Search Results - "Salituro, Gino M"

Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder by Edmondson, Scott D, Zhu, Cheng, Kar, Nam Fung, Di Salvo, Jerry, Nagabukuro, Hiroshi, Sacre-Salem, Beatrice, Dingley, Karen, Berger, Richard, Goble, Stephen D, Morriello, Gregori, Harper, Bart, Moyes, Christopher R, Shen, Dong-Ming, Wang, Liping, Ball, Richard, Fitzmaurice, Aileen, Frenkl, Tara, Gichuru, Loise N, Ha, Sookhee, Hurley, Amanda L, Jochnowitz, Nina, Levorse, Dorothy, Mistry, Shruty, Miller, Randy R, Ormes, James, Salituro, Gino M, Sanfiz, Anthony, Stevenson, Andra S, Villa, Katherine, Zamlynny, Beata, Green, Stuart, Struthers, Mary, Weber, Ann E

“…The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described. An early-generation clinical…”
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Evaluation of CETP activity in vivo under non-steady-state conditions: influence of anacetrapib on HDL-TG flux[S] by McLaren, David G., Previs, Stephen F., Phair, Robert D., Stout, Steven J., Xie, Dan, Chen, Ying, Salituro, Gino M., Xu, Suoyu S., Castro-Perez, Jose M., Opiteck, Gregory J., Akinsanya, Karen O., Cleary, Michele A., Dansky, Hayes M., Johns, Douglas G., Roddy, Thomas P.

“…Studies in lipoprotein kinetics almost exclusively rely on steady-state approaches to modeling. Herein, we have used a non-steady-state experimental design to…”
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Design, Synthesis, and Evaluation of Conformationally Restricted Acetanilides as Potent and Selective β3 Adrenergic Receptor Agonists for the Treatment of Overactive Bladder by Moyes, Christopher R, Berger, Richard, Goble, Stephen D, Harper, Bart, Shen, Dong-Ming, Wang, Liping, Bansal, Alka, Brown, Patricia N, Chen, Airu S, Dingley, Karen H, Di Salvo, Jerry, Fitzmaurice, Aileen, Gichuru, Loise N, Hurley, Amanda L, Jochnowitz, Nina, Miller, Randall R, Mistry, Shruty, Nagabukuro, Hiroshi, Salituro, Gino M, Sanfiz, Anthony, Stevenson, Andra S, Villa, Katherine, Zamlynny, Beata, Struthers, Mary, Weber, Ann E, Edmondson, Scott D

“…A series of conformationally restricted acetanilides were synthesized and evaluated as β3-adrenergic receptor agonists (β3-AR) for the treatment of overactive…”
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Small molecule insulin mimetics reduce food intake and body weight and prevent development of obesity by Zhang, Bei B, Air, Ellen L, Strowski, Mathias Z, Benoit, Stephen C, Conarello, Stacey L, Salituro, Gino M, Guan, Xiao-Ming, Liu, Kun, Woods, Stephen C

“…Obesity and insulin resistance are major risk factors for a number of metabolic disorders, such as type 2 diabetes mellitus. Insulin has been suggested to…”
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A novel method for preparing stabilized amorphous solid dispersion drug formulations using acoustic fusion by Guo, Zack, Boyce, Christopher, Rhodes, Timothy, Liu, Lina, Salituro, Gino M., Lee, Keun-joong, Bak, Annette, Leung, Dennis H.

“…Custom Acoustic Fusion Heating Block Assembly: Acoustic Mixing can be used to homogeneously mix high viscosity materials. Heating block designed and fabricated…”
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Development of a Convenient In Vitro Gel Diffusion Model for Predicting the In Vivo Performance of Subcutaneous Parenteral Formulations of Large and Small Molecules by Leung, Dennis H., Kapoor, Yash, Alleyne, Candice, Walsh, Erika, Leithead, Andrew, Habulihaz, Bahanu, Salituro, Gino M., Bak, Annette, Rhodes, Timothy

“…Parenteral delivery remains a compelling drug delivery route for both large- and small-molecule drugs and can bypass issues encountered with oral absorption…”
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Real-time PCR assay as a simple and efficient tool for viral stability study by Hu, Bing, Dopp, Jared L, Salituro, Gino M, Rubinstein, Leonard J

“…For oncolytic virus trials, regulatory agencies often require pharmaceutical industry to evaluate risks of released viruses from patients to environment. This…”
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Novel Sesquiterpenoids from the Fermentation of Xylaria persicaria Are Selective Ligands for the NPY Y5 Receptor by SMITH, Cameron J., MORIN, Nancy R., BILLS, Gerald F., DOMBROWSKI, Anne W., SALITURO, Gino M., SMITH, Scott K., ZHAO, Annie, MACNEIL, Douglas J.

“…Neuropeptide Y (NPY) is a polypeptide found in the peripheral and central nervous system and is involved in the regulation of feeding. Antagonists of NPY…”
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The Complestatins as HIV-1 Integrase Inhibitors. Efficient Isolation, Structure Elucidation, and Inhibitory Activities of Isocomplestatin, Chloropeptin I, New Complestatins, A and B, and Acid-Hydrolysis Products of Chloropeptin I by Singh, Sheo B, Jayasuriya, Hiranthi, Salituro, Gino M, Zink, Deborah L, Shafiee, Ali, Heimbuch, Brian, Silverman, Keith C, Lingham, Russell B, Genilloud, Olga, Teran, Ana, Vilella, Dolores, Felock, Peter, Hazuda, Daria

“…From the screening of a microbial extract library, isocomplestatin (1), a new axial-chiral isomer of complestatin (2) which is a known rigid bicyclic…”
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Quantitation of Super Basic Peptides in Biological Matrices by a Generic Perfluoropentanoic Acid-Based Liquid Chromatography–Mass Spectrometry Method by Wen, Jianzhong, Wang, Weixun, Lee, Keun-Joong, Choi, Bernard K., Harradine, Paul, Salituro, Gino M., Hittle, Lucinda

“…Peptides represent a promising modality for the design of novel therapeutics that can potentially modulate traditionally non-druggable targets…”
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Modulating Drug Release and Enhancing the Oral Bioavailability of Torcetrapib with Solid Lipid Dispersion Formulations by Liu, Yajun, Salituro, Gino M., Lee, Keun-joong, Bak, Annette, Leung, Dennis H.

“…The development of drug dispersions using solid lipids is a novel formulation strategy that can help address the challenges of poor drug solubility and…”
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Discovery of phenyl acetamides as potent and selective GPR119 agonists by Zhu, Cheng, Wang, Liping, Zhu, Yuping, Guo, Zack Zhiqiang, Liu, Ping, Hu, Zhiyong, Szewczyk, Jason W., Kang, Ling, Chicchi, Gary, Ehrhardt, Anka, Woods, Andrea, Seo, Toru, Woods, Morgan, van Heek, Margaret, Dingley, Karen H., Pang, Jianmei, Salituro, Gino M., Powell, Joyce, Terebetski, Jenna L., Hornak, Viktor, Campeau, Louis-Charles, Orr, Robert K., Ujjainwalla, Feroze, Miller, Michael, Stamford, Andrew, Wood, Harold B., Kowalski, Timothy, Nargund, Ravi P., Edmondson, Scott D.

“…[Display omitted] The paper describes the SAR/SPR studies that led to the discovery of phenoxy cyclopropyl phenyl acetamide derivatives as potent and selective…”
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Discovery of benzamides as potent human β3 adrenergic receptor agonists by Zhu, Cheng, Kar, Nam F., Li, Bing, Costa, Melissa, Dingley, Karen H., Di Salvo, Jerry, Ha, Sookhee N., Hurley, Amanda L., Li, Xiaofang, Miller, Randy R., Salituro, Gino M., Struthers, Mary, Weber, Ann E., Hale, Jeffrey J., Edmondson, Scott D.

“…[Display omitted] The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human…”
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Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder by Harper, Bart H., Wang, Liping, Zhu, Cheng, Kar, Nam F., Li, Bing, Moyes, Christopher R., Goble, Stephen D., Costa, Melissa, Dingley, Karen, Di Salvo, Jerry, Ha, Sookhee N., Hurley, Amanda, Li, Xiaofang, Miller, Randy R., Nagabukuro, Hiroshi, Salituro, Gino M., Smith, Sean, Struthers, Mary, Hale, Jeffrey J., Edmondson, Scott D., Berger, Richard

“…[Display omitted] The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β3-adrenergic receptor for the treatment of…”
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Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder by Harper, Bart H, Wang, Liping, Zhu, Cheng, Kar, Nam F, Li, Bing, Moyes, Christopher R, Goble, Stephen D, Costa, Melissa, Dingley, Karen, Di Salvo, Jerry, Ha, Sookhee N, Hurley, Amanda, Li, Xiaofang, Miller, Randy R, Nagabukuro, Hiroshi, Salituro, Gino M, Smith, Sean, Struthers, Mary, Hale, Jeffrey J, Edmondson, Scott D, Berger, Richard

“…The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β -adrenergic receptor for the treatment of overactive bladder…”
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Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes by Liu, Ping, Hu, Zhiyong, DuBois, Byron G, Moyes, Christopher R, Hunter, David N, Zhu, Cheng, Kar, Nam Fung, Zhu, Yuping, Garfunkle, Joie, Kang, Ling, Chicchi, Gary, Ehrhardt, Anka, Woods, Andrea, Seo, Toru, Woods, Morgan, van Heek, Margaret, Dingley, Karen H, Pang, Jianmei, Salituro, Gino M, Powell, Joyce, Terebetski, Jenna L, Hornak, Viktor, Campeau, Louis-Charles, Lamberson, Joe, Ujjainwalla, Fez, Miller, Michael, Stamford, Andrew, Wood, Harold B, Kowalski, Timothy, Nargund, Ravi P, Edmondson, Scott D

“…We report herein the design and synthesis of a series of potent and selective GPR119 agonists. Our objective was to develop a GPR119 agonist with properties…”
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Development of a Convenient In Vitro Gel Diffusion Model for Predicting the In Vivo Performance of Subcutaneous Parenteral Formulations of Large and Small Molecules by Leung, Dennis H., Kapoor, Yash, Alleyne, Candice, Walsh, Erika, Leithead, Andrew, Habulihaz, Bahanu, Salituro, Gino M., Bak, Annette, Rhodes, Timothy

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Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β₃ adrenergic receptor agonists by Morriello, Gregori J, Wendt, Harvey R, Bansal, Alka, Salvo, Jerry Di, Feighner, Scott, He, Jiafang, Hurley, Amanda L, Hreniuk, Donna L, Salituro, Gino M, Reddy, Marat Vijay, Galloway, Sheila M, McGettigan, Katherine K, Laws, George, McKnight, Crystal, Doss, George A, Tsou, Nancy N, Black, Regina M, Morris, Judy, Ball, Richard G, Sanfiz, Anthony T, Streckfuss, Eric, Struthers, Mary, Edmondson, Scott D

“…A novel class of human β₃-adrenergic receptor agonists was designed in effort to improve selectivity and metabolic stability versus previous disclosed β₃-AR…”
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Activation of Insulin Signal Transduction Pathway and Anti-diabetic Activity of Small Molecule Insulin Receptor Activators by Qureshi, Sajjad A., Ding, Victor, Li, Zhihua, Szalkowski, Deborah, Biazzo-Ashnault, Dawn E., Xie, Dan, Saperstein, Richard, Brady, Edward, Huskey, Su, Shen, Xiaolan, Liu, Kun, Xu, Libo, Salituro, Gino M., Heck, James V., Moller, David E., Jones, A. Brian, Zhang, Bei B.

“…We recently described the identification of a non-peptidyl fungal metabolite (l-783,281, compound 1), which induced activation of human insulin receptor (IR)…”
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Novel Sesquiterpenoids from the Fermentation of Xylaria p ersicaria Are Selective Ligands for the NPY Y5 Receptor by Smith, Cameron J, Morin, Nancy R, Bills, Gerald F, Dombrowski, Anne W, Salituro, Gino M, Smith, Scott K, Zhao, Annie, MacNeil, Douglas J

“…Neuropeptide Y (NPY) is a polypeptide found in the peripheral and central nervous system and is involved in the regulation of feeding. Antagonists of NPY…”
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