Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Eve Irene Lepist"'
Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF
Autor:
Martin L. Decaris, Johanna R. Schaub, Chun Chen, Jacob Cha, Gail G. Lee, Megi Rexhepaj, Steve S. Ho, Vikram Rao, Megan M. Marlow, Prerna Kotak, Erine H. Budi, Lisa Hooi, Jianfeng Wu, Marina Fridlib, Shamra P. Martin, Shaoyi Huang, Ming Chen, Manuel Muñoz, Timothy F. Hom, Paul J. Wolters, Tushar J. Desai, Fernando Rock, Katerina Leftheris, David J. Morgans, Eve-Irene Lepist, Patrick Andre, Eric A. Lefebvre, Scott M. Turner
Publikováno v:
Respiratory Research, Vol 22, Iss 1, Pp 1-14 (2021)
Abstract Rationale αv integrins, key regulators of transforming growth factor-β activation and fibrogenesis in in vivo models of pulmonary fibrosis, are expressed on abnormal epithelial cells (αvβ6) and fibroblasts (αvβ1) in fibrotic lungs. Obj
Externí odkaz:
https://doaj.org/article/f75a5266ef724db48db905d69406f78e
Autor:
Adrian Tomkinson, Gary Phillips, Jayaraman Chandrasekhar, Nicholas Alexander Till, Leena Patel, Jia Hao, Jennifer Treiberg, Joseph Therrien, Kathleen S. Keegan, Mary E. McGrath, Sedillo Kassandra F, Fatima Arjmand, Yelena Zherebina, Stephane Perreault, David Koditek, Clinton K. Matson, Eve-Irene Lepist
Publikováno v:
ACS Med Chem Lett
[Image: see text] A series of PI3Kβ selective inhibitors derived from a novel 4-(1H-benzo[d]imidazol-1-yl)quinoline chemotype has been rationally designed. Crucial to achieving the desired selectivity over the other class I PI3K isoforms, including
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::141717e365da34c534fb82eddbca0b95
https://doi.org/10.1021/acsmedchemlett.0c00095
https://doi.org/10.1021/acsmedchemlett.0c00095
Dual inhibition of αvβ6 and αvβ1 reduces fibrogenesis in lung tissue explants from patients with IPF
Autor:
Patrick Andre, Martin Decaris, Chun Chen, Munoz Manuel, Hom Timothy, Scott M. Turner, Ming Chen, Tushar J. Desai, Megan M. Marlow, Cha Jacob, Eric Lefebvre, Steve S. Ho, Paul J. Wolters, Shaoyi Huang, Eve-Irene Lepist, Katerina Leftheris, David J Morgans, Lisa Hooi, Johanna R. Schaub, Vikram R. Rao, Jianfeng Wu, Marina Fridlib, Fernando Rock, Megi Rexhepaj, Erine H. Budi, Prerna Kotak, Gail Lee, Shamra Martin
Publikováno v:
Respiratory research, vol 22, iss 1
Respiratory Research, Vol 22, Iss 1, Pp 1-14 (2021)
Respiratory Research, Vol 22, Iss 1, Pp 1-14 (2021)
Rationale αv integrins, key regulators of transforming growth factor-β activation and fibrogenesis in in vivo models of pulmonary fibrosis, are expressed on abnormal epithelial cells (αvβ6) and fibroblasts (αvβ1) in fibrotic lungs. Objectives W
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8943da51a8a3553a1e3711bc9a9ed07
https://escholarship.org/uc/item/5q12m0vq
https://escholarship.org/uc/item/5q12m0vq
Autor:
Eve-Irene Lepist, Hunter Gillies, William Smith, Jia Hao, Cassandra Hubert, Robert L St Claire, Kenneth R Brouwer, Adrian S Ray
Publikováno v:
PLoS ONE, Vol 9, Iss 1, p e87548 (2014)
Inhibition of the transporter-mediated hepatobiliary elimination of bile salts is a putative mechanism for liver toxicity observed with some endothelin receptor antagonists (ERAs).Sandwich-cultured human hepatocytes were used to study the hepatobilia
Externí odkaz:
https://doaj.org/article/c42eeeca463f467d81ac31d4e10c3353
Autor:
Adrian S. Ray, Eve-Irene Lepist
Publikováno v:
Expert Opinion on Drug Metabolism & Toxicology. 13:1075-1087
Membrane transport proteins play a central role in regulating the disposition of endobiotics, dietary nutrients and environmental toxins. The inhibition of transporters by drugs has potential physiologic consequences. The full extent of the effect of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f589a07244478e7220c20b5cc252fd2
https://doi.org/10.1080/17425255.2017.1372425
https://doi.org/10.1080/17425255.2017.1372425
Autor:
Eduard Gorina, Johanna R. Schaub, Chun Chen, Fernando Rock, Martin Decaris, Scott Turner, Eric Lefebvre, Eve Irene Lepist
Publikováno v:
Idiopathic interstitial pneumonias.
Integrins αVβ6 and αVβ1 are cell surface proteins that bind to and activate latent TGF-β, resulting in SMAD phosphorylation and pro-fibrotic gene expression. In IPF, both integrins are upregulated in the lung and are thought to play a role in th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b8b517cd46c67bff686b0a8d62ec35c8
https://doi.org/10.1183/13993003.congress-2019.pa1298
https://doi.org/10.1183/13993003.congress-2019.pa1298
Autor:
Elfatih Elzein, Cindy Hong Li, Daniel Soohoo, Britton Kenneth Corkey, Chandru Venkataramani, Xiao-Jun Li, Manoj C. Desai, Nesrine El-Bizri, Haibo Jiang, Kobayashi Tetsuya, Nevena Mollova, Sridharan Rajamani, Jason K. Perry, Arvinder Dhalla, Thao Perry, Xiaofen Li, Robert G. Strickley, Notte Gregory, Gerry Rhodes, Ryoko Hirakawa, Luiz Belardinelli, Eve-Irene Lepist, Parkhill Eric Q, Jeff Zablocki, Oliver L. Saunders, Lu Yafan, Rao Kalla, Dmitry Koltun, Cheng Xie, Gongxin Liu, Wei-Qun Wang, Kris M. Kahlig, Bernard P. Murray, Michael Graupe, Guerrero Juan A, Martinez Ruben, Mark Osier, Lufei Hu
Publikováno v:
Journal of Medicinal Chemistry. 59:9005-9017
Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4d94b0c7942e17b573ee6f2bc8434003
https://doi.org/10.1021/acs.jmedchem.6b00939
https://doi.org/10.1021/acs.jmedchem.6b00939
Autor:
Adrian S. Ray, Eve-Irene Lepist
Publikováno v:
The Journal of Clinical Pharmacology. 56:S73-S81
The kidney, through the distinct processes of passive glomerular filtration and active tubular secretion, plays an important role in the elimination of numerous endobiotics (eg, hormones, metabolites), toxins, nutrients, and drugs. Renal transport pa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7dc64185940c391486e4e58df96f994b
https://doi.org/10.1002/jcph.735
https://doi.org/10.1002/jcph.735
Autor:
Gary Phillips, Nikolai Novikov, Kamal D. Puri, Mary E. McGrath, Leena Patel, Carmen Ip, Arthur Yeung, Latesh Lad, Kirk L. Stevens, Musong Kim, Eve-Irene Lepist, Armando G. Villaseñor, Jayaraman Chandrasekhar, Joseph Therrien, Joshua Kaplan, Jerry Evarts, John R. Somoza, Aaron C. Haran, David Koditek, Stephane Perreault, Bart H. Steiner, Jennifer Treiberg
Publikováno v:
Journal of Medicinal Chemistry. 59:3532-3548
Inhibition of phosphoinositide 3-kinase δ (PI3Kδ) is an appealing target for several hematological malignancies and inflammatory diseases. Herein, we describe the discovery and optimization of a series of propeller shaped PI3Kδ inhibitors comprisi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bbe4b5b6b4c34240fb4472508c6868c
https://doi.org/10.1021/acs.jmedchem.6b00213
https://doi.org/10.1021/acs.jmedchem.6b00213
Autor:
Marilyn M. Giacomini, Xiaomin Liang, Huan-Chieh Chien, Meiling Piao, Jia Hao, Jolyn Twelves, Kathleen M. Giacomini, Eugene C. Chen, Sook Wah Yee, Eve-Irene Lepist, Adrian S. Ray
Publikováno v:
Molecular Pharmaceutics. 12:4301-4310
The biguanide metformin is widely used as first-line therapy for the treatment of type 2 diabetes. Predominately a cation at physiological pH's, metformin is transported by membrane transporters, which play major roles in its absorption and dispositi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bec0fa35f3b2922a8f751a6b23021bd2
https://doi.org/10.1021/acs.molpharmaceut.5b00501
https://doi.org/10.1021/acs.molpharmaceut.5b00501