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26 results on '"Shahripour, Aurash"'

1. Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain

Author

Adams, Gregory L., primary, Pall, Parul S., additional, Grauer, Steven M., additional, Zhou, Xiaoping, additional, Ballard, Jeanine E., additional, Vavrek, Marissa, additional, Kraus, Richard L., additional, Morissette, Pierre, additional, Li, Nianyu, additional, Colarusso, Stefania, additional, Bianchi, Elisabetta, additional, Palani, Anandan, additional, Klein, Rebecca, additional, John, Christopher T., additional, Wang, Deping, additional, Tudor, Matthew, additional, Nolting, Andrew F., additional, Biba, Mirlinda, additional, Nowak, Timothy, additional, Makarov, Alexey A., additional, Reibarkh, Mikhail, additional, Buevich, Alexei V., additional, Zhong, Wendy, additional, Regalado, Erik L., additional, Wang, Xiao, additional, Gao, Qi, additional, Shahripour, Aurash, additional, Zhu, Yuping, additional, de Simone, Daniele, additional, Frattarelli, Tommaso, additional, Pasquini, Nicolo’ Maria, additional, Magotti, Paola, additional, Iaccarino, Roberto, additional, Li, Yuxing, additional, Solly, Kelli, additional, Lee, Keun-Joong, additional, Wang, Weixun, additional, Chen, Feifei, additional, Zeng, Haoyu, additional, Wang, Jixin, additional, Regan, Hilary, additional, Amin, Rupesh P., additional, Regan, Christopher P., additional, Burgey, Christopher S., additional, Henze, Darrell A., additional, Sun, Chengzao, additional, and Tellers, David M., additional

Published
2021
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2. A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors

Author

Tucker, Thomas J., primary, Embrey, Mark W., additional, Alleyne, Candice, additional, Amin, Rupesh P., additional, Bass, Alan, additional, Bhatt, Bhavana, additional, Bianchi, Elisabetta, additional, Branca, Danila, additional, Bueters, Tjerk, additional, Buist, Nicole, additional, Ha, Sookhee N., additional, Hafey, Mike, additional, He, Huaibing, additional, Higgins, John, additional, Johns, Douglas G., additional, Kerekes, Angela D., additional, Koeplinger, Kenneth A., additional, Kuethe, Jeffrey T., additional, Li, Nianyu, additional, Murphy, BethAnn, additional, Orth, Peter, additional, Salowe, Scott, additional, Shahripour, Aurash, additional, Tracy, Rodger, additional, Wang, Weixun, additional, Wu, Chengwei, additional, Xiong, Yusheng, additional, Zokian, Hratch J., additional, Wood, Harold B., additional, and Walji, Abbas, additional

Published
2021
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3. Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design

Author

Alleyne, Candice, primary, Amin, Rupesh P., additional, Bhatt, Bhavana, additional, Bianchi, Elisabetta, additional, Blain, J. Craig, additional, Boyer, Nicolas, additional, Branca, Danila, additional, Embrey, Mark W., additional, Ha, Sookhee N., additional, Jette, Kelli, additional, Johns, Douglas G., additional, Kerekes, Angela D., additional, Koeplinger, Kenneth A., additional, LaPlaca, Derek, additional, Li, Nianyu, additional, Murphy, Beth, additional, Orth, Peter, additional, Ricardo, Alonso, additional, Salowe, Scott, additional, Seyb, Kathleen, additional, Shahripour, Aurash, additional, Stringer, Joseph R., additional, Sun, Yili, additional, Tracy, Rodger, additional, Wu, Chengwei, additional, Xiong, Yusheng, additional, Youm, Hyewon, additional, Zokian, Hratch J., additional, and Tucker, Thomas J., additional

Published
2020
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5. Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold

Author

Zhu, Yuping, de Jesus, Reynalda K., Tang, Haifeng, Walsh, Shawn P., Jiang, Jinlong, Gu, Xin, Teumelsan, Nardos, Shahripour, Aurash, Pio, Barbara, Ding, Fa-Xiang, Ha, Sookhee, Priest, Birgit T., Swensen, Andrew M., Alonso-Galicia, Magdalena, Felix, John P., Brochu, Richard M., Bailey, Timothy, Thomas-Fowlkes, Brande, Zhou, Xiaoyan, Pai, Lee-Yuh, Hampton, Caryn, Hernandez, Melba, Owens, Karen, Ehrhart, Juliann, Roy, Sophie, Kaczorowski, Gregory J., Yang, Lihu, Parmee, Emma R., Sullivan, Kathleen, Garcia, Maria L., and Pasternak, Alexander

Published
2016
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6. Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation

Author

Walsh, Shawn P., Shahripour, Aurash, Tang, Haifeng, de Jesus, Reynalda K., Teumelsan, Nardos, Zhu, Yuping, Frie, Jessica, Priest, Birgit T., Swensen, Andrew M., Alonso-Galicia, Magdalena, Felix, John P., Brochu, Richard M., Bailey, Timothy, Thomas-Fowlkes, Brande, Zhou, Xiaoyan, Pai, Lee-Yuh, Hampton, Caryn, Hernandez, Melba, Owens, Karen, Ehrhart, Juliann, Roy, Sophie, Kaczorowski, Gregory J., Yang, Lihu, Garcia, Maria L., and Pasternak, Alexander

Published
2016
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7. Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, Part I: Transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors

Author

Plummer, Mark S., Cornicelli, Joseph, Roark, Howard, Skalitzky, Donald J., Stankovic, Charles J., Bove, Susan, Pandit, Jayvardhan, Goodman, Annise, Hicks, James, Shahripour, Aurash, Beidler, David, Lu, Xiao Kang, Sanchez, Brian, Whitehead, Christopher, Sarver, Ron, Braden, Timothy, Gowan, Richard, Shen, Xi Qiang, Welch, Katherine, Ogden, Adam, Sadagopan, Nalini, Baum, Heidi, Miller, Howard, Banotai, Craig, Spessard, Cindy, and Lightle, Sandra

Published
2013
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8. Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: Optimization studies and demonstration of in vivo efficacy

Author

Plummer, Mark S., Cornicelli, Joseph, Roark, Howard, Skalitzky, Donald J., Stankovic, Charles J., Bove, Susan, Pandit, Jayvardhan, Goodman, Annise, Hicks, James, Shahripour, Aurash, Beidler, David, Lu, Xiao Kang, Sanchez, Brian, Whitehead, Christopher, Sarver, Ron, Braden, Timothy, Gowan, Richard, Shen, Xi Qiang, Welch, Katherine, Ogden, Adam, Sadagopan, Nalini, Baum, Heidi, Miller, Howard, Banotai, Craig, Spessard, Cindy, and Lightle, Sandra

Published
2013
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9. Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure

Author

Tang, Haifeng, primary, Zhu, Yuping, additional, Teumelsan, Nardos, additional, Walsh, Shawn P., additional, Shahripour, Aurash, additional, Priest, Birgit T., additional, Swensen, Andrew M., additional, Felix, John P., additional, Brochu, Richard M., additional, Bailey, Timothy, additional, Thomas-Fowlkes, Brande, additional, Pai, Lee-Yuh, additional, Hampton, Caryn, additional, Corona, Aaron, additional, Hernandez, Melba, additional, Metzger, Joseph, additional, Forrest, Michael, additional, Zhou, Xiaoyan, additional, Owens, Karen, additional, Tong, Vincent, additional, Parmee, Emma, additional, Roy, Sophie, additional, Kaczorowski, Gregory J., additional, Yang, Lihu, additional, Alonso-Galicia, Magdalena, additional, Garcia, Maria L., additional, and Pasternak, Alexander, additional

Published
2016
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10. Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation

Author

Walsh, Shawn P., primary, Shahripour, Aurash, additional, Tang, Haifeng, additional, Teumelsan, Nardos, additional, Frie, Jessica, additional, Zhu, Yuping, additional, Priest, Birgit T., additional, Swensen, Andrew M., additional, Liu, Jessica, additional, Margulis, Michael, additional, Visconti, Richard, additional, Weinglass, Adam, additional, Felix, John P., additional, Brochu, Richard M., additional, Bailey, Timothy, additional, Thomas-Fowlkes, Brande, additional, Alonso-Galicia, Magdalena, additional, Zhou, Xiaoyan, additional, Pai, Lee-Yuh, additional, Corona, Aaron, additional, Hampton, Caryn, additional, Hernandez, Melba, additional, Bentley, Ross, additional, Chen, Jing, additional, Shah, Kashmira, additional, Metzger, Joseph, additional, Forrest, Michael, additional, Owens, Karen, additional, Tong, Vincent, additional, Ha, Sookhee, additional, Roy, Sophie, additional, Kaczorowski, Gregory J., additional, Yang, Lihu, additional, Parmee, Emma, additional, Garcia, Maria L., additional, Sullivan, Kathleen, additional, and Pasternak, Alexander, additional

Published
2015
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11. Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics

Author

Tang, Haifeng, primary, Walsh, Shawn P., additional, Yan, Yan, additional, de Jesus, Reynalda K., additional, Shahripour, Aurash, additional, Teumelsan, Nardos, additional, Zhu, Yuping, additional, Ha, Sookhee, additional, Owens, Karen A., additional, Thomas-Fowlkes, Brande S., additional, Felix, John P., additional, Liu, Jessica, additional, Kohler, Martin, additional, Priest, Birgit T., additional, Bailey, Timothy, additional, Brochu, Richard, additional, Alonso-Galicia, Magdalena, additional, Kaczorowski, Gregory J., additional, Roy, Sophie, additional, Yang, Lihu, additional, Mills, Sander G., additional, Garcia, Maria L., additional, and Pasternak, Alexander, additional

Published
2012
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12. 4-Anilino-5-carboxamido-2-pyridone Derivatives as Noncompetitive Inhibitors of Mitogen-Activated Protein Kinase Kinase

Author

Spicer, Julie A., primary, Rewcastle, Gordon W., additional, Kaufman, Michael D., additional, Black, Shannon L., additional, Plummer, Mark S., additional, Denny, William A., additional, Quin, John, additional, Shahripour, Aurash B., additional, Barrett, Stephen D., additional, Whitehead, Christopher E., additional, Milbank, Jared B. J., additional, Ohren, Jeffrey F., additional, Gowan, Richard C., additional, Omer, Charles, additional, Camp, Heidi S., additional, Esmaeil, Nadia, additional, Moore, Kelley, additional, Sebolt-Leopold, Judith S., additional, Pryzbranowski, Sally, additional, Merriman, Ronald L., additional, Ortwine, Daniel F., additional, Warmus, Joseph S., additional, Flamme, Cathlin M., additional, Pavlovsky, Alexander G., additional, and Tecle, Haile, additional

Published
2007
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14. Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide

Author

Shahripour, Aurash B, primary, Plummer, Mark S, additional, Lunney, Elizabeth A, additional, Sawyer, Tomi K, additional, Stankovic, Charles J, additional, Connolly, Michael K, additional, Rubin, John R, additional, Walker, Nigel P.C, additional, Brady, Kenneth D, additional, Allen, Hamish J, additional, Talanian, Robert V, additional, Wong, Winnie W, additional, and Humblet, Christine, additional

Published
2001
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16. The Role of 4-phosphonodifluoromethyl- and 4-phosphono-phenylalanine in the selectivity and cellular uptake of SH2 domain ligands

Author

Stankovic, Charles J., primary, Surendran, Narayanan, additional, Lunney, Elizabeth A., additional, Plummer, Mark S., additional, Para, Kimberly S., additional, Shahripour, Aurash, additional, Fergus, James H., additional, Marks, James S., additional, Herrera, Roman, additional, Hubbell, Susan E., additional, Humblet, Christine, additional, Saltiel, Alan R., additional, Stewart, Barbra H., additional, and Sawyer, Tomi K., additional

Published
1997
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18. Structure−Activity Relationships in a Series of Orally Active γ-Hydroxy Butenolide Endothelin Antagonists

Author

Patt, William C., primary, Edmunds, Jeremy J., additional, Repine, Joseph T., additional, Berryman, Kent A., additional, Reisdorph, Billy R., additional, Lee, Chet, additional, Plummer, Mark S., additional, Shahripour, Aurash, additional, Haleen, Stephen J., additional, Keiser, Joan A., additional, Flynn, Mike A., additional, Welch, Kathleen M., additional, Reynolds, Elwood E., additional, Rubin, Ron, additional, Tobias, Brian, additional, Hallak, Hussein, additional, and Doherty, Annette M., additional

Published
1997
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19. Design of peptidomimetic ligands for the pp60src SH2 domain

Author

Plummer, Mark S., primary, Lunney, Elizabeth A., additional, Para, Kimberly S., additional, Shahripour, Aurash, additional, Stankovic, Charles J., additional, Humblet, Christine, additional, Fergus, James H., additional, Marks, James S., additional, Herrera, Roman, additional, Hubbell, Susan, additional, Saltiel, Alan, additional, and Sawyer, Tomi K., additional

Published
1997
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20. Novel phosphotyrosine mimetics in the design of peptide ligands for pp60src SH2 domain

Author

Shahripour, Aurash, primary, Plummer, Mark S., additional, Lunney, Elizabeth A., additional, Para, Kimberly S., additional, Stankovic, Charles J., additional, Rubin, John R., additional, Humblet, Christine, additional, Fergus, James H., additional, Marks, James S., additional, Herrera, Roman, additional, Hubbell, Susan E., additional, Saltiel, Alan R., additional, and Sawyer, Tomi K., additional

Published
1996
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21. Design and Synthesis of Renin Inhibitors: Incorporation of Transition-State Isostere Side Chains That Span from the S1 to the S3 Binding Pockets and Examination of P3-Modified Renin Inhibitors

Author

Shahripour, Aurash, primary, Kaltenbronn, James S., additional, Lunney, Elizabeth A., additional, Steinbaugh, Bruce A., additional, Hamby, James M., additional, Hamilton, Harriet W., additional, Sawyer, Tomi K., additional, Humblet, Christine, additional, and Doherty, Annette M., additional

Published
1995
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23. Design of peptidomimetic ligands for the pp60srcSH2 domain

Author

Plummer, Mark S., Lunney, Elizabeth A., Para, Kimberly S., Shahripour, Aurash, Stankovic, Charles J., Humblet, Christine, Fergus, James H., Marks, James S., Herrera, Roman, Hubbell, Susan, Saltiel, Alan, and Sawyer, Tomi K.

Abstract

Potent ligands of the Src SH2 domain, discovered through structure-based drug design efforts, with the general structure Ac-pTyr-Glu-NRR′ are disclosed.

Published
1997
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26. Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na v 1.7 for the Treatment of Pain.

Author

Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, and Tellers DM

Subjects
Animals, Cell Degranulation drug effects, Cystine chemistry, Drug Design, Hot Temperature, Mast Cells drug effects, Models, Molecular, Pain Measurement drug effects, Rats, Spider Venoms pharmacology, NAV1.7 Voltage-Gated Sodium Channel drug effects, Pain drug therapy, Sodium Channel Blockers chemical synthesis, Sodium Channel Blockers pharmacology, Spider Venoms chemical synthesis
Abstract

Inhibitor cystine knot peptides, derived from venom, have evolved to block ion channel function but are often toxic when dosed at pharmacologically relevant levels in vivo . The article describes the design of analogues of ProTx-II that safely display systemic in vivo blocking of Na v 1.7, resulting in a latency of response to thermal stimuli in rodents. The new designs achieve a better in vivo profile by improving ion channel selectivity and limiting the ability of the peptides to cause mast cell degranulation. The design rationale, structural modeling, in vitro profiles, and rat tail flick outcomes are disclosed and discussed.

Published
2022
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