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Allosteric modulation of neurotransmission
Biochemical PharmacologyThe therapeutic effects of allosteric modulators on neurotransmission are described. The two unique features of allosteric modulators are: (1) separate binding sites on proteins, and (2) the production of altered receptor conformation upon binding.openaire +2 more sourcesAllosteric Modulation of Dopamine Receptors
Mini-Reviews in Medicinal Chemistry, 2005 Allosteric modulators allow for the fine-tuning of receptor responses to endogenous neurotransmitters and exogenous therapeutic agents. Different types of allosteric modulation of dopamine receptors are discussed as well as the significance of such modulation in the control of normal biological processes and in the treatment of disease.openaire +2 more sourcesThe concept of allosteric modulation: an overview
Drug Discovery Today: Technologies, 2013 A brief historical overview of the concept of allosteric interaction is presented together with the different kinds of allosteric control recognized, in the past decades, with the model system of pentameric ligandgated ion channels. Multiple levels of allosteric modulation are identified that include sites distributed in the extracellular ligand ...openaire +2 more sourcesGPCR Allosteric Modulator Discovery
2019 G protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology; about one-third of all marketed drugs target members of this family. GPCR allosteric ligands hold the promise of improved subtype selectivity, spatiotemporal sensitivity, and possible biased property over typical orthosteric ligands.Yiran, Wu, Jiahui, Tong, Kang, Ding, Qingtong, Zhou, Suwen, Zhao +4 moreopenaire +2 more sourcesAllosteric Modulation of Intrinsically Disordered Proteins
2019 The allosteric property of globular proteins is applauded as their intrinsic ability to regulate distant sites, and this property further plays a critical role in a wide variety of cellular regulatory mechanisms. Recent advancements and studies have revealed the manifestation of allostery in intrinsically disordered proteins or regions as allosteric ...Ashfaq Ur, Rehman, Mueed Ur, Rahman, Taaha, Arshad, Hai-Feng, Chen +3 moreopenaire +2 more sourcesDifferential Allosteric Modulation of Cas9 Specificity
Journal of Chemical Theory and ComputationBoth RNA- and protein-based strategies have been developed to mitigate off-target cleavage by CRISPR-Cas9, yielding noncanonical guide RNAs (gRNAs) and Cas9 variants with enhanced gene-editing precision. However, the molecular mechanisms by which such PAM-distal alterations─remote from the nuclease centers─modulate Cas9 activity and specificity remain ...Yuanhao Li, Xin Li, Yingjie Chen, Yanqing Wang, Zhicheng Zuo +4 moreopenaire +2 more sourcesAllosteric Modulators
2010 Jean-Michel Scherrmann, Kim Wolff, Christine A. Franco, Marc N. Potenza, Tayfun Uzbay, Lisiane Bizarro, David C. S. Roberts, Robert L. Balster, Sharon L. Walsh, Barbara J. Mason, Charles J. Heyser, Anthony L. Riley, Steve Kohut, Marie-Louise G. Wadenberg, Heather Wilkins, Paul Newhouse, Anne Jackson, Joachim D. Uys, Peter W. Kalivas, Victoria L. Harvey, Tony Dickenson, Daniel Bertrand, Hans Rollema, Raymond S. Hurst, Gorkem Yararbas, Sakire Pogun, Marie-Louise G. Wadenberg, Debby Van Dam, Peter Paul De Deyn, Samuel G. Siris, Richard W. Foltin, Michael J. Kuhar, Robert L. Balster, Sharon L. Walsh, Robert L. Balster, Sharon L. Walsh, Michel Le Moal, Christoph Hiemke, Nicola Simola, Micaela Morelli, Nicola Simola, Micaela Morelli, Nicola Simola, Micaela Morelli, Alyson J. Bond, James J. Strain, R. Andrew Chambers, R. H. De Rijk, E. R. de Kloet, Bankole A. Johnson, Andreas Marneros, Suzanne H. Mitchell, Harriet de Wit, Mark Slifstein, Klaus A. Miczek, Rosa M. M. de Almeida, Emil F. Coccaro, David S. Baldwin, John Atack, Hilde Lavreysen, Rosa M. M. de Almeida, Klaus A. Miczek, Alyson J. Bond, Alfonso Abizaid, Shimon Amir, Samuel G. Siris, Joseph H. Friedman, Theodora Duka, Jelena Nesic, Falk Kiefer, Karl Mann, Bankole A. Johnson, Barbara J. Mason, Charles J. Heyser, Karl Mann, Falk Kiefer, Christopher L. Cunningham, Barbara J. Mason, Charles J. Heyser, Yesne Alici, William Breitbart, Subhash C. Pandey, Karl Mann, Falk Kiefer, Kieran O’Malley, Kieran O’Malley, Mitul A. Mehta, Linda Dykstra, John Atack, Hilde Lavreysen, Debby Van Dam, Peter Paul De Deyn, Holden D. Brown, Michael E. Ragozzino, Brian E. Leonard, Malcolm Lader, Peter J. Flor, Inga D. Neumann, Linda P. Spear, Holden D. Brown, Michael E. Ragozzino, Daniel Hoyer, Martina de Zwaan, Michael J. Owens, Chase H. Bourke, Philip J. Cowen, Pedro L. Delgado, Hiroyuki Uchida, Shitij Kapur, Harriet de Wit, Lawrence H. Price, Malcolm Lader, Husseini K. Manji, Jorge A. Quiroz, Seiya Miyamoto, Francisco Aboitiz, Ximena Carrasco, F. Xavier Castellanos, Michael J. Owens, Chase H. Bourke, Elizabeth C. Warburton, Husseini K. Manji, Jorge A. Quiroz, Linda Dykstra, James H. Woods, Mei-Chuan Ko, Gail Winger, Andrew Young, Jill B. Becker, Helen J. Cassaday, Paul Willner, Maria Isabel Colado, A. Richard Green, Marilyn E. Carroll, Peter A. Santi, Iván Izquierdo, Lia R. Bevilaqua, Martin Cammarota, Alfonso Abizaid, Shimon Amir, Jason C. G. Halford, Arthur Christopoulos, Gregory D. Stewart, Patrick M. Sexton, Sheldon Preskorn, Megan M. Dahmen, Jana Lincoln, Edoardo Spina, Brian E. Leonard, J. Craig Nelson, Meghan M. Grady, Stephen M. Stahl, Thomas R. E. Barnes, Michael M. Morgan, MacDonald J. Christie, Linda Dykstra, Joseph H. Friedman, Marie-Louise G. Wadenberg, Wiepke Cahn, Heleen B. M. Boos, H. D. Postma, Seiya Miyamoto, W. Wolfgang Fleischhacker, Samuel B. Hutton, Peter J. Flor, Inga D. Neumann, Inga D. Neumann, Peter J. Flor, Peter J. Flor, Inga D. Neumann, Grasielle C. Kincheski, Leandro J. Bertoglio, Antonio Pádua Carobrez, Helio Zangrossi, Frederico Guilherme Graeff, James Winslow, Yogita Chudasama, Paul Newhouse, Heather Wilkins, Naheed (Max) Mirza, Shuang Yu, Nuno Sousa, Osborne F. X. Almeida, Osborne F. X. Almeida, Nuno Sousa, Shuang Yu, Osborne F. X. Almeida, Nuno Sousa, Shuang Yu, Tim C. Kirkham, Tim C. Kirkham, Jason C. G. Halford, Ronald F. Mucha, Cecilia J. Hillard, Cecilia J. Hillard, Kim Wolff, Fiona Thomson, Susan Napier, Marie-Louise G. Wadenberg, Craig A. Erickson +199 moreopenaire +1 more source