Search Results - "Fennell, Kimberly F."

Synthetic antibodies against BRIL as universal fiducial marks for single−particle cryoEM structure determination of membrane proteins by Mukherjee, Somnath, Erramilli, Satchal K., Ammirati, Mark, Alvarez, Frances J. D., Fennell, Kimberly F., Purdy, Michael D., Skrobek, Blazej M., Radziwon, Katarzyna, Coukos, John, Kang, Yanyong, Dutka, Przemysław, Gao, Xiang, Qiu, Xiayang, Yeager, Mark, Eric Xu, H., Han, Seungil, Kossiakoff, Anthony A.

“…We propose the concept of universal fiducials based on a set of pre-made semi-synthetic antibodies (sABs) generated by customized phage display selections…”
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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct by Pandit, Jayvardhan, Forman, Michael D, Fennell, Kimberly F, Dillman, Keith S, Menniti, Frank S

“…We report the X-ray crystal structure of a phosphodiesterase (PDE) that includes both catalytic and regulatory domains. PDE2A (215-900) crystallized as a dimer…”
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An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism by Lees, Joshua A., Dias, João M., Rajamohan, Francis, Fortin, Jean-Philippe, O’Connor, Rebecca, Kong, Jimmy X., Hughes, Emily A. G., Fisher, Ethan L., Tuttle, Jamison B., Lovett, Gabrielle, Kormos, Bethany L., Unwalla, Rayomand J., Zhang, Lei, Dechert Schmitt, Anne-Marie, Zhou, Dahui, Moran, Michael, Stevens, Kimberly A., Fennell, Kimberly F., Varghese, Alison E., Maxwell, Andrew, Cote, Emmaline E., Zhang, Yuan, Han, Seungil

“…GPR61 is an orphan GPCR related to biogenic amine receptors. Its association with phenotypes relating to appetite makes it of interest as a druggable target to…”
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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor by Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X

“…Phosphodiesterase 2A (PDE2A) inhibitors have been reported to demonstrate in vivo activity in preclinical models of cognition. To more fully explore the…”
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Discovery and structural characterization of an allosteric inhibitor of bacterial cis‐prenyltransferase by Danley, Dennis E., Baima, Eric T., Mansour, Mahmoud, Fennell, Kimberly F., Chrunyk, Boris A., Mueller, John P., Liu, Shenping, Qiu, Xiayang

“…Undecaprenyl pyrophosphate synthase (UPPs) is an essential enzyme in a key bacterial cell wall synthesis pathway. It catalyzes the consecutive condensations of…”
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Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4 by Londregan, Allyn T., Aitmakhanova, Karlygash, Bennett, James, Byrnes, Laura J., Canterbury, Daniel P., Cheng, Xiayun, Christott, Thomas, Clemens, Jennifer, Coffey, Steven B., Dias, João M., Dowling, Matthew S., Farnie, Gillian, Fedorov, Oleg, Fennell, Kimberly F., Gamble, Vicki, Gileadi, Carina, Giroud, Charline, Harris, Michael R., Hollingshead, Brett D., Huber, Kilian, Korczynska, Magdalena, Lapham, Kimberly, Loria, Paula M., Narayanan, Arjun, Owen, Dafydd R., Raux, Brigitt, Sahasrabudhe, Parag V., Ruggeri, Roger B., Sáez, Laura Díaz, Stock, Ingrid A., Thuma, Benjamin A., Tsai, Andy, Varghese, Alison E.

“…A series of small-molecule YEATS4 binders have been discovered as part of an ongoing research effort to generate high-quality probe molecules for emerging…”
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Machine Learning for Prioritization of Thermostabilizing Mutations for G-Protein Coupled Receptors by Muk, Sanychen, Ghosh, Soumadwip, Achuthan, Srisairam, Chen, Xiaomin, Yao, XiaoJie, Sandhu, Manbir, Griffor, Matthew C., Fennell, Kimberly F., Che, Ye, Shanmugasundaram, Veerabahu, Qiu, Xiayang, Tate, Christopher G., Vaidehi, Nagarajan

“…Although the three-dimensional structures of G-protein coupled receptors (GPCRs), the largest superfamily of drug targets, have enabled structure-based drug…”
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Structural basis of the acyl-transfer mechanism of human GPAT1 by Johnson, Zachary Lee, Ammirati, Mark, Wasilko, David Jonathan, Chang, Jeanne S., Noell, Stephen, Foley, Timothy L., Yoon, Hyejin, Smith, Kathleen, Asano, Shoh, Hales, Katherine, Wan, Min, Yang, Qingyi, Piotrowski, Mary A., Farley, Kathleen A., Gilbert, Tamara, Aschenbrenner, Lisa M., Fennell, Kimberly F., Dutra, Jason K., Xu, Mary, Guo, Chunyang, Varghese, Alison E., Bellenger, Justin, Quinn, Alandra, am Ende, Christopher W., West, Graham M., Griffor, Matthew C., Bennett, Donald, Calabrese, Matthew, Steppan, Claire M., Han, Seungil, Wu, Huixian

“…Glycerol-3-phosphate acyltransferase (GPAT)1 is a mitochondrial outer membrane protein that catalyzes the first step of de novo glycerolipid biosynthesis…”
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Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist by Schnute, Mark E, Wennerstål, Mattias, Alley, Jennifer, Bengtsson, Martin, Blinn, James R, Bolten, Charles W, Braden, Timothy, Bonn, Tomas, Carlsson, Bo, Caspers, Nicole, Chen, Ming, Choi, Chulho, Collis, Leon P, Crouse, Kimberly, Färnegårdh, Mathias, Fennell, Kimberly F, Fish, Susan, Flick, Andrew C, Goos-Nilsson, Annika, Gullberg, Hjalmar, Harris, Peter K, Heasley, Steven E, Hegen, Martin, Hromockyj, Alexander E, Hu, Xiao, Husman, Bolette, Janosik, Tomasz, Jones, Peter, Kaila, Neelu, Kallin, Elisabet, Kauppi, Björn, Kiefer, James R, Knafels, John, Koehler, Konrad, Kruger, Lars, Kurumbail, Ravi G, Kyne, Jr, Robert E, Li, Wei, Löfstedt, Joakim, Long, Scott A, Menard, Carol A, Mente, Scot, Messing, Dean, Meyers, Marvin J, Napierata, Lee, Nöteberg, Daniel, Nuhant, Philippe, Pelc, Matthew J, Prinsen, Michael J, Rhönnstad, Patrik, Backström-Rydin, Eva, Sandberg, Johnny, Sandström, Maria, Shah, Falgun, Sjöberg, Maria, Sundell, Aron, Taylor, Alexandria P, Thorarensen, Atli, Trujillo, John I, Trzupek, John D, Unwalla, Ray, Vajdos, Felix F, Weinberg, Robin A, Wood, David C, Xing, Li, Zamaratski, Edouard, Zapf, Christoph W, Zhao, Yajuan, Wilhelmsson, Anna, Berstein, Gabriel

“…The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune…”
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Use of Structure-Based Design to Discover a Potent, Selective, In Vivo Active Phosphodiesterase 10A Inhibitor Lead Series for the Treatment of Schizophrenia by Helal, Christopher J, Kang, Zhijun, Hou, Xinjun, Pandit, Jayvardhan, Chappie, Thomas A, Humphrey, John M, Marr, Eric S, Fennell, Kimberly F, Chenard, Lois K, Fox, Carol, Schmidt, Christopher J, Williams, Robert D, Chapin, Douglas S, Siuciak, Judith, Lebel, Lorraine, Menniti, Frank, Cianfrogna, Julia, Fonseca, Kari R, Nelson, Frederick R, O’Connor, Rebecca, MacDougall, Mary, McDowell, Laura, Liras, Spiros

“…Utilizing structure-based virtual library design and scoring, a novel chimeric series of phosphodiesterase 10A (PDE10A) inhibitors was discovered by…”
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Discovery of 3‑Cyano‑N‑(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)‑1H‑pyrrolo[2,3‑b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist by Schnute, Mark E, Wennerstål, Mattias, Alley, Jennifer, Bengtsson, Martin, Blinn, James R, Bolten, Charles W, Braden, Timothy, Bonn, Tomas, Carlsson, Bo, Caspers, Nicole, Chen, Ming, Choi, Chulho, Collis, Leon P, Crouse, Kimberly, Färnegårdh, Mathias, Fennell, Kimberly F, Fish, Susan, Flick, Andrew C, Goos-Nilsson, Annika, Gullberg, Hjalmar, Harris, Peter K, Heasley, Steven E, Hegen, Martin, Hromockyj, Alexander E, Hu, Xiao, Husman, Bolette, Janosik, Tomasz, Jones, Peter, Kaila, Neelu, Kallin, Elisabet, Kauppi, Björn, Kiefer, James R, Knafels, John, Koehler, Konrad, Kruger, Lars, Kurumbail, Ravi G, Kyne, Robert E, Li, Wei, Löfstedt, Joakim, Long, Scott A, Menard, Carol A, Mente, Scot, Messing, Dean, Meyers, Marvin J, Napierata, Lee, Nöteberg, Daniel, Nuhant, Philippe, Pelc, Matthew J, Prinsen, Michael J, Rhönnstad, Patrik, Backström-Rydin, Eva, Sandberg, Johnny, Sandström, Maria, Shah, Falgun, Sjöberg, Maria, Sundell, Aron, Taylor, Alexandria P, Thorarensen, Atli, Trujillo, John I, Trzupek, John D, Unwalla, Ray, Vajdos, Felix F, Weinberg, Robin A, Wood, David C, Xing, Li, Zamaratski, Edouard, Zapf, Christoph W, Zhao, Yajuan, Wilhelmsson, Anna, Berstein, Gabriel

“…The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune…”
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Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism by Ahn, Kay, Boehm, Markus, Brown, Matthew F, Calloway, Jessica, Che, Ye, Chen, Jinshan, Fennell, Kimberly F, Geoghegan, Kieran F, Gilbert, Adam M, Gutierrez, Jemy A, Kalgutkar, Amit S, Lanba, Adhiraj, Limberakis, Chris, Magee, Thomas V, O’Doherty, Inish, Oliver, Robert, Pabst, Brandon, Pandit, Jayvardhan, Parris, Kevin, Pfefferkorn, Jeffrey A, Rolph, Timothy P, Patel, Rushi, Schuff, Brandon, Shanmugasundaram, Veerabahu, Starr, Jeremy T, Varghese, Alison H, Vera, Nicholas B, Vernochet, Cecile, Yan, Jiangli

“…Lysophospholipase-like 1 (LYPLAL1) is an uncharacterized metabolic serine hydrolase. Human genome-wide association studies link variants of the gene encoding…”
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Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor by Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, LaChapelle, Erik A, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X

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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct by Pandit, Jayvardhan, Forman, Michael D., Fennell, Kimberly F., Dillman, Keith S., Menniti, Frank S.

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Discovery and structural characterization of an allosteric inhibitor of bacterial c is ‐prenyltransferase by Danley, Dennis E., Baima, Eric T., Mansour, Mahmoud, Fennell, Kimberly F., Chrunyk, Boris A., Mueller, John P., Liu, Shenping, Qiu, Xiayang

“…Abstract Undecaprenyl pyrophosphate synthase (UPPs) is an essential enzyme in a key bacterial cell wall synthesis pathway. It catalyzes the consecutive…”
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Activation of Human Liver Glycogen Phosphorylase by Alteration of the Secondary Structure and Packing of the Catalytic Core by Rath, Virginia L., Ammirati, Mark, LeMotte, Peter K., Fennell, Kimberly F., Mansour, Mahmoud N., Danley, Dennis E., Hynes, Thomas R., Schulte, Gayle K., Wasilko, David J., Pandit, Jayvardhan

“…Glycogen phosphorylases catalyze the breakdown of glycogen to glucose-1-phosphate, which enters glycolysis to fulfill the energetic requirements of the…”
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What The Structure Of Human Liver Glycogen Phosphorylase A Tells Us About Its Regulation by RATH, VIRGINIA L, AMMIRATI, MARK L, DANLEY, DENNIS E, FENNELL, KIMBERLY F, HYNES, THOMAS R, LEMOTTE, PETER K, MANSOUR, MAHMOUD N, SCHULTE, GAYLE K, WASILKO, DAVID J, PANDIT, JAYVARDHAN

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