Search Results - "SICILIANO, Salvatore J"

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and sar study of 4-pyrazolylpiperidine side chains by SHEN, Dong-Ming, MIN SHU, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, SCHLEIF, William A, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, LINEBERGER, Janet, MILLER, Michael D, EMINI, Emilio A, MILLS, Sander G, CHAPMAN, Kevin T, MALKOWITZ, Lorraine, SPRINGER, Martin S, GOULD, Sandra L, DEMARTINO, Julie A, SICILIANO, Salvatore J, KWEI, Gloria Y

“…Replacement of the flexible connecting chains between the piperidine moiety and an aromatic group in previous CCR5 antagonists with heterocycles, such as…”
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Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection by Veazey, Ronald S, Klasse, Per Johan, Ketas, Thomas J, Reeves, Jacqueline D, Piatak, Jr, Michael, Kunstman, Kevin, Kuhmann, Shawn E, Marx, Preston A, Lifson, Jeffrey D, Dufour, Jason, Mefford, Megan, Pandrea, Ivona, Wolinsky, Steven M, Doms, Robert W, DeMartino, Julie A, Siciliano, Salvatore J, Lyons, Kathy, Springer, Martin S, Moore, John P

“…Human immunodeficiency virus type 1 (HIV-1) fuses with cells after sequential interactions between its envelope glycoproteins, CD4 and a coreceptor, usually CC…”
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CCR5, CXCR4, and CD4 Are Clustered and Closely Apposed on Microvilli of Human Macrophages and T Cells by Singer, I I, Scott, S, Kawka, D W, Chin, J, Daugherty, B L, DeMartino, J A, DiSalvo, J, Gould, S L, Lineberger, J E, Malkowitz, L, Miller, M D, Mitnaul, L, Siciliano, S J, Staruch, M J, Williams, H R, Zweerink, H J, Springer, M S

“…Article Usage Stats Services JVI Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Binding and Functional Properties of Recombinant and Endogenous CXCR3 Chemokine Receptors by Weng, Y, Siciliano, S J, Waldburger, K E, Sirotina-Meisher, A, Staruch, M J, Daugherty, B L, Gould, S L, Springer, M S, DeMartino, J A

“…IP10 and MIG are two members of the CXC branch of the chemokine superfamily whose expression is dramatically up-regulated by interferon (IFN)-γ. The proteins…”
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Two-Site Binding of C5a by its Receptor: An Alternative Binding Paradigm for G Protein-Coupled Receptors by Siciliano, Salvatore J., Rollins, Thomas E., DeMartino, Julie, Konteatis, Zenon, Malkowitz, Lorraine, Van Riper, Gail, Bondy, Steven, Rosen, Hugh, Springer, Martin S.

“…The guanine nucleotide-binding protein-coupled receptor superfamily binds a vast array of biological messengers including lipids, odorants, catecholamines,…”
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Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 1: Discovery and initial structure-activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes by DORN, Conrad P, FINKE, Paul E, DEMARTINO, Julie A, SICILIANO, Salvatore J, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, LINEBERGER, Janet, MILLER, Michael, OATES, Bryan, SCHLEIF, William A, EMINI, Emilio A, BUDHU, Richard J, MILLS, Sander G, MACCOSS, Malcolm, MALKOWITZ, Lorraine, SPRINGER, Martin S, DAUGHERTY, Bruce L, GOULD, Sandra L

“…Screening of the Merck sample collection for compounds with CCR5 receptor binding afforded…”
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A Critical Site in the Core of the CCR5 Chemokine Receptor Required for Binding and Infectivity of Human Immunodeficiency Virus Type 1 by Siciliano, Salvatore J., Kuhmann, Shawn E., Weng, Youmin, Madani, Navid, Springer, Martin S., Lineberger, Janet E., Danzeisen, Renee, Miller, Michael D., Kavanaugh, Michael P., DeMartino, Julie A., Kabat, David

“…Like the CCR5 chemokine receptors of humans and rhesus macaques, the very homologous (∼98–99% identical) CCR5 of African green monkeys (AGMs) avidly binds…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains by Lynch, Christopher L., Willoughby, Christopher A., Hale, Jeffrey J., Holson, Edward J., Budhu, Richard J., Gentry, Amy L., Rosauer, Keith G., Caldwell, Charles G., Chen, Ping, Mills, Sander G., MacCoss, Malcolm, Berk, Scott, Chen, Liya, Chapman, Kevin T., Malkowitz, Lorraine, Springer, Martin S., Gould, Sandra L., DeMartino, Julie A., Siciliano, Salvatore J., Cascieri, Margaret A., Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A., Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio A.

“…The 4-(3-phenylprop-1-yl)piperidine moiety of the 1,3,4-trisubstituted pyrrolidine CCR5 antagonist 1 was modified with electron deficient aromatics as well as…”
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Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: Structure-activity relationships for substituted 2-aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes by FINKE, Paul E, MEURER, Laura C, SICILIANO, Salvatore J, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, LINEBERGER, Janet, MILLER, Michael, SCHLEIF, William A, OATES, Bryan, EMINI, Emilio A, MILLS, Sander G, MACCOSS, Malcolm, MALKOWITZ, Lorraine, SPRINGER, Martin S, DAUGHERTY, Bruce L, GOULD, Sandra L, DEMARTINO, Julie A

“…(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (3) has been…”
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Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds by SHEN, Dong-Ming, MIN SHU, GOULD, Sandra L, DEMARTINO, Julie A, SICILIANO, Salvatore J, LYONS, Kathy, PIVNICHNY, James V, KWEI, Gloria Y, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, SCHLEIF, William A, WILLOUGHBY, Christopher A, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, LINEBERGER, Janet, MILLER, Michael D, EMINI, Emilio A, SHAH, Shrenik, LYNCH, Christopher L, HALE, Jeffrey J, MILLS, Sander G, CHAPMAN, Kevin T, MALKOWITZ, Lorraine, SPRINGER, Martin S

“…Modifications of the alkyl acetic acid portion and the phenyl on pyrrolidine in our lead pyrazole compound 1 afforded the isopropyl compound 9. This compound…”
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Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment by MIN SHU, LOEBACH, Jennifer L, SICILIANO, Salvatore J, DI SALVO, Jerry, LYONS, Kathy, PIVNICHNY, James V, KWEI, Gloria Y, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, SCHLEIF, William A, DANZEISEN, Renee, PARKER, Kerry A, HAZUDA, Daria, KESSLER, Joseph, LINEBERGER, Janet, MILLER, Michael D, EMINI, Emilio A, MILLS, Sander G, CHAPMAN, Kevin T, SHEN, Dong-Ming, MALKOWITZ, Lorraine, SPRINGER, Martin S, GOULD, Sandra L, DEMARTINO, Julie A

“…Extensive SAR studies in our benzylpyrazole series of CCR5 antagonists have shown that both lipophilic and hydrophilic substituents on the phenyl of the benzyl…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: Synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV by LYNCH, Christopher L, HALE, Jeffrey J, DEMARTINO, Julie A, SICILIANO, Salvatore J, CASCIERI, Margaret A, CARELLA, Anthony, CARVER, Gwen, HOLMES, Karen, SCHLEIF, William A, DANZEISEN, Renee, HAZUDA, Daria, KESSLER, Joseph, BUDHU, Richard J, LINEBERGER, Janet, MILLER, Michael, EMINI, Emilio A, GENTRY, Amy L, MILLS, Sander G, CHAPMAN, Kevin T, MACCOSS, Malcolm, MALKOWITZ, Lorraine, SPRINGER, Martin S, GOULD, Sandra L

“…A series of alpha-(pyrrolidin-1-yl)acetic acids is presented as selective and potent antivirals against HIV. Several of the pyrrolidine zwitterions…”
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Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor by Shankaran, K., Donnelly, Karla L., Shah, Shrenik K., Guthikonda, Ravindra N., MacCoss, Malcolm, Mills, Sander G., Gould, Sandra L., Malkowitz, Lorraine, Siciliano, Salvatore J., Springer, Martin S., Carella, Anthony, Carver, Gwen, Hazuda, Daria, Holmes, Karen, Kessler, Joseph, Lineberger, Janet, Miller, Michael D., Emini, Emilio A., Schleif, William A.

“…A series of pyrrolidineacetic acid derivatives ( 1) was prepared and assayed for their CCR5 receptor affinity, anti-HIV-1 activity in a HeLa cell-based assay,…”
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1,3,4 trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains by Willoughby, Christopher A, Rosauer, Keith G, Hale, Jeffery J, Budhu, Richard J, Mills, Sander G, Chapman, Kevin T, MacCoss, Malcolm, Malkowitz, Lorraine, Springer, Martin S, Gould, Sandra L, DeMartino, Julie A, Siciliano, Salvatore J, Cascieri, Margaret A, Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A, Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio A

“…A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding…”
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CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines by Lynch, Christopher L, Gentry, Amy L, Hale, Jeffrey J, Mills, Sander G, MacCoss, Malcolm, Malkowitz, Lorraine, Springer, Martin S, Gould, Sandra L, DeMartino, Julie A, Siciliano, Salvatore J, Cascieri, Margaret A, Doss, George, Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A, Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio A

“…A series of CCR5 antagonists containing bicyclic isoxazolidines was generated through a nitrone mediated cycloaddition with olefins bearing the preferred…”
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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: Polar functionality and its effect on anti-HIV-1 activity by HALE, Jeffrey J, BUDHU, Richard J, HAZUDA, Daria, MILLER, Michael, KESSLER, Joseph, DANZEISEN, Renee, HOLMES, Karen, LINEBERGER, Janet, CARELLA, Anthony, CARVER, Gwen, EMINI, Emilio A, MILLS, Sander G, MACCOSS, Malcolm, GOULD, Sandra L, DEMARTINO, Julie A, SPRINGER, Martin S, SICILIANO, Salvatore J, MALKOWITZ, Lorraine, SCHLEIF, William A

“…Incorporation of acidic functional groups into a lead CCR5 antagonist identified from a targeted combinatorial library resulted in compounds with enhanced…”
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CCR5 Antagonists:  3-(Pyrrolidin-1-yl)propionic Acid Analogues with Potent Anti-HIV Activity by Lynch, Christopher L, Hale, Jeffrey J, Budhu, Richard J, Gentry, Amy L, Finke, Paul E, Caldwell, Charles G, Mills, Sander G, MacCoss, Malcolm, Shen, Dong-Ming, Chapman, Kevin T, Malkowitz, Lorraine, Springer, Martin S, Gould, Sandra L, DeMartino, Julie A, Siciliano, Salvatore J, Cascieri, Margaret A, Carella, Anthony, Carver, Gwen, Holmes, Karen, Schleif, William A, Danzeisen, Renee, Hazuda, Daria, Kessler, Joseph, Lineberger, Janet, Miller, Michael, Emini, Emilio

“…A novel approach to α,α-disubstituted-β-amino acids (β2,2-amino acids) was employed in the synthesis of a series of 3-(pyrrolidin-1-yl)propionic acids…”
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Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists by Shankaran, K., Donnelly, Karla L., Shah, Shrenik K., Caldwell, Charles G., Chen, Ping, Finke, Paul E., Oates, Bryan, MacCoss, Malcolm, Mills, Sander G., DeMartino, Julie A., Gould, Sandra L., Malkowitz, Lorraine, Siciliano, Salvatore J., Springer, Martin S., Kwei, Gloria, Carella, Anthony, Carver, Gwen, Danzeisen, Renee, Hazuda, Daria, Holmes, Karen, Kessler, Joseph, Lineberger, Janet, Miller, Michael D., Emini, Emilio A., Schleif, William A.

“…Ongoing efforts from these laboratories have resulted in the identification of 5-(piperidin-1-yl)-3-phenylpentylsulfones as a potent CCR5 antagonists. The…”
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Arginine 206 of the C5a Receptor Is Critical for Ligand Recognition and Receptor Activation by C-terminal Hexapeptide Analogs (∗) by DeMartino, Julie A., Konteatis, Zenon D., Siciliano, Salvatore J., Van Riper, Gail, Underwood, Dennis J., Fischer, Paul A., Springer, Martin S.

“…C5a is a 74-amino-acid glycoprotein whose receptor is a member of the rhodopsin superfamily. While antagonists have been generated to many of these receptors,…”
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Cloning, expression, and characterization of the human eosinophil eotaxin receptor by Daugherty, B L, Siciliano, S J, DeMartino, J A, Malkowitz, L, Sirotina, A, Springer, M S

“…Although there is a mounting body of evidence that eosinophils are recruited to sites of allergic inflammation by a number of beta-chemokines, particularly…”
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