Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Kelly E. Desino"'
Autor:
Kelly E. Desino, Balakrishna Hosmane, Stella Doktor, Edward Price, David A. Degoey, J. Cory Kalvass
Publikováno v:
Journal of Medicinal Chemistry. 64:9389-9403
Models intended to predict intestinal absorption are an essential part of the drug development process. Although many models exist for capturing intestinal absorption, many questions still exist around the applicability of these models to drug types
Autor:
Searle Xenia B, Wenqing Gao, Andrew M. Swensen, Timothy A. Vortherms, Hong Yong, Clinton Yeung, Corina Balut, Philip R. Kym, Yihong Fan, Ashvani K. Singh, Greszler Stephen N, Kelly E. Desino, Andrew Bogdan, Ying Jia, Chris Tse, Xueqing Wang, Bo Liu
Publikováno v:
Journal of Medicinal Chemistry. 61:1436-1449
Cystic fibrosis (CF) is a multiorgan disease of the lungs, sinuses, pancreas, and gastrointestinal tract that is caused by a dysfunction or deficiency of the cystic fibrosis transmembrane conductance regulator (CFTR) protein, an epithelial anion chan
Autor:
Richard McCarthy, Rebecca M. Edelmayer, Maria A. Argiriadi, Didier Bressac, Craig Wallace, Michael E. Kort, Yibing Wang, Laura Leys, Eric C. Breinlinger, J. Wetter, Zhi Su, Jean-Michel Luccarini, P. Honore, K. Salte, Philippe Masson, Christian Goess, Stephen B. Gauld, Kevin P. Cusack, Donna Gauvin, S. Huang, Dominique Potin, Sébastien Jacquet, S. McGaraughty, Kelly E. Desino
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 371(1)
Blockade of interleukin (IL)-23 or IL-17 with biologics is clinically validated as a treatment of psoriasis. However, the clinical impact of targeting other nodes within the IL-23/IL-17 pathway, especially with small molecules, is less defined. We re
Autor:
Soniya Vaidya, Phillip M. Gerk, Kenneth L. Audus, Abner N. Nyandege, Marie V. St-Pierre, Andrei M. Mikheev, Kelly E. Desino, Jashvant D. Unadkat, Anand A. Joshi
Publikováno v:
Pharmaceutical Research. 33:2847-2878
The human placenta fulfills a variety of essential functions during prenatal life. Several ABC transporters are expressed in the human placenta, where they play a role in the transport of endogenous compounds and may protect the fetus from exogenous
Autor:
Kara L. Queeney, Maria A. Argiriadi, Anil Vasudevan, Jürgen Dinges, Eric Dominguez, Kelly E. Desino, Christopher M. Harris, Grier A. Wallace, Tegest Kebede, Hetal Patel, Denise C. Perron
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2297-2302
Inhibition of sphingosine-1-phosphate lyase has recently been proposed as a potential treatment option for inflammatory disorders such as multiple sclerosis, rheumatoid arthritis, and inflammatory bowel disease. In this report we describe our hit-to-
Autor:
Susanne Winiwarter, Fabio Broccatelli, Holger Fischer, Rieko Arimoto, Carl Petersson, Christopher Keefer, Prashant V. Desai, Kelly E. Desino, Franco Lombardo
Publikováno v:
Journal of medicinal chemistry. 60(22)
In silico tools to investigate absorption, distribution, metabolism, excretion, and pharmacokinetics (ADME-PK) properties of new chemical entities are an integral part of the current industrial drug discovery paradigm. While many companies are active
Autor:
Salvatore Guccione, Mary L. Michaelis, Rona R. Ramsay, Rosario Pignatello, Kenneth L. Audus, Sabah Ansar, Livia Basile, Kelly E. Desino
Publikováno v:
Biochemical Pharmacology. 78:1412-1417
A variety of approaches have been taken to improve the brain penetration of pharmaceutical agents. The amphipathic character of a compound can improve its interaction with the lipid bilayer within cell membranes, and as a result improve permeability.
Autor:
Hanumaiah Telikepalli, Douglas R. Powell, Mary L. Michaelis, Emily A. Reiff, Gunda I. Georg, Sabah Ansar, Kelly E. Desino, Kenneth L. Audus, Richard H. Himes
Publikováno v:
Journal of Medicinal Chemistry. 52:7537-7543
Compounds that interact with microtubules, such as paclitaxel, have been shown to possess protective properties against beta-amyloid (Abeta) induced neurodegeneration associated with Alzheimer's disease. In this work, the novel agent (3R,5S,7as)-(3,5
Autor:
Haibo Ge, Gunda I. Georg, Sarah Güthe, Kelly E. Desino, Richard H. Himes, Anna Seelig, Veena Vasandani, Kenneth L. Audus, Jariat Oyetunji, Brandon J. Turunen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5971-5974
A focused library of TX-67 (C10 hemi-succinate) analogs has been prepared, including C7 regioisomers, esters, amides, and one-carbon homologs. These were prepared to investigate whether the lack of TX-67 interaction with P-glycoprotein (Pgp) is due t
Autor:
Kelly E. Desino, Antonie Rice, Brandon J. Turunen, Richard H. Himes, Dinah Dutta, Jacquelyn K. Huff, Apurba Datta, Anna Seelig, Kenneth L. Audus, Jared T. Spletstoser, Gunda I. Georg
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:495-498
A single-site modification of paclitaxel analogs at the C10 position on the baccatin III core that reduces interaction with P-glycoprotein in bovine brain microvessel endothelial cells is described. Modification and derivatization of the C10 position