Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Simon Charles Goodacre"'
Autor:
Kuen Yeap, John S. Wai, Maia Vinogradova, Yu Zhong, Lori Friedman, Xiaojing Wang, Daniel Otwine, Jiangpeng Liao, Nick Ray, James R. Kiefer, Vidhi Mody, Jun Li, Fabien Roussel, Deepak Sampath, Simon Charles Goodacre, Jun Liang, Michelle Nannini, Sharada Labadie, Xiaoping Zheng, Ellen Ingalla, Steven J. Hartman, Birong Zhang, Jae H. Chang, Tao Wang, Yingqing Ran, Jason R. Zbieg, Amy Sambrone, Kwong Wah Lai, Amy Young, Ciara Metcalfe, Neville James Mclean, Robert A. Blake, Tracy Kleinheinz
Publikováno v:
ACS Med Chem Lett
[Image: see text] Estrogen receptor alpha (ERα) is a well-validated drug target for ER-positive (ER+) breast cancer. Fulvestrant is FDA-approved to treat ER+ breast cancer and works through two mechanisms—as a full antagonist and selective estroge
Autor:
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
Publikováno v:
Journal of medicinal chemistry. 64(16)
Breast cancer remains a leading cause of cancer death in women, representing a significant unmet medical need. Here, we disclose our discovery efforts culminating in a clinical candidate, 35 (GDC-9545 or giredestrant). 35 is an efficient and potent s
Autor:
Xingrong Liu, Nico Ghilardi, Simon Charles Goodacre, Michael Siu, Jim Nonomiya, G. Buckley, Adam R. Johnson, Yun-Xing Cheng, F.A. Romero, Nick Ray, Rohan Mendonca, C. Robinson, Yuen Po-Wai, Jane R. Kenny, Marya Liimatta, Terry Kellar, Mark Zak, Gary Salmon, J. Lloyd, D.G. Brown, Neville James Mclean, Joseph P. Lyssikatos, Emily J. Hanan, Patrick J. Lupardus, Pawan Bir Kohli, Christopher A. Hurley, Guiling Zhao, Paul Gibbons, Peter H. Crackett
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1522-1531
Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1, JAK2, and TYK2) to its receptor
Autor:
Kuen Yeap, Birong Zhang, Jae H. Chang, Lori Friedman, Nick Ray, Jiangpeng Liao, Xiaojing Wang, Amy Sambrone, Jun Li, Yu Zhong, Ellen Ingalla, Jason R. Zbieg, Daniel F. Ortwine, Vidhi Mody, John S. Wai, Tao Wang, Maia Vinogradova, Sharada Labadie, Steven J. Hartman, Tracy Kleinheinz, Nev McLean, Tommy Lai, Simon Charles Goodacre, Deepak Sampath, Jun Liang, Fabien Roussel, James R. Kiefer, Ciara Metcalfe, Xiaoping Zheng, Yingqing Ran, Michelle Nannini, Robert A. Blake
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 50:128335
Fulvestrant is an FDA-approved drug with a dual mechanism of action (MOA), acting as a full antagonist and degrader of the estrogen receptor protein. A significant limitation of fulvestrant is the dosing regimen required for efficacy. Due to its high
Autor:
Stephen Schmidt, Kevin R Clark, Joseph P. Lyssikatos, Brent A. Appleton, Joy Drobnick, Huifen Chen, Christian Wiesmann, Kerry Chapman, Jason Halladay, Ivana Yen, Ping Wu, Lewis J. Gazzard, Simon Charles Goodacre, Steve Sideris, Shiva Malek, Karen Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5704-5709
Checkpoint kinase 1 (ChK1) is activated in response to DNA damage, acting to temporarily block cell cycle progression and allow for DNA repair. It is envisaged that inhibition of ChK1 will sensitize tumor cells to treatment with DNA-damaging therapie
Autor:
Leo Berezhkovsky, Mark Ultsch, Jan Smith, Wade S. Blair, Adam R. Johnson, Calum Macleod, Simon Charles Goodacre, Jason DeVoss, Jun Liang, Kapil Menghrajani, Jim Driscoll, Nico Ghilardi, Wenqian Yang, Steven Magnuson, Karen Williams, Anne van Abbema, Donnie Delarosa, Pawan Bir Kohli, Hieu Nguyen, Kathy Barrett, Steven Shia, Birong Zhang, Sue Sohn, Zhonghua Lin, Christine Chang, Mercedesz Balazs, Priscilla Mantik, Yingjie Lai, Charles Eigenbrot, Vickie Tsui, Amy Sambrone, Ivan Peng, Lawren C. Wu
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(18)
Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through constraint of the rotatable amide bond connecting the pyridine and aryl rings of compound 1. Further optimization
Autor:
John Liu, Stephanie Addo, Gauri Deshmukh, Wyne P. Lee, Mark Zak, Ivan Peng, Hart S. Dengler, Julia Lloyd, Simon Charles Goodacre, Nicholas Charles Ray, Eric Suto, Pawan Bir Kohli, Savita Ubhayakar, Cristine M. Quiason-Huynh, Xiumin Wu, Cornelia H. Rinderknecht, Sheerin K. Shahidi-Latham, Youngsu Kwon, Marya Liimatta, Janet Jackman, Gary Cain, Jane R. Kenny, Gary Salmon, Brent S. McKenzie, Mike Briggs, Adam R. Johnson, Kathy Barrett, Nico Ghilardi
Publikováno v:
Science translational medicine. 10(468)
Preclinical and clinical evidence indicates that a subset of asthma is driven by type 2 cytokines such as interleukin-4 (IL-4), IL-5, IL-9, and IL-13. Additional evidence predicts pathogenic roles for IL-6 and type I and type II interferons. Because
Autor:
Guillaume Médard, Stephen P. Schmidt, Raman Narukulla, Emanuela Gancia, Jason Halladay, Sarah Major, Sharon Yee, Brenda Burton, Ping Wu, Lorraine Axford, Simon Charles Goodacre, Michael Flagella, Eileen Mary Seward, Joy Drobnick, Joanne Hewitt, Charles Ellwood, Lewis J. Gazzard, Judi Ramiscal, Samuel Kintz, Matthew Gill, Calum Macleod, Hazel Hunt, Kerry Chapman, Shiva Malek, Peter H. Crackett, Huifen Chen, Christian Wiesmann, Ivana Yen, Jennifer Epler, Karen Williams, Elizabeth Blackwood, Joseph P. Lyssikatos
Publikováno v:
Journal of medicinal chemistry. 58(12)
Checkpoint kinase 1 (ChK1) plays a key role in the DNA damage response, facilitating cell-cycle arrest to provide sufficient time for lesion repair. This leads to the hypothesis that inhibition of ChK1 might enhance the effectiveness of DNA-damaging
Autor:
Gerard R. Dawson, David S. Reynolds, Elizabeth M. Garrett, Sharlene Bull, Paul J. Whiting, John R. Atack, Richard J. Newman, Thomas W. Rosahl, Rosa L. Fradley, Gillian F. O'Meara, Simon Charles Goodacre, Keith A. Wafford, David James Hallett, Martin R. Guscott
Publikováno v:
Journal of Psychopharmacology. 21:384-391
Non-selective benzodiazepines, such as diazepam, interact with equivalent affinity and agonist efficacy at GABAA receptors containing either an α1, α2, α3 or α5 subunit. However, which of these particular subtypes are responsible for the anticonv
Autor:
Kevin John Merchant, Steve Thomas, Emanuela Gancia, Alexander Charles Humphries, David James Hallett, Myra Gilligan, Simon Charles Goodacre
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1518-1522
8-Fluoroimidazo[1,2-a]pyridine has been established as a physicochemical mimic of imidazo[1,2-a]pyrimidine, using both in silico and traditional techniques. Furthermore, a novel synthesis of a 3,7-disubstituted-8-fluoroimidazopyridine 3 has been deve