Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Paul G Leonard"'
Autor:
Cindy Benod, Rosa Villagomez, Carly S Filgueira, Peter K Hwang, Paul G Leonard, Guillaume Poncet-Montange, Senapathy Rajagopalan, Robert J Fletterick, Jan-Åke Gustafsson, Paul Webb
Publikováno v:
PLoS ONE, Vol 9, Iss 6, p e99440 (2014)
Nuclear receptors (NRs) are an important group of ligand-dependent transcriptional factors. Presently, no natural or synthetic ligand has been identified for a large group of orphan NRs. Small molecules to target these orphan NRs will provide unique
Externí odkaz:
https://doaj.org/article/137a4a00219b404e842bee770fbb9ed8
Autor:
Kevin G. Hicks, Ahmad A. Cluntun, Heidi L. Schubert, Sean R. Hackett, Jordan A. Berg, Paul G. Leonard, Mariana A. Ajalla Aleixo, Youjia Zhou, Alex J. Bott, Sonia R. Salvatore, Fei Chang, Aubrie Blevins, Paige Barta, Samantha Tilley, Aaron Leifer, Andrea Guzman, Ajak Arok, Sarah Fogarty, Jacob M. Winter, Hee-Chul Ahn, Karen N. Allen, Samuel Block, Iara A. Cardoso, Jianping Ding, Ingrid Dreveny, William C. Gasper, Quinn Ho, Atsushi Matsuura, Michael J. Palladino, Sabin Prajapati, Pengkai Sun, Kai Tittmann, Dean R. Tolan, Judith Unterlass, Andrew P. VanDemark, Matthew G. Vander Heiden, Bradley A. Webb, Cai-Hong Yun, Pengkai Zhao, Bei Wang, Francisco J. Schopfer, Christopher P. Hill, Maria Cristina Nonato, Florian L. Muller, James E. Cox, Jared Rutter
Publikováno v:
Science
Metabolic networks are interconnected and influence diverse cellular processes. The protein-metabolite interactions that mediate these networks are frequently low affinity and challenging to systematically discover. We developed mass spectrometry int
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::352755dceffe88559d81ce00a2f38a1e
https://doi.org/10.1126/science.abm3452
https://doi.org/10.1126/science.abm3452
Autor:
Nancy E. Kohl, Zhijun Kang, Connor A. Parker, Yuting Sun, Yongying Jiang, Simon S. Yu, Cross Jason, Ningping Feng, Faika Mseeh, Timothy McAfoos, Maria Emilia Di Francesco, Timothy P. Heffernan, Angela L. Harris, Brooke A. Meyers, Paul G. Leonard, Joseph R. Marszalek, Christopher C. Williams, Qi Wu, Jeffrey J. Kovacs, Pijus K. Mandal, Jason P Burke, Giulio Draetta, Barbara Czako, Philip Jones, Christopher Carroll
Publikováno v:
Journal of Medicinal Chemistry. 64:15141-15169
Src homology 2 (SH2) domain-containing phosphatase 2 (SHP2) plays a role in receptor tyrosine kinase (RTK), neurofibromin-1 (NF-1), and Kirsten rat sarcoma virus (KRAS) mutant-driven cancers, as well as in RTK-mediated resistance, making the identifi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::52237ec958405671436618b3a028bf48
https://doi.org/10.1021/acs.jmedchem.1c01132
https://doi.org/10.1021/acs.jmedchem.1c01132
Autor:
Norma Rogers, Stephan Krapp, Faika Mseeh, Richard T. Lewis, Keith Mikule, Michelle Han, Jay Theroff, Yongying Jiang, Keith M. Wilcoxen, Cross Jason, Dana Pfaffinger, Michael J. Soth, Paul G. Leonard, Philip Jones, Pijus K. Mandal, Angela L. Harris, Martin R. Tremblay, Simon S. Yu, Jason P Burke, Connor A. Parker, Barbara Czako, Alessia Petrocchi, Naphtali J. Reyna, Joseph R. Marszalek, Matthew M. Hamilton, Timothy McAfoos, Brett W. Virgin-Downey, Graham Trevitt, Alfred Lammens, Alan Xu
Publikováno v:
Journal of Medicinal Chemistry. 64:11302-11329
Indoleamine 2,3-dioxygenase 1 (IDO1), a heme-containing enzyme that mediates the rate-limiting step in the metabolism of l-tryptophan to kynurenine, has been widely explored as a potential immunotherapeutic target in oncology. We developed a class of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec33cf6551a670d4d40eaab2894a6f60
https://doi.org/10.1021/acs.jmedchem.1c00679
https://doi.org/10.1021/acs.jmedchem.1c00679
Autor:
Xiaobo Wang, Jeffrey J. Ackroyd, Yongying Jiang, Florian L. Muller, Yuting Sun, Federica Pisaneschi, Theresa Tran, Nikunj Satani, Cong-Dat Pham, Waldemar Priebe, Barbara Czako, Qi Wu, Paul G. Leonard, Ronald A. DePinho, Joseph R. Marszalek, John M. Asara, Pijus K. Mandal, Yasaman Barekatain, Susana Castro Pando, William G. Bornmann, Rafal Zielinski, Naima Hammoudi, Sunada Khadka, David Maxwell, Kenisha Arthur, Yu Hsi Lin, Quanyu Xu, Dimitra K. Georgiou, Victoria C. Yan, Zhijun Kang, Zhenghong Peng
Publikováno v:
Nature metabolism
Inhibiting glycolysis remains an aspirational approach for the treatment of cancer. We have previously identified a subset of cancers harbouring homozygous deletion of the glycolytic enzyme enolase (ENO1) that have exceptional sensitivity to inhibiti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20ad9fc9f1e815ba077a140b6ba621df
https://doi.org/10.1038/s42255-020-00313-3
https://doi.org/10.1038/s42255-020-00313-3
Autor:
Timothy P. Heffernan, Angela L. Harris, Martin R. Tremblay, Connor A. Parker, Yongying Jiang, Robert A. Mullinax, Cross Jason, Jihai Pang, Qi Wu, Edward Q. Chang, Sonal Gera, Keith M. Wilcoxen, Paul G. Leonard, Zhen Liu, Jeffrey J. Kovacs, Erika Suzuki, Barbara Czako, Ningping Feng, Joseph R. Marszalek, Nakia D. Spencer, Pijus K. Mandal, Jason P Burke, Simon S. Yu, Keith Mikule, Faika Mseeh, Philip Jones, Giulio Draetta
Publikováno v:
Journal of Medicinal Chemistry. 63:9888-9911
Tumor-associated macrophages (TAMs) have a significant presence in the tumor stroma across multiple human malignancies and are believed to be beneficial to tumor growth. Targeting CSF1R has been proposed as a potential therapy to reduce TAMs, especia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::477eb096ec2e1d0be3af1800c7acd0a9
https://doi.org/10.1021/acs.jmedchem.0c00936
https://doi.org/10.1021/acs.jmedchem.0c00936
Autor:
Yi Li, Haiying Chen, Bing Tian, Pingyuan Wang, Paul G. Leonard, Allan R. Brasier, Zhiqing Liu, Eric A. Wold, Sarah Joseph, Jia Zhou
Publikováno v:
J Med Chem
Bromodomain-containing protein 4 (BRD4) represents a promising drug target for anti-inflammatory therapeutics. Herein, we report the design, synthesis, and pharmacological evaluation of novel chromone derivatives via scaffold hopping to discover a ne
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efe91a085c18f561ec1afa0cf5547c25
https://doi.org/10.1021/acs.jmedchem.0c00035
https://doi.org/10.1021/acs.jmedchem.0c00035
Autor:
Zhiqing Liu, Yi Li, Haiying Chen, Hsien-Tsung Lai, Pingyuan Wang, Shwu-Yuan Wu, Eric A. Wold, Paul G. Leonard, Sarah Joseph, Haitao Hu, Cheng-Ming Chiang, Allan R. Brasier, Bing Tian, Jia Zhou
Publikováno v:
J Med Chem
Bromodomain-containing protein 4 (BRD4) is an emerging epigenetic drug target for intractable inflammatory disorders. The lack of highly selective inhibitors among BRD4 family members has stalled the collective understanding of this critical system a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c045f0d6c993fde71c5af9e8db998b5
https://pubmed.ncbi.nlm.nih.gov/34982556
https://pubmed.ncbi.nlm.nih.gov/34982556
Autor:
Barbara, Czako, Yuting, Sun, Timothy, McAfoos, Jason B, Cross, Paul G, Leonard, Jason P, Burke, Christopher L, Carroll, Ningping, Feng, Angela L, Harris, Yongying, Jiang, Zhijun, Kang, Jeffrey J, Kovacs, Pijus, Mandal, Brooke A, Meyers, Faika, Mseeh, Connor A, Parker, Simon S, Yu, Christopher C, Williams, Qi, Wu, Maria Emilia, Di Francesco, Giulio, Draetta, Timothy, Heffernan, Joseph R, Marszalek, Nancy E, Kohl, Philip, Jones
Publikováno v:
Journal of medicinal chemistry. 64(20)
Src homology 2 (SH2) domain-containing phosphatase 2 (SHP2) plays a role in receptor tyrosine kinase (RTK), neurofibromin-1 (NF-1), and Kirsten rat sarcoma virus (KRAS) mutant-driven cancers, as well as in RTK-mediated resistance, making the identifi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ef1c5b3d344a33f3d6564080b26ff7f2
https://pubmed.ncbi.nlm.nih.gov/34643390
https://pubmed.ncbi.nlm.nih.gov/34643390
Autor:
Alessandro Carugo, Robert A. Mullinax, Mary Geck Do, Meredith A. Miller, Virginia Giuliani, Qing Chang, Giulio Draetta, John M. Asara, Sahil Seth, Melinda Smith, Norma Rogers, Joseph R. Marszalek, Jing Han, Philip Jones, Paul G. Leonard, Trang N. Tieu, Yongying Jiang, Brooke A. Meyers, Ronald A. DePinho, Timothy P. Heffernan, Michael Peoples, Marc O. Warmoes, Barbara Czako, Ningping Feng, Carlo Toniatti, Lili Miao, Xi Shi, Yuting Sun, Xiaoyan Ma, Florian L. Muller, Christopher A. Bristow, Wylie S. Palmer, Madhavi Bandi, Shuping Zhao, Faika Mseeh, Pietro Morlacchi, Philip L. Lorenzi, Timothy Lofton
Publikováno v:
Cell Reports, Vol 26, Iss 2, Pp 469-482.e5 (2019)
Summary: The plasticity of a preexisting regulatory circuit compromises the effectiveness of targeted therapies, and leveraging genetic vulnerabilities in cancer cells may overcome such adaptations. Hereditary leiomyomatosis renal cell carcinoma (HLR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::35e500f8c834bef5282453e6ef86d304
http://www.sciencedirect.com/science/article/pii/S2211124718319739
http://www.sciencedirect.com/science/article/pii/S2211124718319739