Research ArticleArticle
VU6036720: The First Potent and Selective In Vitro Inhibitor of Heteromeric Kir4.1/5.1 Inward Rectifier Potassium Channels
Samantha J. McClenahan, Caitlin N. Kent, Sujay V. Kharade, Elena Isaeva, Jade C. Williams, Changho Han, Andrew Terker, Robert Gresham III, Roman M. Lazarenko, Emily L. Days, Ian M. Romaine, Joshua A. Bauer, Olivier Boutaud, Gary A. Sulikowski, Raymond Harris, C. David Weaver, Alexander Staruschenko, Craig W. Lindsley and Jerod S. Denton
Molecular Pharmacology May 2022, 101 (5) 357-370; DOI: https://doi.org/10.1124/molpharm.121.000464
Samantha J. McClenahan
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Caitlin N. Kent
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Sujay V. Kharade
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Elena Isaeva
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Jade C. Williams
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Changho Han
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Andrew Terker
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Robert Gresham III
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Roman M. Lazarenko
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Emily L. Days
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Ian M. Romaine
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Joshua A. Bauer
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Olivier Boutaud
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Gary A. Sulikowski
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Raymond Harris
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
C. David Weaver
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Alexander Staruschenko
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Craig W. Lindsley
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Jerod S. Denton
Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
Article Information
vol. 101 no. 5 357-370
PubMed
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Online ISSN
History
- Received November 18, 2021
- Accepted February 14, 2022
- Published online April 7, 2022.
Article Versions
- Earlier version (March 3, 2022 - 23:51).
- You are viewing the most recent version of this article.
Copyright & Usage
Copyright © 2022 by The American Society for Pharmacology and Experimental Therapeutics
Author Information
- Samantha J. McClenahan1,
- Caitlin N. Kent1,
- Sujay V. Kharade,
- Elena Isaeva,
- Jade C. Williams,
- Changho Han,
- Andrew Terker,
- Robert Gresham III,
- Roman M. Lazarenko,
- Emily L. Days,
- Ian M. Romaine,
- Joshua A. Bauer,
- Olivier Boutaud,
- Gary A. Sulikowski,
- Raymond Harris,
- C. David Weaver,
- Alexander Staruschenko,
- Craig W. Lindsley, and
- Jerod S. Denton
- Departments of Anesthesiology (S.J.M., S.V.K., R.G., R.M.L., J.S.D.), Biochemistry (J.A.B.), Chemistry (C.N.K., J.C.W., I.M.R., C.D.W., G.A.S., C.W.L.), Pharmacology (E.L.D., C.D.W., C.W.L., C.H., O.B., J.S.D.), and Nephrology (A.T., R.H.), and Vanderbilt Institute of Chemical Biology (J.A.B., G.S., C.D.W., C.W.L., J.S.D.), Vanderbilt University, Nashville, Tennessee; Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin (E.I.); and Department of Molecular Pharmacology and Physiology, University of South Florida, Tampa, Florida (A.S.)
- Address correspondence to:
Dr. Jerod S. Denton, 1161 21st Avenue South, T4208 Medical Center North, Nashville, TN 37232. E-mail: jerod.s.denton{at}vumc.org
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Research ArticleArticle
Kir4.1/5.1 Inhibitor VU6036720
Samantha J. McClenahan, Caitlin N. Kent, Sujay V. Kharade, Elena Isaeva, Jade C. Williams, Changho Han, Andrew Terker, Robert Gresham, Roman M. Lazarenko, Emily L. Days, Ian M. Romaine, Joshua A. Bauer, Olivier Boutaud, Gary A. Sulikowski, Raymond Harris, C. David Weaver, Alexander Staruschenko, Craig W. Lindsley and Jerod S. Denton
Molecular Pharmacology May 1, 2022, 101 (5) 357-370; DOI: https://doi.org/10.1124/molpharm.121.000464
Research ArticleArticle
Kir4.1/5.1 Inhibitor VU6036720
Samantha J. McClenahan, Caitlin N. Kent, Sujay V. Kharade, Elena Isaeva, Jade C. Williams, Changho Han, Andrew Terker, Robert Gresham, Roman M. Lazarenko, Emily L. Days, Ian M. Romaine, Joshua A. Bauer, Olivier Boutaud, Gary A. Sulikowski, Raymond Harris, C. David Weaver, Alexander Staruschenko, Craig W. Lindsley and Jerod S. Denton
Molecular Pharmacology May 1, 2022, 101 (5) 357-370; DOI: https://doi.org/10.1124/molpharm.121.000464
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