Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Lawrence M. Szewczuk"'
Autor:
Carl A. Machutta, Christopher S. Kollmann, Kenneth E. Lind, Xiaopeng Bai, Pan F. Chan, Jianzhong Huang, Lluis Ballell, Svetlana Belyanskaya, Gurdyal S. Besra, David Barros-Aguirre, Robert H. Bates, Paolo A. Centrella, Sandy S. Chang, Jing Chai, Anthony E. Choudhry, Aaron Coffin, Christopher P. Davie, Hongfeng Deng, Jianghe Deng, Yun Ding, Jason W. Dodson, David T. Fosbenner, Enoch N. Gao, Taylor L. Graham, Todd L. Graybill, Karen Ingraham, Walter P. Johnson, Bryan W. King, Christopher R. Kwiatkowski, Joël Lelièvre, Yue Li, Xiaorong Liu, Quinn Lu, Ruth Lehr, Alfonso Mendoza-Losana, John Martin, Lynn McCloskey, Patti McCormick, Heather P. O’Keefe, Thomas O’Keeffe, Christina Pao, Christopher B. Phelps, Hongwei Qi, Keith Rafferty, Genaro S. Scavello, Matt S. Steiginga, Flora S. Sundersingh, Sharon M. Sweitzer, Lawrence M. Szewczuk, Amy Taylor, May Fern Toh, Juan Wang, Minghui Wang, Devan J. Wilkins, Bing Xia, Gang Yao, Jean Zhang, Jingye Zhou, Christine P. Donahue, Jeffrey A. Messer, David Holmes, Christopher C. Arico-Muendel, Andrew J. Pope, Jeffrey W. Gross, Ghotas Evindar
Publikováno v:
Nature Communications, Vol 8, Iss 1, Pp 1-11 (2017)
Encoded Library Technology (ELT) has streamlined the identification of chemical ligands for protein targets in drug discovery. Here, the authors optimize the ELT approach to screen multiple proteins in parallel and identify promising targets and anti
Externí odkaz:
https://doaj.org/article/a0c4424f2eeb46a689586e4828ae7887
Autor:
Guozhang Xu, Zhijie Liu, Xinkang Wang, Tianbao Lu, Renee L. DesJarlais, Tho Thieu, Jing Zhang, Zheng Huang Devine, Fuyong Du, Qiu Li, Cynthia M. Milligan, Paul Shaffer, Peder E. Cedervall, John C. Spurlino, Christopher F. Stratton, Beth Pietrak, Lawrence M. Szewczuk, Victoria Wong, Ruth A. Steele, Wouter Bruinzeel, Madhu Chintala, Jose Silva, Michael D. Gaul, Mark J. Macielag, Ravi Nargund
Publikováno v:
Journal of medicinal chemistry. 65(15)
Activated factor XI (FXIa) inhibitors are promising novel anticoagulants with low bleeding risk compared with current anticoagulants. The discovery of potent FXIa inhibitors with good oral bioavailability has been challenging. Herein, we describe our
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d97b97b82cd74e1de0878b0437d2311e
https://pubmed.ncbi.nlm.nih.gov/35862732
https://pubmed.ncbi.nlm.nih.gov/35862732
Autor:
Carl A. Machutta, Christopher S. Kollmann, Kenneth E. Lind, Xiaopeng Bai, Pan F. Chan, Jianzhong Huang, Lluis Ballell, Svetlana Belyanskaya, Gurdyal S. Besra, David Barros-Aguirre, Robert H. Bates, Paolo A. Centrella, Sandy S. Chang, Jing Chai, Anthony E. Choudhry, Aaron Coffin, Christopher P. Davie, Hongfeng Deng, Jianghe Deng, Yun Ding, Jason W. Dodson, David T. Fosbenner, Enoch N. Gao, Taylor L. Graham, Todd L. Graybill, Karen Ingraham, Walter P. Johnson, Bryan W. King, Christopher R. Kwiatkowski, Joël Lelièvre, Yue Li, Xiaorong Liu, Quinn Lu, Ruth Lehr, Alfonso Mendoza-Losana, John Martin, Lynn McCloskey, Patti McCormick, Heather P. O’Keefe, Thomas O’Keeffe, Christina Pao, Christopher B. Phelps, Hongwei Qi, Keith Rafferty, Genaro S. Scavello, Matt S. Steiginga, Flora S. Sundersingh, Sharon M. Sweitzer, Lawrence M. Szewczuk, Amy Taylor, May Fern Toh, Juan Wang, Minghui Wang, Devan J. Wilkins, Bing Xia, Gang Yao, Jean Zhang, Jingye Zhou, Christine P. Donahue, Jeffrey A. Messer, David Holmes, Christopher C. Arico-Muendel, Andrew J. Pope, Jeffrey W. Gross, Ghotas Evindar
Publikováno v:
Nature Communications, Vol 9, Iss 1, Pp 1-1 (2018)
Nature Communications 8: Article number: 16081 (2017); Published: 17 July 2017, Updated: 13 July 2018 The original version of this Article omitted the following from the Acknowledgements: ‘We thank Robert Kirkpatrick for implementing the high throu
Externí odkaz:
https://doaj.org/article/ee8d0f7b2ad14f48b638c180d558c296
Autor:
Yong Jiang, Tia Lewis, Patricia M. McCormick, Michael Schaber, Beth Pietrak, Rachel D. Totoritis, Marc A. Holbert, Lawrence M. Szewczuk, Daniel Fornwald, William G. Bonnette, Geoffrey Quinque, Maggie Grimes, Rosalie E. Matico, Ed Dul, Randy K. Bledsoe, Derrick W. Meinhold, Stephanie Chen
Publikováno v:
Scientific Reports, Vol 9, Iss 1, Pp 1-11 (2019)
Scientific Reports
Scientific Reports
Significant resource is spent by drug discovery project teams to generate numerous, yet unique target constructs for the multiple platforms used to drive drug discovery programs including: functional assays, biophysical studies, structural biology, a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1b0cbe26de02a861c13c08b95ac2b93
http://link.springer.com/article/10.1038/s41598-019-49149-2
http://link.springer.com/article/10.1038/s41598-019-49149-2
Autor:
Mary Ann Hardwicke, Hong Lin, Karl F. Erhard, John D. Martin, Ren Xie, Kaushik Raha, Rosanna Tedesco, Jin Zeng, Yanqiu Qian, Patricia M. Kratz, Yong Jiang, Ted Cecconie, Stan F. Martens, Angela Smallwood, Patrick McDevitt, James F. Mack, Baoguang Zhao, Stephenie B. Chen, Anthony J. Jurewicz, Juan I. Luengo, Mark J. Schulz, Nino Campobasso, Catherine A. Oleykowski, Lawrence M. Szewczuk, Alan R. Rendina, Cynthia M. Rominger, Benjamin J. Schwartz, Leng Nickels, Junya Qu, Jacques Briand
Publikováno v:
ACS Medicinal Chemistry Letters. 7:217-222
A novel series of potent and selective hexokinase 2 (HK2) inhibitors, 2,6-disubstituted glucosamines, has been identified based on HTS hits, exemplified by compound 1. Inhibitor-bound crystal structures revealed that the HK2 enzyme could adopt an "in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aec5386353626ba6f7f23a2d64607cd6
https://doi.org/10.1021/acsmedchemlett.5b00214
https://doi.org/10.1021/acsmedchemlett.5b00214
Autor:
Jeffrey A. Messer, Yun Ding, Jianghe Deng, Paolo A. Centrella, Todd L. Graybill, Jean Zhang, Patti McCormick, Carl A. Machutta, Robert H. Bates, John Martin, Joël Lelièvre, Quinn Lu, Jingye Zhou, Alfonso Mendoza-Losana, Xiaopeng Bai, Christopher S. Kollmann, David J. Holmes, Keith Rafferty, Christina S. Pao, Christopher C. Arico-Muendel, Heather O’Keefe, Aaron Coffin, Taylor L. Graham, David Barros-Aguirre, Sandy Chang, Christopher P. Davie, Hongwei Qi, Flora S. Sundersingh, Minghui Wang, Karen A. Ingraham, Jing Chai, Thomas O’Keeffe, Juan Wang, Gang Yao, Lluis Ballell, Jianzhong Huang, Anthony E. Choudhry, Bryan W. King, Andrew J. Pope, Ghotas Evindar, Xiaorong Liu, May Fern Toh, Christine Patricia Donahue, Jeffrey W. Gross, Pan F. Chan, Walter P. Johnson, Ruth Lehr, Hongfeng Deng, Kenneth E Lind, Matt S. Steiginga, Jason W. Dodson, Gurdyal S. Besra, Amy N. Taylor, Devan J. Wilkins, Yue Li, Lawrence M. Szewczuk, Svetlana L. Belyanskaya, Genaro S. Scavello, Sharon Sweitzer, Christopher R. Kwiatkowski, Lynn McCloskey, Bing Xia, Enoch Gao, Christopher B. Phelps, David T. Fosbenner
Publikováno v:
Nature Communications, Vol 9, Iss 1, Pp 1-1 (2018)
Nature Communications 8: Article number: 16081 (2017); Published: 17 July 2017, Updated: 13 July 2018 The original version of this Article omitted the following from the Acknowledgements: ‘We thank Robert Kirkpatrick for implementing the high throu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d87eaf46a6638b2650fa3a4f95e4cf2b
https://doi.org/10.1038/ncomms16227
https://doi.org/10.1038/ncomms16227
Autor:
William G. Bonnette, Jeffrey W. Gross, Geoffrey Quinque, Ann F. Hoffman, Lawrence M. Szewczuk, Yong Jiang, Marc A. Holbert
Publikováno v:
Analytical biochemistry. 559
Aggregated compounds can promiscuously and nonspecifically associate with proteins resulting in either false inhibition or activation of many different protein target classes. We developed a high-content imaging assay in a 384-well format using fluor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5747e7249f452482c34062338b410b7
https://pubmed.ncbi.nlm.nih.gov/30142329
https://pubmed.ncbi.nlm.nih.gov/30142329
Autor:
Wangfang Hou, Thomas D. Meek, Kyung O. Johanson, Xuan Hong, Taylor I Graham, Mui H Cheung, Edward Dul, Sunny T Hung, Allen Oliff, Lawrence M. Szewczuk, Robert B. Kirkpatrick, Thau F. Ho, John J. Kerrigan, Tia Lewis, Martin Brandt, Christopher S. Jones, Sanjay Kumar, Benjamin J. Schwartz, Hong Zhang, Da-Yuan Wang, Patricia M. McCormick, Amber D Harper-Jones
Publikováno v:
ASSAY and Drug Development Technologies. 11:308-325
Small ubiquitin-like modifier (SUMO) belongs to the family of ubiquitin-like proteins (Ubls) that can be reversibly conjugated to target-specific lysines on substrate proteins. Although covalently sumoylated products are readily detectible in gel-bas
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc91df0d4f9ac3d7c5264ef039275fed
https://doi.org/10.1089/adt.2012.501
https://doi.org/10.1089/adt.2012.501
Autor:
Todd L. Graybill, John D. Martin, Jason W. Dodson, Hongfeng Deng, Christopher P. Davie, Christopher C. Arico-Muendel, Minghui Wang, Hongwei Qi, Sandy S. Chang, David J. Holmes, Karen A. Ingraham, Kenneth E Lind, Heather O’Keefe, Carl A. Machutta, David Barros-Aguirre, Christine Patricia Donahue, Christina S. Pao, Jeffrey W. Gross, Ghotas Evindar, Jean Zhang, Bing Xia, Juan Wang, Patti McCormick, Xiaorong Liu, Jianzhong Huang, Joël Lelièvre, Quinn Lu, Pan F. Chan, Matt S. Steiginga, Lynn McCloskey, Christopher S. Kollmann, Taylor L. Graham, Xiaopeng Bai, Jing Chai, Yue Li, Walter P. Johnson, Ruth Lehr, Lawrence M. Szewczuk, Jingye Zhou, Lluis Ballell, Genaro S. Scavello, Robert H. Bates, Anthony E. Choudhry, Aaron Coffin, Sharon Sweitzer, Christopher R. Kwiatkowski, Andrew J. Pope, Enoch Gao, Christopher B. Phelps, David T. Fosbenner, Keith Rafferty, Thomas O’Keeffe, Gang Yao, Bryan W. King, Svetlana L. Belyanskaya, May Fern Toh, Gurdyal S. Besra, Amy N. Taylor, Devan J. Wilkins, Alfonso Mendoza-Losana, Paolo A. Centrella, Flora S. Sundersingh, Jeffrey A. Messer, Yun Ding, Jianghe Deng
Publikováno v:
Nature Communications
Nature Communications, Vol 8, Iss 1, Pp 1-11 (2017)
Nature Communications, Vol 8, Iss 1, Pp 1-11 (2017)
The identification and prioritization of chemically tractable therapeutic targets is a significant challenge in the discovery of new medicines. We have developed a novel method that rapidly screens multiple proteins in parallel using DNA-encoded libr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fd5399c3ed244a244dc84c19085f169
https://pubmed.ncbi.nlm.nih.gov/30004092
https://pubmed.ncbi.nlm.nih.gov/30004092
Autor:
William J. Drury, Mary Katherine Tarrant, Vedangi Sample, Philip A. Cole, Jin Zhang, Lawrence M. Szewczuk
Publikováno v:
Biochemistry. 47:10407-10419
Melatonin is a key circadian rhythm hormone that is produced in a diurnal pattern, driven by changes in the level of the biosynthetic enzyme serotonin N-acetyltransferase [arylalkylamine N-acetyltransferase (AANAT)]1 (1, 2). The neuroendocrine networ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11fea474c67b67e7ccc4a8bbf4904dbe
https://doi.org/10.1021/bi801189d
https://doi.org/10.1021/bi801189d