يعرض 1 - 10 نتائج من 41 نتيجة بحث عن '"Martin James Wythes"', وقت الاستعلام: 0.88s تنقيح النتائج
  1. 1
    SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

    المؤلفون: Karen A. Maegley, Kephart Susan Elizabeth, Christopher P. Dillon, Manli Shi, Kristen Jensen-Pergakes, Prakash B. Palde, Ya-Li Deng, Chi-Yeh Chung, Natalie Miller, John Sherrill, Wei Liu, Ryan L. Patman, Shinji Yamazaki, Tao Xie, Fen Wang, Hieu Lam, Eleanore Hendrickson, John F. Braganza, Yuli Wang, Robert Arnold Kumpf, Shannon Karlicek Bryant, Thomas A Paul, Noah Spiegel, Martin James Wythes, Amy Nemeth, Stephanie Scales, Elizabeth A. McMillan, Michelle Tran-Dubé, Alexei Brooun, Vesta Goshtasbi, Eugene Rui, Michele McTigue, Indrawan James Mcalpine, Tatlock John H

    المصدر: Molecular Cancer Therapeutics. 21:3-15

    مصطلحات موضوعية: Protein-Arginine N-Methyltransferases, S-Adenosylmethionine, Cancer Research, Cell signaling, Spliceosome, Lung Neoplasms, Chemistry, Cellular differentiation, Protein arginine methyltransferase 5, Alternative splicing, Drug Resistance, Apoptosis, Cell cycle, Mice, Oncology, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, RNA splicing, Cancer cell, Cancer research, Animals, Humans, Female, Cell Proliferation

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::621805778a73d6732ba64af7ea279a54
    https://doi.org/10.1158/1535-7163.mct-21-0620

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  2. 2
    Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

    المؤلفون: Jie Guo, Li-Chin Yao, Christopher P. Dillon, Wenlin Li, Stefano Crosignani, Karen A. Maegley, Danying Cai, Reece Marillier, Sandra Cauwenberghs, Manfred Kraus, Virginie Rabolli, Valeria Fantin, Benoît Van den Eynde, Deepak Dalvie, Joseph Tumang, Derek W. Bartlett, Martin James Wythes, Vince Torti, Xianxian Zheng, Sofie Denies, Gregory Driessens, Bruno Gomes, Nichol Miller, Konstantinos Tsaparikos, Nicole Streiner, Marie-Claire Letellier, Chad Ray, Romain Pirson

    المصدر: Molecular Cancer Therapeutics. 17:2530-2542

    مصطلحات موضوعية: 0301 basic medicine, Cancer Research, Indoles, T-Lymphocytes, medicine.medical_treatment, Succinimides, Antineoplastic Agents, Antibodies, Monoclonal, Humanized, B7-H1 Antigen, Substrate Specificity, Immune tolerance, Interferon-gamma, 03 medical and health sciences, chemistry.chemical_compound, Lymphocytes, Tumor-Infiltrating, 0302 clinical medicine, Downregulation and upregulation, Cell Line, Tumor, medicine, Animals, Humans, Indoleamine-Pyrrole 2,3,-Dioxygenase, CTLA-4 Antigen, Enzyme Inhibitors, Indoleamine 2,3-dioxygenase, Kynurenine, Cell Proliferation, Mice, Inbred BALB C, Tumor microenvironment, Chemistry, Antibodies, Monoclonal, FOXP3, Stereoisomerism, Immunotherapy, Immune checkpoint, Mice, Inbred C57BL, 030104 developmental biology, Oncology, 030220 oncology & carcinogenesis, Biocatalysis, Cancer research, Female

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4e86621e1bbba77214c450e8001b4c6
    https://doi.org/10.1158/1535-7163.mct-17-1104

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  3. 3
    Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497)

    المؤلفون: Michael R. Collins, Robert Steven Kania, Connie Fan, Sutton Scott Channing, Dominique Verhelle, Kephart Susan Elizabeth, Martin James Wythes, Shuiwang Wang, Karen A. Maegley, Lisa Nguyen, Daniel Tyler Richter, A.E. Stewart, Pei-Pei Kung, Buwen Huang, Shikhar Sharma, Shinji Yamazaki, Ya-Li Deng, Rita Grantner, Patrick Bingham, Robert Arnold Kumpf, Penney Khamphavong, Jinjiang Zhu, Dac M. Dinh, Manfred Kraus, Wei Liu, Sean Uryu, Jillian E. Spangler, Wenyue Hu, Hui Wang, Robert A. Rollins, Cody Krivacic, Zehnder Luke Raymond, Neal W. Sach, Alexei Brooun, John Sherrill, Shijian Ren, Martin A. Edwards, Huichun Zhu, Ketan S. Gajiwala, Shuibo Xin, Hovhannes J. Gukasyan

    المصدر: Journal of Medicinal Chemistry. 61:650-665

    مصطلحات موضوعية: 0301 basic medicine, Chemistry, Stereochemistry, Ligand (biochemistry), 03 medical and health sciences, chemistry.chemical_compound, 030104 developmental biology, In vivo, Drug Discovery, Lactam, Molecular Medicine, Moiety, Molecule, Solubility, Lead compound, ADME

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::f30f1b1d2d6acfd5a3cfe913d0c1179d
    https://doi.org/10.1021/acs.jmedchem.7b01375

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  4. 4
    Abstract 1160: SAM competitive PRMT5 inhibitor PF06939999 demonstrates antitumor activity in splicing dysregulated NSCLC with decreased liability of drug resistance

    المؤلفون: Eleanore Hendrickson, Martin James Wythes, Indrawan James Mcalpine, Karen A. Maegley, Christopher P. Dillon, Fen Wang, Kephart Susan Elizabeth, Amy Nemeth, Prakash B. Palde, Manli Shi, Kristen Jensen-Pergakes, Shinji Yamazaki, Tao Xie, Chi-Yeh Chung, Michelle Tran-Dubé, Tatlock John H, Stephanie Scales, Hieu Lam, Eugene Rui, Thomas A Paul, Elizabeth A. McMillan, Robert Arnold Kumpf, Ryan L. Patman, Michele McTigue, Natalie Miller, Ya-Li Deng, Yuli Wang, Noah Spiegel, Alexei Brooun, John Sherrill, Wei Liu, John F. Braganza

    المصدر: Cancer Research. 81:1160-1160

    مصطلحات موضوعية: Antitumor activity, Cancer Research, Oncology, Chemistry, Protein arginine methyltransferase 5, RNA splicing, Cancer research, Drug resistance

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::ffac773af19496024ab15b63ff654a26
    https://doi.org/10.1158/1538-7445.am2021-1160

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  5. 5
    Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase

    المؤلفون: Dafydd R. Owen, Aiping Dong, Martin James Wythes, Steven Kennedy, Dalia Barsyte-Lovejoy, Matthieu Schapira, Hong Wu, Rajiah Aldrin Denny, Viacheslav V. Trush, Mihir D. Parikh, Agustin Casimiro-Garcia, Renato Ferreira de Freitas, Masoud Vedadi, Magdalena Swewczyk, Hong Zeng, Tatlock John H, Fengling Li, Alexandria P. Taylor, Robert Arnold Kumpf, Peter Brown, Cheryl H. Arrowsmith

    المصدر: Journal of medicinal chemistry. 62(17)

    مصطلحات موضوعية: Models, Molecular, S-Adenosylmethionine, Methyltransferase, Lysine, 01 natural sciences, Small Molecule Libraries, 03 medical and health sciences, Structure-Activity Relationship, Drug Discovery, Structure–activity relationship, Humans, Binding site, Enzyme Inhibitors, Enhancer, Cells, Cultured, 030304 developmental biology, Cell Proliferation, chemistry.chemical_classification, 0303 health sciences, Binding Sites, Dose-Response Relationship, Drug, Molecular Structure, Substrate (chemistry), Histone-Lysine N-Methyltransferase, Small molecule, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Enzyme, chemistry, Biochemistry, Molecular Medicine

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e491e646b8409403d237931a50d510f6
    https://pubmed.ncbi.nlm.nih.gov/31415173

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  6. 6
    Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1 H -indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate

    المؤلفون: Nichol Miller, Marie Cordonnier, Hélène Cannelle, Frederik Deroose, Joseph Tumang, James Soloweij, Bruno Gomes, Stefano Crosignani, Michel Negrerie, Patrick Bingham, Karen A. Maegley, A.E. Stewart, Sandra Cauwenberghs, Martin James Wythes, Pauline Bottemanne, Benoît Van den Eynde, Stephen E. Kaiser, Vince Torti, Manfred Kraus, Brion W. Murray, Jun Li Feng, Deepak Dalvie, Manfred Schneider, Samantha Elizabeth Greasley

    المساهمون: iTeos Therapeutics (iTeos), Pfizer, Asclepia Outsourcing Solutions, Laboratoire d'Optique et Biosciences (LOB), Centre National de la Recherche Scientifique (CNRS)-Institut National de la Santé et de la Recherche Médicale (INSERM)-École polytechnique (X), Université Catholique de Louvain = Catholic University of Louvain (UCL)

    المصدر: Journal of Medicinal Chemistry
    Journal of Medicinal Chemistry, American Chemical Society, 2017, 60 (23), pp.9617-9629. ⟨10.1021/acs.jmedchem.7b00974⟩

    مصطلحات موضوعية: 0301 basic medicine, Male, Indoles, Succinimides, Pharmacology, Crystallography, X-Ray, Pyrrolidine, Immune tolerance, Cell Line, 03 medical and health sciences, chemistry.chemical_compound, Mice, Structure-Activity Relationship, Dogs, Drug Discovery, Structure–activity relationship, Animals, Humans, Indoleamine-Pyrrole 2,3,-Dioxygenase, [SDV.BBM]Life Sciences [q-bio]/Biochemistry, Molecular Biology, Enzyme Inhibitors, Indoleamine 2,3-dioxygenase, ComputingMilieux_MISCELLANEOUS, ADME, chemistry.chemical_classification, Effector, Oxidoreductase inhibitor, 3. Good health, Rats, Molecular Docking Simulation, Macaca fascicularis, 030104 developmental biology, Enzyme, chemistry, Cancer research, Molecular Medicine

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9b3e812bb87fe80822746419021eb31
    https://hal-polytechnique.archives-ouvertes.fr/hal-01760561

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  7. 7
    Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

    المؤلفون: Hovhannes J. Gukasyan, Michael R. Collins, Sutton Scott Channing, Kephart Susan Elizabeth, Shinji Yamazaki, Sacha Ninkovic, Simon Bergqvist, Fen Wang, Robert Arnold Kumpf, Michael Ryskin, Patrick Bingham, Pei-Pei Kung, Dominique Verhelle, Brian Yip, Karen A. Maegley, Robert A. Rollins, Peter A. Wells, Martha A. Ornelas, Buwen Huang, Valeria Fantin, Xiu Yu, Stephanie Scales, Wade Diehl, Indrawan James Mcalpine, Cody Krivacic, Mei Cui, Lisa Nguyen, Wenyue Hu, Tatlock John H, Dac M. Dinh, Martin James Wythes, Connie Fan, Gary Li, Martin Paul Edwards, Rui Eugene Yuanjin, John F. Braganza, Zehnder Luke Raymond, Wei-Guo Zhang

    المصدر: Journal of medicinal chemistry. 59(18)

    مصطلحات موضوعية: 0301 basic medicine, Models, Molecular, Lactams, Stereochemistry, Pyridones, Antineoplastic Agents, Mice, SCID, 03 medical and health sciences, chemistry.chemical_compound, Mice, In vivo, Amide, Cell Line, Tumor, Neoplasms, Drug Discovery, Potency, Moiety, Animals, Humans, Enhancer of Zeste Homolog 2 Protein, Ligand efficiency, Isoquinolines, 030104 developmental biology, chemistry, Lipophilic efficiency, Cyclization, Drug Design, Lactam, Molecular Medicine, Female, Linker

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f62bbe5fc41702928ba23fd544b9fadd
    https://pubmed.ncbi.nlm.nih.gov/27936698

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  8. 8
    Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-Containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-Amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide

    المؤلفون: Tanya Michelle Jewell, Robert Steven Kania, Anand Sistla, Bennett Michael John, Michael R. Gehring, Evan Smith, Zehnder Luke Raymond, Shinji Yamazaki, Karen A. Maegley, Elena Z. Dovalsantos, Ben Burke, Fen Wang, Sacha Ninkovic, Jeff Wang, Joe Zhongxiang Zhou, Pei-Pei Kung, Min-Jean Yin, Michael J. Hickey, Martin James Wythes, Jerry Meng, Buwen Huang, Ping Kang, John F. Braganza, Ketan S. Gajiwala, Tatlock John H, Pramod P. Mehta

    المصدر: Journal of Medicinal Chemistry. 54:3368-3385

    مصطلحات موضوعية: Pyrimidine, biology, Chemistry, Stereochemistry, medicine.drug_class, Carboxamide, Metabolic stability, Combinatorial chemistry, Hsp90, Bioavailability, chemistry.chemical_compound, Heat shock protein, Drug Discovery, Alkoxy group, biology.protein, medicine, Molecular Medicine, Potency

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::3fc866a72d07c6999eda9ddc940a1344
    https://doi.org/10.1021/jm200128m

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  9. 9
    Abstract 4857: Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity

    المؤلفون: Indrawan James Mcalpine, Shinji Yamazaki, Wei Liu, Zhenxiong Wang, Michelle Tran-Dubé, Deng Ya-Li, Kristen Jensen-Pergakes, Brad Hirakawa, Ryan L. Patman, Karen A. Maegley, Joseph Billitti, Martin James Wythes, Tatlock John H, Fen Wang, Robert Arnold Kumpf, Tao Zhang, Stephanie Scales, Noah Spiegel, Rui Eugene Yuanjin, John F. Braganza, Michele McTigue, Alexei Brooun

    المصدر: Cancer Research. 78:4857-4857

    مصطلحات موضوعية: 0301 basic medicine, Cancer Research, Arginine, Chemistry, Protein arginine methyltransferase 5, Ligand (biochemistry), In vitro, 03 medical and health sciences, 030104 developmental biology, Protein structure, Oncology, Biochemistry, RNA splicing, Transcriptional regulation, Nucleoside

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::2b8092ccb21304e98d228226d2d47f11
    https://doi.org/10.1158/1538-7445.am2018-4857

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  10. 10
    Stereoselective syntheses of protected β-hydroxy-α-amino acids using (arylthio)nitrooxiranes

    المؤلفون: Zoe M. Adams, Richard F. W. Jackson, Nicholas J. Palmer, Martin James Wythes, Harshad Kantilal Rami

    المصدر: Journal of the Chemical Society, Perkin Transactions 1. :937-948

    مصطلحات موضوعية: chemistry.chemical_classification, chemistry.chemical_compound, Stereospecificity, chemistry, Nucleophile, Stereochemistry, Alkene, Diastereomer, Organic chemistry, Stereoselectivity, Thioester, Peroxide, Aldehyde

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::e74ca24190f58eba21492d7525e97603
    https://doi.org/10.1039/a901077g

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