Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Lina Setti"'
Autor:
Sharadha Subramanian, Valery Polyakov, Giordano Caponigro, Amy Lambert, Lina Setti, Ann Van Abbema, Nicholas Keen, Matthew Burger, Mallika Singh, Emma Lees, Michael Patrick Dillon, Alice Rico, Wenlin Shao, Mohamad Hekmat-Nejad, Lesley A. Mathews Griner, Stacey Rivera, Robert J. Aversa, William R. Sellers, Victor Tamez, Joshua M. Korn, Lifeng Wan, Yan Lou, Benjamin R. Taft, Payman Amiri, Savithri Ramurthy, Richard Zang, Darrin Stuart, Jacob R. Haling, Yuji Mishina, Fang Shen, Giselle Nishiguchi, Yun Feng, John Tellew, Vesselina G. Cooke
Publikováno v:
Cancer Research. 78:DDT01-04
The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at multiple nodes, the most prevalent of which are mutations in RAS or BRAF. While BRAFV600 mutant tumors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::76907a35f9f8efc44acd72426349c320
https://doi.org/10.1158/1538-7445.am2018-ddt01-04
https://doi.org/10.1158/1538-7445.am2018-ddt01-04
Autor:
Stephen Basham, Brent A. Appleton, Rama Jain, Lina Setti, Savithri Ramurthy, Paul Feucht, Jiong Lan, Anne B. Jefferson, Laura Doyle, Bob Warne, Mika Lindvall, Sharadha Subramanian, Gordana Atallah, Michelle Mathur, Abran Costales, Cynthia M. Shafer
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(19)
Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and additional hydrophobic contacts yielded the azaindole series which exhibited potent, picomolar RSK2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2f1f7be087371238d9479060ac06a29
https://pubmed.ncbi.nlm.nih.gov/30170943
https://pubmed.ncbi.nlm.nih.gov/30170943
Autor:
Anne B. Jefferson, Lina Setti, Mika Lindvall, Savithri Ramurthy, Stephen Basham, Bob Warne, Laura Doyle, Rama Jain, Brent A. Appleton, Paul Feucht, Cynthia M. Shafer, Sharadha Subramanian, Gordana Atallah, Abran Costales, Jiong Lan, Michelle Mathur
Publikováno v:
Journal of Medicinal Chemistry. 58:6766-6783
While the p90 ribosomal S6 kinase (RSK) family has been implicated in multiple tumor cell functions, the full understanding of this kinase family has been restricted by the lack of highly selective inhibitors. A bis-phenol pyrazole was identified fro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8c94f318909b498d62abc06bd4b2219
https://doi.org/10.1021/acs.jmedchem.5b00450
https://doi.org/10.1021/acs.jmedchem.5b00450
Autor:
Yan Lou, Sharadha Subramanian, Yingyun Wang, Lifeng Wan, John Tellew, Laura Tandeske, Benjamin R. Taft, Kalyani Gampa, Jacob R. Haling, Gisele Nishiguchi, Lina Setti, Alice Rico, Sylvia Ma, Payman Amiri, Mallika Singh, Huw Tanner, Brent A. Appleton, Robert J. Aversa, Sepideh Vaziri, Shenlin Huang, Johanna M. Jansen, Anne Van Abbema, Jing Yuan, Vesselina G. Cooke, Hanne Merritt, Aaron Smith, Wenlin Shao, Valery Polyakov, Fei Feng, Savithri Ramurthy, Matthew Burger, Mulugeta Mamo, Lesley A. Mathews Griner, Vijay Sethuraman, Victoriano Tamez, Michael Patrick Dillon, Emma Lees, Ina Dix, Paul A. Barsanti, Richard Zang, Darrin Stuart, Mohammad Hekmat-Nejad
Publikováno v:
Journal of medicinal chemistry. 60(12)
RAS oncogenes have been implicated in30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant tumors has been established in genetically engineered mouse models and human tumor cells. To d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2623e531b4911ee04267b3f1e132c67
https://pubmed.ncbi.nlm.nih.gov/28557458
https://pubmed.ncbi.nlm.nih.gov/28557458
Autor:
Sharadha Subramanian, Anne B. Jefferson, Ida Aronchik, Cynthia M. Shafer, Paul Feucht, Gordana Atallah, Elizabeth Ornelas, Abran Costales, Bob Warne, Mika Lindvall, Michelle Mathur, Lina Setti, Brent A. Appleton, Laura Doyle, Rama Jain, Stephen Basham, Jiong Lan, Savithri Ramurthy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1592-1596
2-Amino-7-substituted benzoxazole analogs were identified by HTS as inhibitors of RSK2. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of improving in vitro and target modulation po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08c69ff2547aba8e408f17b8304fdf63
https://doi.org/10.1016/j.bmcl.2014.01.058
https://doi.org/10.1016/j.bmcl.2014.01.058
Autor:
Ann C. Petersen, Andreas Jekle, David Mark Rotstein, André deRosier, Remy Lemoine, Changhua Ji, Gabrielle Heilek, Lina Setti, Pamela Berry
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4753-4756
The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd9c7f3af9705e82d96ddf190e20a495
https://doi.org/10.1016/j.bmcl.2010.06.135
https://doi.org/10.1016/j.bmcl.2010.06.135
Autor:
David Mark Rotstein, André deRosier, Jutta Wanner, Gabrielle Heilek, Andreas Jekle, Changhua Ji, Lijing Chen, Remy Lemoine, Ann C. Petersen, Lina Setti
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1830-1833
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2dea64728384350b45a732bd5be9b2d2
https://doi.org/10.1016/j.bmcl.2010.02.004
https://doi.org/10.1016/j.bmcl.2010.02.004
Autor:
Cheng-I. Mau, Andreas Jekle, Ferenc Makra, Surya Sankuratri, Paul Weller, André deRosier, Eun Kyung Lee, Gabriel Stephen Deems, Gabrielle Heilek, David Mark Rotstein, Changhua Ji, Shelley K. Gleason, Christine E. Brotherton-Pleiss, Marianna Dioszegi, Lubov Filonova, Lina Setti, Pamela Berry, Alejandra Trejo-Martin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5401-5406
A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a12820458536333a16236817f9aa665
https://doi.org/10.1016/j.bmcl.2009.07.122
https://doi.org/10.1016/j.bmcl.2009.07.122
Autor:
Marcia Renzetti, Jones Philip Stephen, Ralph Garippa, Glyn Williams, Joseph A. Sergi, Ying Peng, Kevin Richard Guertin, Fiorenza Falcioni, Hilary A. Overton, Lida Qi, Rogely Boyce, Andrée R. Olivier, Karen Wang, Rachel M. Dunsdon, Mathew Taylor, Brian William Dymock, Lina Setti
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2895-2898
A novel series of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents have been identified. These compounds show non-selective inhibitory properties against a panel of protein tyrosine phosphatases including PTP1B. Comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a17384433d52272fadaa8c14dd8bbe1
https://doi.org/10.1016/s0960-894x(03)00623-1
https://doi.org/10.1016/s0960-894x(03)00623-1
Autor:
Lina Setti, Robert J. Aversa, Rama Jain, George Thomas, Savithri Ramurthy, Lorena Taricani, Robert Elling, Mark Knapp, Paul A. Barsanti, Yipin Lu, Matthew Cox, Michelle Mathur, Yue Pan, Xianming Jin, Patrick J Rudewicz, Cheng Hu, Michael Patrick Dillon, Qin Yue, Sharadha Subramanian, Jiong Lan, Linda Xiao
Compound 13 was discovered through morphing of the ATR biochemical HTS hit 1. The ABI series was potent and selective for ATR. Incorporation of a 6-azaindole afforded a marked increase in cellular potency but was associated with poor PK and hERG ion
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afedc70e6a8e79dca0042a4913c70c0a
https://europepmc.org/articles/PMC4291699/
https://europepmc.org/articles/PMC4291699/
