Search Results - "Mirzadegan, T."

Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle by Mirzadegan, T, Diehl, F, Ebi, B, Bhakta, S, Polsky, I, McCarley, D, Mulkins, M, Weatherhead, G S, Lapierre, J M, Dankwardt, J, Morgans, Jr, D, Wilhelm, R, Jarnagin, K

“…Monocyte chemoattracant-1 (MCP-1) stimulates leukocyte chemotaxis to inflammatory sites, such as rheumatoid arthritis, atherosclerosis, and asthma, by use of…”
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D3R Grand Challenge 3: blind prediction of protein–ligand poses and affinity rankings by Gaieb, Zied, Parks, Conor D., Chiu, Michael, Yang, Huanwang, Shao, Chenghua, Walters, W. Patrick, Lambert, Millard H., Nevins, Neysa, Bembenek, Scott D., Ameriks, Michael K., Mirzadegan, Tara, Burley, Stephen K., Amaro, Rommie E., Gilson, Michael K.

“…The Drug Design Data Resource aims to test and advance the state of the art in protein–ligand modeling by holding community-wide blinded, prediction…”
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Sequence Analyses of G-Protein-Coupled Receptors:  Similarities to Rhodopsin by Mirzadegan, Tara, Benkö, Gil, Filipek, Sławomir, Palczewski, Krzysztof

“…G-protein-coupled receptors (GPCRs) 1 constitute a large superfamily of receptor proteins responsible for signal transduction (see http://www.gpcr.org/7tm )…”
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Synthesis and SAR of bulky 1-azabicyclo[2.2.1]-3-one oximes as muscarinic receptor subtype selective agonists by Tecle, H, Lauffer, D J, Mirzadegan, T, Moos, W H, Moreland, D W, Pavia, M R, Schwarz, R D, Davis, R E

“…The synthesis of a series of potent and efficacious 1-azabicyclo[2.2.1]heptan-3-one oxime muscarinic agonists is described. The oximes have extended appendages…”
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CI-1017, a functionally M1-selective muscarinic agonist: design, synthesis, and preclinical pharmacology by Tecle, H, Schwarz, R.D, Barrett, S.D, Callahan, M.J, Caprathe, B.W, Davis, R.E, Doyle, P, Emmerling, M, Lauffer, D.J, Mirzadegan, T, Moreland, D.W, Lipiniski, W, Nelson, C, Raby, C, Spencer, C, Spiegel, K, Thomas, A.J, Jaen, J.C

“…The five muscarinic receptor subtypes (M1–M5) are characterized by seven helices that define a transmembrane cavity which serves as the binding pocket for…”
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Substrate-dependent inhibition or stimulation of HIV RNase H activity by non-nucleoside reverse transcriptase inhibitors (NNRTIs) by Hang, Julie Q., Li, Yu, Yang, Yanli, Cammack, Nick, Mirzadegan, Tara, Klumpp, Klaus

“…HIV reverse transcriptase (HIV-RT) contains two distinct protein domains catalyzing DNA polymerase and RNase H activities. Non-nucleoside reverse transcriptase…”
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(±)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oximes: Potent muscarinic agonists by Tecle, H., Lauffer, D.J., Davis, R.E., Mirzadegan, T., Moreland, D.W., Schwan, R.D., Thomas, A.J., Raby, C., Eubanks, D., Brann, M.R., Jaen, J.C.

“…Synthesis and SAR of a new class of 1-azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oxime muscarinic agonists are described. Depending on…”
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Z-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl) oximes as potential m1-subtype selective muscarinic agonists by Tecle, H., Jaen, J.C., Augelli-Szafran, C., Barrett, S.D., Caprathe, B.W., Lauffer, D.J., Mirzadegan, T., Moos, W.H., Moreland, D.W., Pavia, M.R., Schwarz, R.D., Thomas, A.J., Davis, R.E.

“…The synthesis and SAR of a series of Z-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl) oximes are described. The biochemistry and pharmacology of PD…”
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Identification of Residues in the Monocyte Chemotactic Protein-1 That Contact the MCP-1 Receptor, CCR2 by Hemmerich, Stefan, Paavola, Chad, Bloom, Adam, Bhakta, Sunil, Freedman, Richard, Grunberger, Dorit, Krstenansky, John, Lee, Simon, McCarley, Debbie, Mulkins, Mary, Wong, Belinda, Pease, Joe, Mizoue, Laura, Mirzadegan, Tara, Polsky, Irene, Thompson, Kelly, Handel, Tracy M, Jarnagin, Kurt

“…The CC chemokine, MCP-1, has been identified as a major chemoattractant for T cells and monocytes, and plays a significant role in the pathology of…”
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Substitution of lysine-181 to aspartic acid in the third transmembrane region of the endothelin (ET) type B receptor selectively reduces its high-affinity binding with ET-3 peptide by Mauzy, C, Wu, L H, Egloff, A M, Mirzadegan, T, Chung, F Z

“…In the G protein-coupled receptor family, a highly conserved aspartic acid located within the third transmembrane domain has been shown to be involved in…”
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Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors by Campbell, Jeffrey A., Bordunov, Viola, Broka, Chris A., Browner, Michelle F., Kress, James M., Mirzadegan, Tara, Ramesha, Chakk, Sanpablo, Bong F., Stabler, Russell, Takahara, Patricia, Villasenor, Armando, Walker, Keith A.M., Wang, Jin-Hai, Welch, Mary, Weller, Paul

“…The introduction of 3-arylmethyl, 3-aryloxy and 3-arylthio moieties into a 6-methylsulfonylindole framework using rational drug design led to potent, selective…”
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Design of Annulated Pyrazoles As Inhibitors of HIV-1 Reverse Transcriptase by Sweeney, Z.K., Harris, S.F., Arora, N., Javanbakht, H., Li, Y., Fretland, J., Davidson, J.P., Billedeau, J.R., Gleason, S., Hirschfeld, D., Kennedy-Smith, J.J., Mirzadegan, T., Roetz, R., Smith, M., Sperry, S., Suh, J.M., Wu, J., Tsing, S., Villasenor, A.G., Paul, A., Su, G.

“…Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are recommended components of preferred combination antiretroviral therapies used for the treatment of…”
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Lactams as EP4 Prostanoid Receptor Agonists. 3. Discovery of N-Ethylbenzoic Acid 2-Pyrrolidinones as Subtype Selective Agents by Elworthy, Todd R, Brill, Emma R, Chiou, San-San, Chu, Frances, Harris, Jason R, Hendricks, R. Than, Huang, Jane, Kim, Woongki, Lach, Leang K, Mirzadegan, Tara, Yee, Calvin, Walker, Keith A. M

“…Two distinct synthetic schemes were applied to access heteroatom-containing α-chain lactams or lactams terminated as aryl acids. The latter lactams were…”
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Sequence Analyses of G-Protein-Coupled Receptors:  Similarities to Rhodopsin by Mirzadegan, Tara, Benkö, Gil, Filipek, Sałomir, Palczewski, Krzysztof

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Possible Role of the 11-cis-Retinyl Conformation in Controlling the Dual Decay Processes of Excited Rhodopsin by Robert S. H. Liu, Hammond, George S., Mirzadegan, Taraneh, Turro, Nicholas J.

“…In this work, we examine how the reported dual decay processes of rhodopsin and binding site stereospecificity can be accounted for by the recently available…”
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Crystal Structure of Phenylmethanesulfonyl Fluoride-Treated Human Chymase at 1.9 Å by McGrath, Mary E, Mirzadegan, Tara, Schmidt, Brian F

“…The X-ray crystal structure of human chymase has been determined to 1.9 Å resolution using molecular replacement methods. This first structure of human chymase…”
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Design and Synthesis of m1-Selective Muscarinic Agonists:  (R)-(−)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3‘-Methoxyphenyl)-2-propynyl)- oxime Maleate (CI-1017), a Functionally m1-Selective Muscarinic Agonist by Tecle, Haile, Barrett, Stephen D, Lauffer, David J, Augelli-Szafran, Corinne, Brann, Mark R, Callahan, Michael J, Caprathe, Bradley. W, Davis, Robert E, Doyle, Patricia D, Eubanks, David, Lipiniski, William, Mirzadegan, Tara, Moos, Walter H, Moreland, D. W, Nelson, Carrie B, Pavia, Michael R, Raby, Charlotte, Schwarz, Roy D, Spencer, Carolyn J, Thomas, Anthony J, Jaen, Juan C

“…The synthesis and SAR of a series of (Z)-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl)oximes are described. The biochemistry and pharmacology of…”
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Azulenic retinoids: novel nonbenzenoid aromatic retinoids with anticancer activity by Asato, Alfred E, Peng, Ao, Hossain, Mohammad Z, Mirzadegan, Taraneh, Bertram, John S

“…Several novel azulene-containing retinoids were prepared and evaluated for their ability to suppress carcinogen-induced neoplastic transformation and to…”
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Replacement of lysine-181 by aspartic acid in the third transmembrane region of endothelin type B receptor reduces its affinity to endothelin peptides and sarafotoxin 6c without affecting G protein coupling by Zhu, G, Wu, L H, Mauzy, C, Egloff, A M, Mirzadegan, T, Chung, F Z

“…A conserved aspartic acid residue in the third transmembrane region of many of the G protein-coupled receptors has been shown to play a role in ligand binding…”
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The shape of a three-dimensional binding site of rhodopsin based on molecular modeling analyses of isomeric and other visual pigment analogues: bioorganic studies of visual pigments. XI by LIU, R. S. H, MIRZADEGAN, T

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