Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Sergiy Levin"'
Publikováno v:
Bio-Protocol, Vol 10, Iss 24 (2020)
G-protein coupled receptors (GPCRs) remain at the forefront of drug discovery efforts. Detailed assessment of features contributing to GPCR ligand engagement in a physiologically relevant environment is imperative to the development of new therapeuti
Externí odkaz:
https://doaj.org/article/30c0400fe0cb45b6ab6b4948fd1821d6
Autor:
Michael P. Killoran, Sergiy Levin, Michelle E. Boursier, Kristopher Zimmerman, Robin Hurst, Mary P. Hall, Thomas Machleidt, Thomas A. Kirkland, Rachel Friedman Ohana
Publikováno v:
Molecules, Vol 26, Iss 10, p 2857 (2021)
Gaining insight into the pharmacology of ligand engagement with G-protein coupled receptors (GPCRs) under biologically relevant conditions is vital to both drug discovery and basic research. NanoLuc-based bioluminescence resonance energy transfer (Na
Externí odkaz:
https://doaj.org/article/6603ab2a2c3e4fc183fbdeba047372cc
Autor:
Florence Gbahou, Sergiy Levin, Irina G. Tikhonova, Gloria Somalo Barranco, Charlotte Izabelle, Rachel Friedman Ohana, Ralf Jockers
Publikováno v:
ACS Pharmacology & Translational Science. 5:668-678
The two human melatonin receptors MT
Autor:
Rachel Friedman Ohana, Keith V. Wood, Robin Hurst, Kristopher Zimmerman, Michael M. Rosenblatt, Sergiy Levin, Thomas Machleidt, Thomas A. Kirkland
Publikováno v:
ACS Chemical Biology. 16:404-413
Identification of physiologically relevant targets for lead compounds emerging from drug discovery screens is often the rate-limiting step toward understanding their mechanism of action and potential for undesired off-target effects. To this end, we
Autor:
Michelle E. Boursier, Thomas Machleidt, Christopher T. Eggers, Keith V. Wood, Robin Hurst, Kris Zimmerman, Thomas A. Kirkland, Braeden L. Butler, Rachel Friedman Ohana, Sergiy Levin
Publikováno v:
J Biol Chem
G protein-coupled receptors (GPCRs) are prominent targets to new therapeutics for a range of diseases. Comprehensive assessments of their cellular interactions with bioactive compounds, particularly in a kinetic format, are imperative to the developm
Autor:
Sergiy Levin, Keith V. Wood, Rachel Friedman Ohana, Robin Hurst, Matthew B. Robers, Thomas A. Kirkland, Thomas Machleidt, Mike Rosenblatt, Lance P. Encell
Publikováno v:
Scientific Reports
Scientific Reports, Vol 9, Iss 1, Pp 1-12 (2019)
Scientific Reports, Vol 9, Iss 1, Pp 1-12 (2019)
Ligand binding assays routinely employ fluorescently-labeled protein ligands to quantify the extent of binding. These ligands are commonly generated through chemical modification of accessible lysine residues, which often results in heterogeneous pop
Autor:
Keith V. Wood, Robin Hurst, H. Tetsuo Uyeda, Matthew B. Robers, Paul Otto, Rachel Friedman Ohana, Thomas A. Kirkland, Sergiy Levin, Lance P. Encell, Kris Zimmerman, Carolyn C. Woodroofe
Publikováno v:
ACS Chemical Biology. 10:2316-2324
Phenotypic screening of compound libraries is a significant trend in drug discovery, yet success can be hindered by difficulties in identifying the underlying cellular targets. Current approaches rely on tethering bioactive compounds to a capture tag
Autor:
Sergiy Levin, Stephen J. Dwight
Publikováno v:
Organic letters. 18(20)
A one-step, operationally simple protocol for the synthesis of isomerically pure rhodamine dyes from phthalaldehydic acids is reported. Using a mixture of 2,2,2-trifluoroethanol and water as reaction media allows for clean and efficient formation of
Autor:
Kris Zimmerman, Melanie Dart, Sergiy Levin, Rachel Friedman Ohana, Lance P. Encell, Thomas A. Kirkland, H. Tetsuo Uyeda, Keith V. Wood, Robin Hurst, Monika G. Wood, Marie K. Schwinn
Publikováno v:
ACS chemical biology. 11(9)
The benefits provided by phenotypic screening of compound libraries are often countered by difficulties in identifying the underlying cellular targets. We recently described a new approach utilizing a chloroalkane capture tag, which can be chemically
Autor:
Mei Cong, Matthew B. Robers, Monika G. Wood, Kevin Kupcho, Keith V. Wood, James Robert Hartnett, Sergiy Levin, Thomas A. Kirkland, Danette L. Daniels, Carolyn C. Woodroofe, Andrew L. Niles, Melanie Dart, Kristopher Zimmerman, Thomas Machleidt, Chad Zimprich, Rachel Friedman Ohana, Yi-Qiang Cheng, Michael R. Slater
Publikováno v:
Nature Communications
The therapeutic action of drugs is predicated on their physical engagement with cellular targets. Here we describe a broadly applicable method using bioluminescence resonance energy transfer (BRET) to reveal the binding characteristics of a drug with