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Search results for: David C. Chiara

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article

Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands

Pavel Y. Savechenkov, David C. Chiara, Rooma Desai, Alexander T. Stern, more

European Journal of Medicinal Chemistry > 2017 > 136 > C > 334-347

Neuroactive steroids are potent positive allosteric modulators of GABA_A receptors (GABA_AR), but the locations of their GABA_AR binding sites remain poorly defined. To discover these sites, we synthesized two photoreactive analogs of alphaxalone, an anesthetic neurosteroid targeting GABA_AR, 11β-(4-azido-2,3,5,6-tetrafluorobenzoyloxy)allopregnanolone, (F4N3Bzoxy-AP) and 11-aziallopregnanolone (11-AziAP)...

article

Interactions of a Photoreactive Steroid Anesthetic (F4N3-Alphaxalone) with Human α1β3γ2 GABA-A Receptors

David C. Chiara, Pavel Y. Savechenkov, Xiaojuan Zhou, Rooma Desai, more

Biophysical Journal > 2016 > 110 > 3 Supplement 1 > 455a

article

Anesthetics target interfacial transmembrane sites in nicotinic acetylcholine receptors

Stuart A. Forman, David C. Chiara, Keith W. Miller

Neuropharmacology > 2015 > 96 > Part B > 169-177

General anesthetics are a heterogeneous group of small amphiphilic ligands that interact weakly at multiple allosteric sites on many pentameric ligand gated ion channels (pLGICs), resulting in either inhibition, potentiation of channel activity, or both. Allosteric principles imply that modulator sites must change configuration and ligand affinity during receptor state transitions. Thus, general anesthetics...

article

Photoaffinity Labeling of Nicotinic Receptors: Diversity of Drug Binding Sites!

Ayman K Hamouda, Selwyn S Jayakar, David C Chiara, Jonathan B Cohen

Journal of Molecular Neuroscience > 2014 > 53 > 3 > 480-486

For almost 30 years, photoaffinity labeling and protein microsequencing techniques have been providing novel insights about the structure of nicotinic acetylcholine receptors (nAChR) and the diversity of nAChR drug binding sites. Photoaffinity labeling allows direct identification of amino acid residues contributing to a drug binding site without prior knowledge of the location of the binding site...

article

Photoaffinity Labeling the Propofol Binding Site in GLIC

David C. Chiara, Qiang Chen, Tommy Tillman, Jonathan F. Gill, more

Biophysical Journal > 2013 > 104 > 2 Supplement 1 > 636a

article

p -(4-Azipentyl)propofol: A Potent Photoreactive General Anesthetic Derivative of Propofol

Deirdre S. Stewart, Pavel Y. Savechenkov, Zuzana Dostalova, David C. Chiara, more

Journal of Medicinal Chemistry > 2011 > 54 > 23 > 8124 - 8135

article

Structural Differences in the Nicotinic Acetylcholine Receptor (NACHR) ion Channel Between Open and Desensitized States Revealed by Time-Resolved Photolabeling with [3H]Chlorpromazine (CPZ)

David C. Chiara, Innocent H. Yamodo, Keith W. Miller, Jonathan B. Cohen

Biophysical Journal > 2011 > 100 > 3 Supplement 1 > 275a

article

Identifying an Etomidate Binding Site in Heterologously Expressed Human Alpha1/Beta3 GABAA Receptors (GABAAR) Using Photoactive Etomidate Analogs

Selwyn S. Jayakar∗, Zuzana Dostalova, David C. Chiara, Xiaojuan Zhou, more

Biophysical Journal > 2011 > 100 > 3 Supplement 1 > 271a

article

Conformational Changes in the Nicotinic Acetylcholine Receptor during Gating and Desensitization

Innocent H. Yamodo, David C. Chiara, Jonathan B. Cohen, Keith W. Miller

Biochemistry > 2010 > 49 > 1 > 156 - 165

article

Characterization of the Etomidate Binding Site in Expressed α1β3 GABAAR by Photoaffinity Labeling

David C. Chiara, Zuzana Dostalova, Aiping Liu, Xiaojuan Zhou, more

Biophysical Journal > 2010 > 98 > 3 Supplement 1 > 704a

article

[ ³ H]Chlorpromazine Photolabeling of the Torpedo Nicotinic Acetylcholine Receptor Identifies Two State-Dependent Binding Sites in the Ion Channel

David C. Chiara, Ayman K. Hamouda, Michael R. Ziebell, Luis A. Mejia, more

Biochemistry > 2009 > 48 > 42 > 10066 - 10077

article

Photoaffinity Labeling the Agonist Binding Sites of nAChRs with [3H]Epibatidine

Shouryadeep Srivastava, Ayman K. Hamouda, Mitesh Sanghvi, Akash Pandhare, more

Biophysical Journal > 2009 > 96 > 3 Supplement 1 > 167a

article

Probing the Structure of the Affinity-Purified and Lipid-Reconstituted Torpedo Nicotinic Acetylcholine Receptor ^†

Ayman K. Hamouda, David C. Chiara, Michael P. Blanton, Jonathan B. Cohen

Biochemistry > 2008 > 47 > 48 > 12787 - 12794

article

Identifying the Lipid−Protein Interface of the α4β2 Neuronal Nicotinic Acetylcholine Receptor: Hydrophobic Photolabeling Studies with 3-(Trifluoromethyl)-3-( m -[ ¹²⁵ I]iodophenyl)diazirine ^†

Ayman K. Hamouda, Mitesh Sanghvi, David C. Chiara, Jonathan B. Cohen, more

Biochemistry > 2007 > 46 > 48 > 13837 - 13846

article

[ ³ H]Benzophenone Photolabeling Identifies State-Dependent Changes in Nicotinic Acetylcholine Receptor Structure ^†

Galo Garcia, David C. Chiara, Selvanayagam Nirthanan, Ayman K. Hamouda, more

Biochemistry > 2007 > 46 > 36 > 10296 - 10307

article

Mapping the Structural Requirements for Nicotinic Acetylcholine Receptor Activation by Using Tethered Alkyltrimethylammonium Agonists and Antagonists ^†

Deirdre S. Stewart, David C. Chiara, Jonathan B. Cohen

Biochemistry > 2006 > 45 > 35 > 10641 - 10653

article

Cholesterol Interacts with Transmembrane α-Helices M1, M3, and M4 of the Torpedo Nicotinic Acetylcholine Receptor: Photolabeling Studies Using [ ³ H]Azicholesterol ^†

Ayman K. Hamouda, David C. Chiara, Daniel Sauls, Jonathan B. Cohen, more

Biochemistry > 2006 > 45 > 3 > 976 - 986

article

Photolabeling the Torpedo Nicotinic Acetylcholine Receptor with 4-Azido-2,3,5,6-tetrafluorobenzoylcholine, a Partial Agonist ^†

Selvanayagam Nirthanan, Michael R. Ziebell, David C. Chiara, Filbert Hong, more

Biochemistry > 2005 > 44 > 41 > 13447 - 13456

article

Identification of Nicotinic Acetylcholine Receptor Amino Acids Photolabeled by the Volatile Anesthetic Halothane ^†

David C. Chiara, Lawrence J. Dangott, Roderic G. Eckenhoff, Jonathan B. Cohen

Biochemistry > 2003 > 42 > 46 > 13457 - 13467

article

Identification of Amino Acids in the Nicotinic Acetylcholine Receptor Agonist Binding Site and Ion Channel Photolabeled by 4-[(3-Trifluoromethyl)-3 H -Diazirin-3-yl]Benzoylcholine, a Novel Photoaffinity Antagonist ^†

David C. Chiara, Jonathan C. Trinidad, Dong Wang, Michael R. Ziebell, more

Biochemistry > 2003 > 42 > 2 > 271 - 283

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