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Items: 46


Identifying Drugs that Bind Selectively to Intersubunit General Anesthetic Sites in the α1β3γ2 GABAAR Transmembrane Domain.

Jayakar SS, Zhou X, Chiara DC, Jarava-Barrera C, Savechenkov PY, Bruzik KS, Tortosa M, Miller KW, Cohen JB.

Mol Pharmacol. 2019 Jun;95(6):615-628. doi: 10.1124/mol.118.114975. Epub 2019 Apr 5.


A photoreactive analog of allopregnanolone enables identification of steroid-binding sites in a nicotinic acetylcholine receptor.

Yu Z, Chiara DC, Savechenkov PY, Bruzik KS, Cohen JB.

J Biol Chem. 2019 May 10;294(19):7892-7903. doi: 10.1074/jbc.RA118.007172. Epub 2019 Mar 28.


Inhibitable photolabeling by neurosteroid diazirine analog in the β3-Subunit of human hetereopentameric type A GABA receptors.

Wu B, Jayakar SS, Zhou X, Titterton K, Chiara DC, Szabo AL, Savechenkov PY, Kent DE, Cohen JB, Forman SA, Miller KW, Bruzik KS.

Eur J Med Chem. 2019 Jan 15;162:810-824. doi: 10.1016/j.ejmech.2018.11.019. Epub 2018 Nov 19.


Photoaffinity Labeling of Pentameric Ligand-Gated Ion Channels: A Proteomic Approach to Identify Allosteric Modulator Binding Sites.

Jayakar SS, Ang G, Chiara DC, Hamouda AK.

Methods Mol Biol. 2017;1598:157-197. doi: 10.1007/978-1-4939-6952-4_7.


Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.

Savechenkov PY, Chiara DC, Desai R, Stern AT, Zhou X, Ziemba AM, Szabo AL, Zhang Y, Cohen JB, Forman SA, Miller KW, Bruzik KS.

Eur J Med Chem. 2017 Aug 18;136:334-347. doi: 10.1016/j.ejmech.2017.04.043. Epub 2017 Apr 21.


Unraveling amino acid residues critical for allosteric potentiation of (α4)3(β2)2-type nicotinic acetylcholine receptor responses.

Wang ZJ, Deba F, Mohamed TS, Chiara DC, Ramos K, Hamouda AK.

J Biol Chem. 2017 Jun 16;292(24):9988-10001. doi: 10.1074/jbc.M116.771246. Epub 2017 Apr 26.


General Anesthetic Binding Sites in Human α4β3δ γ-Aminobutyric Acid Type A Receptors (GABAARs).

Chiara DC, Jounaidi Y, Zhou X, Savechenkov PY, Bruzik KS, Miller KW, Cohen JB.

J Biol Chem. 2016 Dec 16;291(51):26529-26539. Epub 2016 Nov 7.


Multiple Non-Equivalent Interfaces Mediate Direct Activation of GABAA Receptors by Propofol.

Eaton MM, Germann AL, Arora R, Cao LQ, Gao X, Shin DJ, Wu A, Chiara DC, Cohen JB, Steinbach JH, Evers AS, Akk G.

Curr Neuropharmacol. 2016;14(7):772-80. Review.


Positive and Negative Allosteric Modulation of an α1β3γ2 γ-Aminobutyric Acid Type A (GABAA) Receptor by Binding to a Site in the Transmembrane Domain at the γ+-β- Interface.

Jayakar SS, Zhou X, Savechenkov PY, Chiara DC, Desai R, Bruzik KS, Miller KW, Cohen JB.

J Biol Chem. 2015 Sep 18;290(38):23432-46. doi: 10.1074/jbc.M115.672006. Epub 2015 Jul 30.


Anesthetics target interfacial transmembrane sites in nicotinic acetylcholine receptors.

Forman SA, Chiara DC, Miller KW.

Neuropharmacology. 2015 Sep;96(Pt B):169-77. doi: 10.1016/j.neuropharm.2014.10.002. Epub 2014 Oct 12. Review.


Multiple propofol-binding sites in a γ-aminobutyric acid type A receptor (GABAAR) identified using a photoreactive propofol analog.

Jayakar SS, Zhou X, Chiara DC, Dostalova Z, Savechenkov PY, Bruzik KS, Dailey WP, Miller KW, Eckenhoff RG, Cohen JB.

J Biol Chem. 2014 Oct 3;289(40):27456-68. doi: 10.1074/jbc.M114.581728. Epub 2014 Aug 1.


Identifying barbiturate binding sites in a nicotinic acetylcholine receptor with [3H]allyl m-trifluoromethyldiazirine mephobarbital, a photoreactive barbiturate.

Hamouda AK, Stewart DS, Chiara DC, Savechenkov PY, Bruzik KS, Cohen JB.

Mol Pharmacol. 2014 May;85(5):735-46. doi: 10.1124/mol.113.090985. Epub 2014 Feb 21.


Photoaffinity labeling the propofol binding site in GLIC.

Chiara DC, Gill JF, Chen Q, Tillman T, Dailey WP, Eckenhoff RG, Xu Y, Tang P, Cohen JB.

Biochemistry. 2014 Jan 14;53(1):135-42. doi: 10.1021/bi401492k. Epub 2013 Dec 30.


Photoaffinity labeling of nicotinic receptors: diversity of drug binding sites!

Hamouda AK, Jayakar SS, Chiara DC, Cohen JB.

J Mol Neurosci. 2014 Jul;53(3):480-6. doi: 10.1007/s12031-013-0150-1. Epub 2013 Oct 26. Review.


Cysteine substitutions define etomidate binding and gating linkages in the α-M1 domain of γ-aminobutyric acid type A (GABAA) receptors.

Stewart DS, Hotta M, Li GD, Desai R, Chiara DC, Olsen RW, Forman SA.

J Biol Chem. 2013 Oct 18;288(42):30373-86. doi: 10.1074/jbc.M113.494583. Epub 2013 Sep 5.


Specificity of intersubunit general anesthetic-binding sites in the transmembrane domain of the human α1β3γ2 γ-aminobutyric acid type A (GABAA) receptor.

Chiara DC, Jayakar SS, Zhou X, Zhang X, Savechenkov PY, Bruzik KS, Miller KW, Cohen JB.

J Biol Chem. 2013 Jul 5;288(27):19343-57. doi: 10.1074/jbc.M113.479725. Epub 2013 May 15.


Allyl m-trifluoromethyldiazirine mephobarbital: an unusually potent enantioselective and photoreactive barbiturate general anesthetic.

Savechenkov PY, Zhang X, Chiara DC, Stewart DS, Ge R, Zhou X, Raines DE, Cohen JB, Forman SA, Miller KW, Bruzik KS.

J Med Chem. 2012 Jul 26;55(14):6554-65. doi: 10.1021/jm300631e. Epub 2012 Jul 17.


Mapping general anesthetic binding site(s) in human α1β3 γ-aminobutyric acid type A receptors with [³H]TDBzl-etomidate, a photoreactive etomidate analogue.

Chiara DC, Dostalova Z, Jayakar SS, Zhou X, Miller KW, Cohen JB.

Biochemistry. 2012 Jan 31;51(4):836-47. doi: 10.1021/bi201772m. Epub 2012 Jan 23.


p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol.

Stewart DS, Savechenkov PY, Dostalova Z, Chiara DC, Ge R, Raines DE, Cohen JB, Forman SA, Bruzik KS, Miller KW.

J Med Chem. 2011 Dec 8;54(23):8124-35. doi: 10.1021/jm200943f. Epub 2011 Nov 10.


Numerous classes of general anesthetics inhibit etomidate binding to gamma-aminobutyric acid type A (GABAA) receptors.

Li GD, Chiara DC, Cohen JB, Olsen RW.

J Biol Chem. 2010 Mar 19;285(12):8615-20. doi: 10.1074/jbc.M109.074708. Epub 2010 Jan 18.


Conformational changes in the nicotinic acetylcholine receptor during gating and desensitization.

Yamodo IH, Chiara DC, Cohen JB, Miller KW.

Biochemistry. 2010 Jan 12;49(1):156-65. doi: 10.1021/bi901550p.


[(3)H]chlorpromazine photolabeling of the torpedo nicotinic acetylcholine receptor identifies two state-dependent binding sites in the ion channel.

Chiara DC, Hamouda AK, Ziebell MR, Mejia LA, Garcia G 3rd, Cohen JB.

Biochemistry. 2009 Oct 27;48(42):10066-77. doi: 10.1021/bi901271w.


Neurosteroids allosterically modulate binding of the anesthetic etomidate to gamma-aminobutyric acid type A receptors.

Li GD, Chiara DC, Cohen JB, Olsen RW.

J Biol Chem. 2009 May 1;284(18):11771-5. doi: 10.1074/jbc.C900016200. Epub 2009 Mar 12.


Time-resolved photolabeling of the nicotinic acetylcholine receptor by [3H]azietomidate, an open-state inhibitor.

Chiara DC, Hong FH, Arevalo E, Husain SS, Miller KW, Forman SA, Cohen JB.

Mol Pharmacol. 2009 May;75(5):1084-95. doi: 10.1124/mol.108.054353. Epub 2009 Feb 13.


Probing the structure of the affinity-purified and lipid-reconstituted torpedo nicotinic acetylcholine receptor.

Hamouda AK, Chiara DC, Blanton MP, Cohen JB.

Biochemistry. 2008 Dec 2;47(48):12787-94. doi: 10.1021/bi801476j.


Identification of binding sites in the nicotinic acetylcholine receptor for TDBzl-etomidate, a photoreactive positive allosteric effector.

Nirthanan S, Garcia G 3rd, Chiara DC, Husain SS, Cohen JB.

J Biol Chem. 2008 Aug 8;283(32):22051-62. doi: 10.1074/jbc.M801332200. Epub 2008 Jun 4.


[3H]Benzophenone photolabeling identifies state-dependent changes in nicotinic acetylcholine receptor structure.

Garcia G 3rd, Chiara DC, Nirthanan S, Hamouda AK, Stewart DS, Cohen JB.

Biochemistry. 2007 Sep 11;46(36):10296-307. Epub 2007 Aug 9.


Identification of a GABAA receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog.

Li GD, Chiara DC, Sawyer GW, Husain SS, Olsen RW, Cohen JB.

J Neurosci. 2006 Nov 8;26(45):11599-605.


alpha-Conotoxin GI benzoylphenylalanine derivatives. (1)H-NMR structures and photoaffinity labeling of the Torpedo californica nicotinic acetylcholine receptor.

Kasheverov IE, Chiara DC, Zhmak MN, Maslennikov IV, Pashkov VS, Arseniev AS, Utkin YN, Cohen JB, Tsetlin VI.

FEBS J. 2006 Apr;273(7):1373-88.


Photolabeling the Torpedo nicotinic acetylcholine receptor with 4-azido-2,3,5,6-tetrafluorobenzoylcholine, a partial agonist.

Nirthanan S, Ziebell MR, Chiara DC, Hong F, Cohen JB.

Biochemistry. 2005 Oct 18;44(41):13447-56.


Gating-enhanced accessibility of hydrophobic sites within the transmembrane region of the nicotinic acetylcholine receptor's {delta}-subunit. A time-resolved photolabeling study.

Arevalo E, Chiara DC, Forman SA, Cohen JB, Miller KW.

J Biol Chem. 2005 Apr 8;280(14):13631-40. Epub 2005 Jan 21. Erratum in: J Biol Chem. 2005 Jun 10;280(23):22556.


Identification of nicotinic acetylcholine receptor amino acids photolabeled by the volatile anesthetic halothane.

Chiara DC, Dangott LJ, Eckenhoff RG, Cohen JB.

Biochemistry. 2003 Nov 25;42(46):13457-67.


Site of resting state inhibition of the nicotinic acetylcholine receptor by a hydrophobic inhibitor.

Chiara DC, Kloczewiak MA, Addona GH, Yu JA, Cohen JB, Miller KW.

Biochemistry. 2001 Jan 9;40(1):296-304.


Active-site peptides of acetylcholinesterase of Electrophorus electricus: labelling of His-440 by 1-bromo-[2-14C]pinacolone and Ser-200 by tritiated diisopropyl fluorophosphate.

Salih E, Chishti SB, Vicedomine P, Cohen SG, Chiara DC, Cohen JB.

Biochim Biophys Acta. 1994 Oct 19;1208(2):324-31. Erratum in: Biochim Biophys Acta 1995 Jan 5;1246(1):107.


Amino acid sequence of porcine heart fumarase.

Sacchettini JC, Frazier MW, Chiara DC, Banaszak LJ, Grant GA.

Biochem Biophys Res Commun. 1988 May 31;153(1):435-40.


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