Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation

Por Gregory, Karen J., Conn, P. Jeffrey
Publicado no Mol Pharmacol (2015)

Allosteric Modulation of Muscarinic Acetylcholine Receptors

Por Gregory, Karen J, Sexton, Patrick M, Christopoulos, Arthur
Publicado em 2007

Allosteric Modulation of Metabotropic Glutamate Receptors: Structural Insights and Therapeutic Potential

Por Gregory, Karen J., Dong, Elizabeth N., Meiler, Jens, Conn, P. Jeffrey
Publicado em 2010

Stimulus Bias Provides Evidence for Conformational Constraints in the Structure of a G Protein-coupled Receptor

Por Gregory, Karen J., Sexton, Patrick M., Tobin, Andrew B., Christopoulos, Arthur
Publicado em 2012

Allosteric Modulation of Metabotropic Glutamate Receptors

Por Sheffler, Douglas J., Gregory, Karen J., Rook, Jerri M., Conn, P. Jeffrey
Publicado em 2011

Identification of Orthosteric and Allosteric Site Mutations in M(2) Muscarinic Acetylcholine Receptors That Contribute to Ligand-selective Signaling Bias

Por Gregory, Karen J., Hall, Nathan E., Tobin, Andrew B., Sexton, Patrick M., Christopoulos, Arthur
Publicado em 2010

Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: implications for optimizing preclinical neuroscience drug discovery

Por Sengmany, Kathy, Singh, Junaid, Stewart, Gregory D., Conn, P. Jeffrey, Christopoulos, Arthur, Gregory, Karen J.
Publicado no Neuropharmacology (2016)

A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity: MUSCARINIC PARTIAL AGONIST McN-A-343 AS A BITOPIC ORTHOSTERIC/ALLOSTERIC LIGAND

Por Valant, Celine, Gregory, Karen J., Hall, Nathan E., Scammells, Peter J., Lew, Michael J., Sexton, Patrick M., Christopoulos, Arthur
Publicado em 2008

Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators

Por Gregory, Karen J., Velagaleti, Ranganadh, Thal, David M., Brady, Ryan M., Christopoulos, Arthur, Conn, P. Jeffrey, Lapinsky, David J.
Publicado no ACS Chem Biol (2016)

Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology

Por Hammond, Alexis S., Rodriguez, Alice L., Townsend, Steven D., Niswender, Colleen M., Gregory, Karen J., Lindsley, Craig W., Conn, P. Jeffrey
Publicado em 2010

Structure-Activity Analysis of Biased Agonism at the Human Adenosine A(3) Receptor

Por Baltos, Jo-Anne, Paoletta, Silvia, Nguyen, Anh T. N., Gregory, Karen J., Tosh, Dilip K., Christopoulos, Arthur, Jacobson, Kenneth A., May, Lauren T.
Publicado no Mol Pharmacol (2016)

Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors

Por Lindsley, Craig W., Emmitte, Kyle A., Hopkins, Corey R., Bridges, Thomas M., Gregory, Karen J., Niswender, Colleen M., Conn, P. Jeffrey
Publicado no Chem Rev (2016)

Selective Actions of Novel Allosteric Modulators Reveal Functional Heteromers of Metabotropic Glutamate Receptors in the CNS

Por Yin, Shen, Noetzel, Meredith J., Johnson, Kari A., Zamorano, Rocio, Jalan-Sakrikar, Nidhi, Gregory, Karen J., Conn, P. Jeffrey, Niswender, Colleen M.
Publicado em 2014

Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor

Por Leach, Katie, Gregory, Karen J, Kufareva, Irina, Khajehali, Elham, Cook, Anna E, Abagyan, Ruben, Conigrave, Arthur D, Sexton, Patrick M, Christopoulos, Arthur
Publicado no Cell Res (2016)

Probing the Metabotropic Glutamate Receptor 5 (mGlu(5)) Positive Allosteric Modulator (PAM) Binding Pocket: Discovery of Point Mutations That Engender a “Molecular Switch” in PAM P...

Por Gregory, Karen J., Nguyen, Elizabeth D., Reiff, Sean D., Squire, Emma F., Stauffer, Shaun R., Lindsley, Craig W., Meiler, Jens, Conn, P. Jeffrey
Publicado em 2013

Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator()

Por Wu, Huixian, Wang, Chong, Gregory, Karen J., Han, Gye Won, Cho, Hyekyung P., Xia, Yan, Niswender, Colleen M., Katritch, Vsevolod, Meiler, Jens, Cherezov, Vadim, Conn, P. Jeffrey, Stevens, Raymond C.
Publicado em 2014

Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

Por Gregory, Karen J., Noetzel, Meredith J., Rook, Jerri M., Vinson, Paige N., Stauffer, Shaun R., Rodriguez, Alice L., Emmitte, Kyle A., Zhou, Ya, Chun, Aspen C., Felts, Andrew S., Chauder, Brian A., Lindsley, Craig W., Niswender, Colleen M., Conn, P. Jeffrey
Publicado em 2012

Identification of Specific Ligand–Receptor Interactions That Govern Binding and Cooperativity of Diverse Modulators to a Common Metabotropic Glutamate Receptor 5 Allosteric Site

Por Gregory, Karen J., Nguyen, Elizabeth D., Malosh, Chrysa, Mendenhall, Jeffrey L., Zic, Jessica Z., Bates, Brittney S., Noetzel, Meredith J., Squire, Emma F., Turner, Eric M., Rook, Jerri M., Emmitte, Kyle A., Stauffer, Shaun R., Lindsley, Craig W., Meiler, Jens, Conn, P. Jeffrey
Publicado em 2014

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy

Por Nickols, Hilary Highfield, Yuh, Joannes P., Gregory, Karen J., Morrison, Ryan D., Bates, Brittney S., Stauffer, Shaun R., Emmitte, Kyle A., Bubser, Michael, Peng, Weimin, Nedelcovych, Michael T., Thompson, Analisa, Lv, Xiaohui, Xiang, Zixiu, Daniels, J. Scott, Niswender, Colleen M., Lindsley, Craig W., Jones, Carrie K., Conn, P. Jeffrey
Publicado no J Pharmacol Exp Ther (2016)

Discovery of (2-(2-Benzoxazoyl amino)-4-Aryl-5-Cyanopyrimidine mGlu(5) NAMs: From Artificial Neural Network Virtual Screen to in vivo Tool Compound

Por Mueller, Ralf, Dawson, Eric S., Meiler, Jens, Rodriguez, Alice L., Chauder, Brian A., Bates, Brittney S., Felts, Andrew S., Lamb, Jeffrey P., Menon, Usha N., Jadhav, Sataywan B., Kane, Alexander S., Jones, Carrie K., Gregory, Karen J., Niswender, Colleen M., Conn, P. Jeffrey, Olsen, Christopher M., Winder, Danny G., Emmitte, Kyle A., Lindsley, Craig W.
Publicado em 2012