, A.; Dolan, M.; Oya, S.; Cabrera, M.; Wang, L.; Wong, D. 分享 收藏
Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one, by Fragment-Based Drug Design (vol 64, pg 12893, 2021) Sabat, Mark; Dougan, Douglas R.; Ermolieff, Jacques; Halkowycz, Petro; Knight, Beverly; Lawson, J. David; Scorah, Nicholas; Smith, Christopher R.; Taylor, Ewan R.; Vu, Phong; Wyrick, Corey; Wang, Haixia; Balakrishna, Deepika; Hixon, Mark; Madakamutil, Loui; McConn, Donavon 分享 收藏
Synthetic fluorescent MYC probe: Inhibitor binding site elucidation and development of a high-throughput screening assay Shirey, Ryan J.; Hart, Jonathan R.; Sridharan, BanuPriya; Novick, Scott J.; Turner, Lewis D.; Zhou, Bin; Nielsen, Alexander L.; Eubanks, Lisa M.; Ueno, Lynn; Hixon, Mark S.; Lairson, Luke L.; Spicer, Timothy P.; Scampavia, Louis D.; Griffin, Patrick R.; Vogt, Peter K.; Janda, Kim D. 分享 收藏
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Synthetic molecules for disruption of the MYC protein-protein interface Jacob, Nicholas T.; Miranda, Pedro O.; Shirey, Ryan J.; Gautam, Ritika; Zhou, Bin; Izquierdo, M. Elena de Orbe; Hixon, Mark S.; Hart, Jonathan R.; Ueno, Lynn; Vogt, Peter K.; Janda, Kim D. 分享 收藏
Pre-clinical evaluation of two novel benzamides, LB-102 and 103, for the treatment of schizophrenia Neill, J.; Grayson, B.; Podda, G.; Cadinu, D.; Beconi, M.; Grattan, V.; Hixon, M. S.; Prensky, Z.; Vaino, A. 分享 收藏
MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody Farrell, Pamela J.; Matuszkiewicz, Jennifer; Balakrishna, Deepika; Pandya, Shweta; Hixon, Mark S.; Kamran, Ruhi; Chu, Shaosong; Lawson, J. David; Okada, Kengo; Hori, Akira; Mizutani, Akio; Iwata, Hidehisa; de Jong, Ron; Hibner, Barbara; Vincent, Patrick 分享 收藏