Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design
Alleyne, Candice, Amin, Rupesh P, Bhatt, Bhavana, Bianchi, Elisabetta, Blain, J. Craig, Boyer, Nicolas, Branca, Danila, Embrey, Mark W, Ha, Sookhee N, Jette, Kelli, Johns, Douglas G, Kerekes, Angela D, Koeplinger, Kenneth A, LaPlaca, Derek, Li, Nianyu, Murphy, Beth, Orth, Peter, Ricardo, Alonso, Salowe, Scott, Seyb, Kathleen, Shahripour, Aurash, Stringer, Joseph R, Sun, Yili, Tracy, Rodger, Wu, Chengwei, Xiong, Yusheng, Youm, Hyewon, Zokian, Hratch J, Tucker, Thomas J
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Journal Article
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics
Tang, Haifeng, Walsh, Shawn P, Yan, Yan, de Jesus, Reynalda K, Shahripour, Aurash, Teumelsan, Nardos, Zhu, Yuping, Ha, Sookhee, Owens, Karen A, Thomas-Fowlkes, Brande S, Felix, John P, Liu, Jessica, Kohler, Martin, Priest, Birgit T, Bailey, Timothy, Brochu, Richard, Alonso-Galicia, Magdalena, Kaczorowski, Gregory J, Roy, Sophie, Yang, Lihu, Mills, Sander G, Garcia, Maria L, Pasternak, Alexander
Published in ACS medicinal chemistry letters (10.05.2012)
Published in ACS medicinal chemistry letters (10.05.2012)
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Journal Article
4-Anilino-5-carboxamido-2-pyridone Derivatives as Noncompetitive Inhibitors of Mitogen-Activated Protein Kinase Kinase
Spicer, Julie A, Rewcastle, Gordon W, Kaufman, Michael D, Black, Shannon L, Plummer, Mark S, Denny, William A, Quin, John, Shahripour, Aurash B, Barrett, Stephen D, Whitehead, Christopher E, Milbank, Jared B. J, Ohren, Jeffrey F, Gowan, Richard C, Omer, Charles, Camp, Heidi S, Esmaeil, Nadia, Moore, Kelley, Sebolt-Leopold, Judith S, Pryzbranowski, Sally, Merriman, Ronald L, Ortwine, Daniel F, Warmus, Joseph S, Flamme, Cathlin M, Pavlovsky, Alexander G, Tecle, Haile
Published in Journal of medicinal chemistry (18.10.2007)
Published in Journal of medicinal chemistry (18.10.2007)
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Journal Article
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors
Tucker, Thomas J, Embrey, Mark W, Alleyne, Candice, Amin, Rupesh P, Bass, Alan, Bhatt, Bhavana, Bianchi, Elisabetta, Branca, Danila, Bueters, Tjerk, Buist, Nicole, Ha, Sookhee N, Hafey, Mike, He, Huaibing, Higgins, John, Johns, Douglas G, Kerekes, Angela D, Koeplinger, Kenneth A, Kuethe, Jeffrey T, Li, Nianyu, Murphy, BethAnn, Orth, Peter, Salowe, Scott, Shahripour, Aurash, Tracy, Rodger, Wang, Weixun, Wu, Chengwei, Xiong, Yusheng, Zokian, Hratch J, Wood, Harold B, Walji, Abbas
Published in Journal of medicinal chemistry (25.11.2021)
Published in Journal of medicinal chemistry (25.11.2021)
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Journal Article
Structure-Based design of nonpeptide inhibitors of interleukin-1β converting enzyme (ICE, Caspase-1)
Shahripour, Aurash B, Plummer, Mark S, Lunney, Elizabeth A, Albrecht, Hans P, Hays, Sheryl J, Kostlan, Catherine R, Sawyer, Tomi K, Walker, Nigel P.C, Brady, Kenneth D, Allen, Hamish J, Talanian, Robert V, Wong, Winnie W, Humblet, Christine
Published in Bioorganic & medicinal chemistry (2002)
Published in Bioorganic & medicinal chemistry (2002)
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Journal Article
Discovery of a Novel Series of Orally Active Non-Peptide Endothelin-A (ETA) Receptor-Selective Antagonists
Doherty, Annette M, Patt, William C, Edmunds, Jeremy J, Berryman, Kent A, Reisdorph, Billy R, Plummer, Mark S, Shahripour, Aurash, Lee, Chet, Cheng, Xue-Min
Published in Journal of medicinal chemistry (01.04.1995)
Published in Journal of medicinal chemistry (01.04.1995)
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Journal Article
Design, Synthesis, and Cocrystal Structure of a Nonpeptide Src SH2 Domain Ligand
Plummer, Mark S, Holland, Debra R, Shahripour, Aurash, Lunney, Elizabeth A, Fergus, James H, Marks, James S, McConnell, Patrick, Mueller, W. Thomas, Sawyer, Tomi K
Published in Journal of medicinal chemistry (07.11.1997)
Published in Journal of medicinal chemistry (07.11.1997)
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Journal Article
Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide
Shahripour, Aurash B, Plummer, Mark S, Lunney, Elizabeth A, Sawyer, Tomi K, Stankovic, Charles J, Connolly, Michael K, Rubin, John R, Walker, Nigel P.C, Brady, Kenneth D, Allen, Hamish J, Talanian, Robert V, Wong, Winnie W, Humblet, Christine
Published in Bioorganic & medicinal chemistry letters (22.10.2001)
Published in Bioorganic & medicinal chemistry letters (22.10.2001)
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Journal Article
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain
Adams, Gregory L, Pall, Parul S, Grauer, Steven M, Zhou, Xiaoping, Ballard, Jeanine E, Vavrek, Marissa, Kraus, Richard L, Morissette, Pierre, Li, Nianyu, Colarusso, Stefania, Bianchi, Elisabetta, Palani, Anandan, Klein, Rebecca, John, Christopher T, Wang, Deping, Tudor, Matthew, Nolting, Andrew F, Biba, Mirlinda, Nowak, Timothy, Makarov, Alexey A, Reibarkh, Mikhail, Buevich, Alexei V, Zhong, Wendy, Regalado, Erik L, Wang, Xiao, Gao, Qi, Shahripour, Aurash, Zhu, Yuping, de Simone, Daniele, Frattarelli, Tommaso, Pasquini, Nicolo’ Maria, Magotti, Paola, Iaccarino, Roberto, Li, Yuxing, Solly, Kelli, Lee, Keun-Joong, Wang, Weixun, Chen, Feifei, Zeng, Haoyu, Wang, Jixin, Regan, Hilary, Amin, Rupesh P, Regan, Christopher P, Burgey, Christopher S, Henze, Darrell A, Sun, Chengzao, Tellers, David M
Published in Journal of medicinal chemistry (13.01.2022)
Published in Journal of medicinal chemistry (13.01.2022)
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Journal Article
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na v 1.7 for the Treatment of Pain
Adams, Gregory L, Pall, Parul S, Grauer, Steven M, Zhou, Xiaoping, Ballard, Jeanine E, Vavrek, Marissa, Kraus, Richard L, Morissette, Pierre, Li, Nianyu, Colarusso, Stefania, Bianchi, Elisabetta, Palani, Anandan, Klein, Rebecca, John, Christopher T, Wang, Deping, Tudor, Matthew, Nolting, Andrew F, Biba, Mirlinda, Nowak, Timothy, Makarov, Alexey A, Reibarkh, Mikhail, Buevich, Alexei V, Zhong, Wendy, Regalado, Erik L, Wang, Xiao, Gao, Qi, Shahripour, Aurash, Zhu, Yuping, de Simone, Daniele, Frattarelli, Tommaso, Pasquini, Nicolo' Maria, Magotti, Paola, Iaccarino, Roberto, Li, Yuxing, Solly, Kelli, Lee, Keun-Joong, Wang, Weixun, Chen, Feifei, Zeng, Haoyu, Wang, Jixin, Regan, Hilary, Amin, Rupesh P, Regan, Christopher P, Burgey, Christopher S, Henze, Darrell A, Sun, Chengzao, Tellers, David M
Published in Journal of medicinal chemistry (13.01.2022)
Published in Journal of medicinal chemistry (13.01.2022)
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Journal Article
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold
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., Pasternak, Alexander
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
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Journal Article
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
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, Lightle, Sandra
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
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Journal Article
Discovery of MK-7145, an Oral Small Molecule ROMK Inhibitor for the Treatment of Hypertension and Heart Failure
Tang, Haifeng, Zhu, Yuping, Teumelsan, Nardos, Walsh, Shawn P, Shahripour, Aurash, Priest, Birgit T, Swensen, Andrew M, Felix, John P, Brochu, Richard M, Bailey, Timothy, Thomas-Fowlkes, Brande, Pai, Lee-Yuh, Hampton, Caryn, Corona, Aaron, Hernandez, Melba, Metzger, Joseph, Forrest, Michael, Zhou, Xiaoyan, Owens, Karen, Tong, Vincent, Parmee, Emma, Roy, Sophie, Kaczorowski, Gregory J, Yang, Lihu, Alonso-Galicia, Magdalena, Garcia, Maria L, Pasternak, Alexander
Published in ACS medicinal chemistry letters (14.07.2016)
Published in ACS medicinal chemistry letters (14.07.2016)
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Journal Article
Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation
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., Pasternak, Alexander
Published in Bioorganic & medicinal chemistry letters (01.05.2016)
Published in Bioorganic & medicinal chemistry letters (01.05.2016)
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Journal Article
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
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, Lightle, Sandra
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
Published in Bioorganic & medicinal chemistry letters (01.06.2013)
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Journal Article
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation
Walsh, Shawn P, Shahripour, Aurash, Tang, Haifeng, Teumelsan, Nardos, Frie, Jessica, Zhu, Yuping, Priest, Birgit T, Swensen, Andrew M, Liu, Jessica, Margulis, Michael, Visconti, Richard, Weinglass, Adam, Felix, John P, Brochu, Richard M, Bailey, Timothy, Thomas-Fowlkes, Brande, Alonso-Galicia, Magdalena, Zhou, Xiaoyan, Pai, Lee-Yuh, Corona, Aaron, Hampton, Caryn, Hernandez, Melba, Bentley, Ross, Chen, Jing, Shah, Kashmira, Metzger, Joseph, Forrest, Michael, Owens, Karen, Tong, Vincent, Ha, Sookhee, Roy, Sophie, Kaczorowski, Gregory J, Yang, Lihu, Parmee, Emma, Garcia, Maria L, Sullivan, Kathleen, Pasternak, Alexander
Published in ACS medicinal chemistry letters (09.07.2015)
Published in ACS medicinal chemistry letters (09.07.2015)
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Journal Article
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
PASTERNAK ALEXANDER, ZHU YUPING, TEUMELSAN NARDOS H, YANG LIHU, SHAHRIPOUR AURASH, TANG HAIFENG, WALSH SHAWN P
Year of Publication 06.02.2012
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Year of Publication 06.02.2012
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Cyclic polypeptides for PCSK9 inhibition
Costantini, Willy, Tucker, Thomas Joseph, Boyer, Nicolas Cedric, Ingenito, Raffaele, Dhamnaskar, Ketki Ashok, Xiong, Yusheng, Ricardo, Alonso, Ma, Zhong, Kerekes, Angela Dawn, Shahripour, Aurash, Wu, Chengwei, Bianchi, Elisabetta, Branca, Danila, Ha, Sookhee Nicole, Youm, Hyewon
Year of Publication 19.03.2024
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Year of Publication 19.03.2024
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Cyclic polypeptides for PCSK9 inhibition
Costantini, Willy, Tucker, Thomas Joseph, Embrey, Mark W, Boyer, Nicolas Cedric, Ingenito, Raffaele, Conte, Immacolata, Xiong, Yusheng, Santoprete, Alessia, Colarusso, Stefania, Ricardo, Alonso, Kerekes, Angela Dawn, LaPlaca, Derek M, Shahripour, Aurash, Wu, Chengwei, Bianchi, Elisabetta, Branca, Danila, Stringer, Joseph R, Gilbert, Eric J, Costante, Roberto, Ha, Sookhee Nicole, Youm, Hyewon
Year of Publication 18.06.2024
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Year of Publication 18.06.2024
Patent
CYCLIC POLYPEPTIDES FOR PCSK9 INHIBITION
Costantini, Willy, Tucker, Thomas Joseph, Boyer, Nicolas Cedric, Ingenito, Raffaele, Dhamnaskar, Ketki Ashok, Xiong, Yusheng, Ricardo, Alonso, Ma, Zhong, Kerekes, Angela Dawn, Shahripour, Aurash, Wu, Chengwei, Bianchi, Elisabetta, Branca, Danila, Ha, Sookhee Nicole, Youm, Hyewon
Year of Publication 20.04.2023
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Year of Publication 20.04.2023
Patent