المؤلفون: Jun Liang (251318), Jason R. Zbieg (1892965), Robert A. Blake (8974823), Jae H. Chang (1429789), Stephen Daly (2430460), Antonio G. DiPasquale (1274730), Lori S. Friedman (166879), Thomas Gelzleichter (11113391), Matthew Gill (589302), Jennifer M. Giltnane (11113394), Simon Goodacre (1577413), Jane Guan (166826), Steven J. Hartman (10157036), Ellen Rei Ingalla (8908757), Lorn Kategaya (11113397), James R. Kiefer (1443889), Tracy Kleinheinz (1845637), Sharada S. Labadie (1833826), Tommy Lai (2572615), Jun Li (6494), Jiangpeng Liao (1947631), Zhiguo Liu (594653), Vidhi Mody (8908760), Neville McLean (2128303), Ciara Metcalfe (8908763), Michelle A. Nannini (11113400), Jason Oeh (1845505), Martin G. O’Rourke (11113403), Daniel F. Ortwine (1600621), Yingqing Ran (2100610), Nicholas C. Ray (3064926), Fabien Roussel (3030714), Amy Sambrone (1551289), Deepak Sampath (640340), Leah K. Schutt (11113406), Maia Vinogradova (8908772), John Wai (1503217), Tao Wang (12008), Ingrid E. Wertz (11113409), Jonathan R. White (11113412), Siew Kuen Yeap (1346391), Amy Young (251900), Birong Zhang (1947472), Xiaoping Zheng (566379), Wei Zhou (24328), Yu Zhong (291917), Xiaojing Wang (147040)

مصطلحات موضوعية: Cell Biology, Genetics, Neuroscience, Pharmacology, Biotechnology, Cancer, Infectious Diseases, Chemical Sciences not elsewhere classified, Information Systems not elsewhere classified, Exceptional Preclinical Profile, dose, Bioavailable, human, candidate, combination, liability, Phase, Orally, antagonist, Breast Cancer Breast cancer, wild-type ER α tumor model, GDC -9545, estrogen receptor degrader, antiproliferation, SERD, interaction, Estrogen Receptor Antagonist, giredestrant, Fine-tuning, PDX

العلاقة: https://figshare.com/articles/journal_contribution/GDC-9545_Giredestrant_A_Potent_and_Orally_Bioavailable_Selective_Estrogen_Receptor_Antagonist_and_Degrader_with_an_Exceptional_Preclinical_Profile_for_ER_Breast_Cancer/14959973Test

الإتاحة: https://doi.org/10.1021/acs.jmedchem.1c00847.s001Test

المؤلفون: Martin O'Rourke, Nicholas Charles Ray, Thomas Gelzleichter, Leah Schutt, Ellen Ingalla, Neville James Mclean, Xiaojing Wang, Stephen Daly, Yingqing Ran, Jiangpeng Liao, Tommy Lai, Yu Zhong, Jun Liang, Sharada Labadie, Lori Friedman, Amy Sambrone, Jun Li, Robert A. Blake, Tao Wang, Liu Zhiguo, Birong Zhang, Steven J. Hartman, Jae H. Chang, Wei Zhou, Jane Guan, Vidhi Mody, Jonathan White, Fabien Roussel, Antonio G. DiPasquale, Jason R. Zbieg, Daniel F. Ortwine, Amy Young, James R. Kiefer, Maia Vinogradova, Simon Charles Goodacre, Deepak Sampath, Tracy Kleinheinz, Xiaoping Zheng, Jennifer M. Giltnane, Lorn Kategaya, Ingrid E. Wertz, Matthew Gill, Ciara Metcalfe, Siew Kuen Yeap, John S. Wai, Jason Oeh, Michelle Nannini

المصدر: Journal of medicinal chemistry. 64(16)

مصطلحات موضوعية: Phases of clinical research, Estrogen receptor, Antineoplastic Agents, Breast Neoplasms, Mice, Structure-Activity Relationship, Breast cancer, Dogs, In vivo, Drug Discovery, medicine, Animals, Humans, Dosing, Molecular Structure, Chemistry, Antagonist, Estrogen Receptor alpha, medicine.disease, Xenograft Model Antitumor Assays, In vitro, Rats, Macaca fascicularis, Cell culture, Cancer research, MCF-7 Cells, Molecular Medicine, Female, Estrogen Receptor Antagonists, Carbolines

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee86fe3f8068fbb2ff9647a59eadb710Test
https://pubmed.ncbi.nlm.nih.gov/34251202Test

المؤلفون: Sharada S. Labadie, Jun Li, Robert A. Blake, Jae H. Chang, Simon Goodacre, Steven J. Hartman, Weiling Liang, James R. Kiefer, Tracy Kleinheinz, Tommy Lai, Jiangpeng Liao, Daniel F. Ortwine, Vidhi Mody, Nicholas C. Ray, Fabien Roussel, Maia Vinogradova, Siew Kuen Yeap, Birong Zhang, Xiaoping Zheng, Jason R. Zbieg, Jun Liang, Xiaojing Wang

المصدر: Bioorganicmedicinal chemistry letters. 29(16)

مصطلحات موضوعية: Flavonoids, Organic Chemistry, Clinical Biochemistry, Estrogen Receptor alpha, Pharmaceutical Science, Administration, Oral, Stereoisomerism, Crystallography, X-Ray, Biochemistry, Rats, Structure-Activity Relationship, Drug Stability, Drug Discovery, MCF-7 Cells, Microsomes, Liver, Molecular Medicine, Animals, Azetidines, Humans, Molecular Biology

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac7b8e6efb534204e3e55a5bc39c8825Test
https://pubmed.ncbi.nlm.nih.gov/31311734Test

المؤلفون: Philip Stephen Jackson, Robert Heald, Siew Kuen Yeap, Bryan K. Chan, Michael D. Lainchbury, Ivana Yen, Christine Yu, Stephen P. Schmidt, Marian C. Bryan, Inna Zilberleyb, Jianping Yin, Steve Sideris, Shiva Malek, Eileen Mary Seward, Charles Eigenbrot, Hank La, Shumei Wang, Christine Tam, Gabriele Schaefer, Emily J. Hanan, Jennafer Dotson, Timothy P. Heffron, Daniel J. Burdick, Yuan Chen, Hans E. Purkey

المصدر: Journal of Medicinal Chemistry

مصطلحات موضوعية: Threonine, Lung Neoplasms, Aminopyridines, Crystallography, X-Ray, Article, chemistry.chemical_compound, T790M, Methionine, Gefitinib, Carcinoma, Non-Small-Cell Lung, Drug Discovery, medicine, Humans, Epidermal growth factor receptor, Protein Kinase Inhibitors, EGFR inhibitors, biology, Cell growth, Molecular biology, High-Throughput Screening Assays, respiratory tract diseases, ErbB Receptors, Diaminopyrimidine, Amino Acid Substitution, chemistry, Protein kinase domain, Drug Resistance, Neoplasm, Mutation, biology.protein, Molecular Medicine, Erlotinib, medicine.drug

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::535b284cca6032b3ca3d447ff8a6c52fTest
https://doi.org/10.1021/jm501578nTest

المؤلفون: Charles Eigenbrot, Robert Heald, Bryan K. Chan, Michael D. Lainchbury, Timothy P. Heffron, Hans E. Purkey, Hank La, Philip Stephen Jackson, Stephen P. Schmidt, Gabriele Schaefer, Emily Chan, Marian C. Bryan, Ivana Yen, Jamie D. Knight, Daniel J. Burdick, Yuan Chen, Lily Shao, Richard L. Elliott, Jennafer Dotson, Shiva Malek, Christine Yu, Krista K. Bowman, Steve Sideris, Hanan Emily, Shumei Wang, Saundra Clausen, Siew Kuen Yeap, Eileen Mary Seward, Trisha Dela Vega

المصدر: Journal of medicinal chemistry. 59(19)

مصطلحات موضوعية: 0301 basic medicine, Models, Molecular, Lung Neoplasms, Mutant, Antineoplastic Agents, Crystallography, X-Ray, 03 medical and health sciences, T790M, Mice, 0302 clinical medicine, In vivo, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Drug Discovery, Animals, Humans, Epidermal growth factor receptor, Binding site, Lung, Protein Kinase Inhibitors, EGFR inhibitors, Cell Proliferation, biology, Chemistry, Point mutation, Molecular biology, In vitro, respiratory tract diseases, ErbB Receptors, 030104 developmental biology, Drug Resistance, Neoplasm, 030220 oncology & carcinogenesis, Mutation, biology.protein, Molecular Medicine

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d4580624912774874fa97c4be36fcefTest
https://pubmed.ncbi.nlm.nih.gov/27564586Test