Zobrazeno 1 - 10
of 55
pro vyhledávání: '"Michael Sabio"'
Autor:
Sajedeh, Lotfaliansaremi, Stephen, Cornwell, Candice, Casillas, Michael, Sabio, Peter, Tolias, William, Windsor, Sunil, Paliwal
Publikováno v:
Chemical Biology & Drug Design. 101:837-847
Oncology clinical development programs have targeted the RAS/RAF/MEK/ERK signaling pathway with small molecule inhibitors for a variety of cancers during the past decades, and most therapies have shown limited or minimal success. Specific BRAF and ME
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f89b3f85c6cd332c9de408a81d14f885
https://doi.org/10.1111/cbdd.14186
https://doi.org/10.1111/cbdd.14186
Publikováno v:
Medical Research Archives. 8
The Ras-ERK mitogen-activated protein kinase (MAPK) pathway is hyperactive in >30% of all human cancers, prompting the development of RAS, RAF, MEK, and ERK inhibitors. The identification of intracellular signaling cascades, which promote the growth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a9b83296ccfcc96a02f4f4886084011a
https://doi.org/10.18103/mra.v8i4.2086
https://doi.org/10.18103/mra.v8i4.2086
Autor:
Haoshuang Zhao, Naoko Tanaka, Wei Chu, Ueli Gubler, Michael Sabio, Sid Topiol, Peter Tolias, Kuo-Sen Huang
Publikováno v:
Medical Research Archives. 8
By analyzing KRas and HRas X-ray structures, we developed a novel strategy that involves the design of a series of “synthetic” or “artificial” KRas mutations, namely T20I, D57E, D57F, T58A, T58V, and G60A, individually introduced into KRas wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1d3a7ef86a5542a4ecce2db002202124
https://doi.org/10.18103/mra.v8i6.2137
https://doi.org/10.18103/mra.v8i6.2137
Autor:
Michael Sabio, Sid Topiol
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:484-494
We illustrate, with a focus on mGluR5, how the recently published, first X-ray structures of mGluR 7TM domains, specifically those of mGluR1 and mGluR5 complexed with negative allosteric modulators (NAMs), will begin to influence ligand- (e.g., drug-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0425e8568bd22c2a1d9ed7b7d5495d2c
https://doi.org/10.1016/j.bmcl.2015.11.087
https://doi.org/10.1016/j.bmcl.2015.11.087
Publikováno v:
The FASEB Journal. 34:1-1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d1b48a7f1832644316bc36a27d1c152d
https://doi.org/10.1096/fasebj.2020.34.s1.02433
https://doi.org/10.1096/fasebj.2020.34.s1.02433
Autor:
Abhishek Sharma, Benita S. Katzenellenbogen, Michael Sabio, Sarat Chandarlapaty, Geoffrey L. Greene, Christopher G. Mayne, Shengjia Lin, Kathryn E. Carlson, John A. Katzenellenbogen, Jian Min, Valeria Sanabria Guillen, Naina Sharma, Weiyi Toy
A major risk for patients having estrogen receptor α (ERα)-positive breast cancer is the recurrence of drug-resistant metastases after initial successful treatment with endocrine therapies. Recent studies have implicated a number of activating muta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dce9b01261f6c80da30ddf31402d6323
https://europepmc.org/articles/PMC6469989/
https://europepmc.org/articles/PMC6469989/
Autor:
Michael Sabio, Sid Topiol
X-ray structures for ligand-modulated GPCRs were not available until 2007 and were limited to class A GPCRs. The recent availability of X-ray structures for mGluR5, a class C GPCR, provides a valuable tool for understanding drug action. For mGluR5, p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5c805a228c10efa45d28b4342e00e098
https://doi.org/10.1016/bs.aiq.2017.03.003
https://doi.org/10.1016/bs.aiq.2017.03.003
Autor:
Noel J. Boyle, Jessie Weiss, Gamini Chandrasena, Lingyun Wu, Andrew D. White, Dario Doller, Michael Sabio, John M. Peterson, Eman Edelmenky, Rajinder Bhardwaj, Xinyan Huang, Chien An Chen, Jiang Yu, Burns James Ford, Bin Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1458-1461
The NPY5 receptor binding and pharmacokinetic properties of a novel series of cis-1-oxo-heterocyclyl-4-amido-cyclohexane derivatives are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f150a8e5e1c03e2d0966895d4d5e9256
https://doi.org/10.1016/j.bmcl.2014.02.023
https://doi.org/10.1016/j.bmcl.2014.02.023
Autor:
Manuel Cajina, Megan Nattini, Michael Sabio, Michael S. Reitman, Dario Doller, Kevin G. Liu, Maria D. Bacolod, Hermogenes N. Jimenez, Sang-Phyo Hong, Michelle A. Uberti
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3235-3239
4-(1-Phenyl-1H-pyrazol-4-yl)quinoline (1) was identified by screening the Lundbeck compound collection, and characterized as having mGlu4 receptor positive allosteric modulator properties. Compound 1 is selective over other mGlu receptors and a panel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b69b52a2908d3eaca5c8afd4f35dc6a
https://doi.org/10.1016/j.bmcl.2012.03.032
https://doi.org/10.1016/j.bmcl.2012.03.032
Autor:
Poda Suresh Babu, Michelle A. Uberti, Arun Ranganathn, Michael Sabio, Claus T. Christoffersen, Veena Menon, Vincent H. Jorgensen, Kenneth A. Jones
Publikováno v:
ASSAY and Drug Development Technologies. 6:787-794
A luminescence assay using a new plate reader, the LumiLux (PerkinElmer, Waltham, MA), has been validated for high-throughput screening (HTS). In this study, we compared the aequorin luminescence-based calcium mobilization assay to the fluorescence-b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b2671105a552d9b37d214aa7192ea90
https://doi.org/10.1089/adt.2008.157
https://doi.org/10.1089/adt.2008.157