Novel Allosteric Modulators of G Protein-coupled Receptors

Por Gentry, Patrick R., Sexton, Patrick M., Christopoulos, Arthur
Publicado no J Biol Chem (2015)

Drugs for Allosteric Sites on Receptors

Por Wenthur, Cody J., Gentry, Patrick R., Mathews, Thomas P., Lindsley, Craig W.
Publicado em 2013

Chemical Lead Optimization of a pan G(q) mAChR M(1), M(3), M(5) Positive Allosteric Modulator (PAM) Lead. Part II. Development of potent and highly selective M(1) PAM

Por Bridges, Thomas M., Kennedy, J. Phillip, Noetzel, Meredith J., Breininger, Micah L., Gentry, Patrick R., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2010

Synthesis and SAR of a Novel Positive Allosteric Modulator (PAM) of the Metabotropic Glutamate Receptor 4 (mGluR4)

Por Williams, Richard, Johnson, Kari A., Gentry, Patrick R., Niswender, Colleen M., Weaver, Charles D., Conn, P. Jeffrey, Lindsley, Craig W., Hopkins, Corey R.
Publicado em 2009

Chemical Lead Optimization of a pan G(q) mAChR M(1), M(3), M(5) Positive Allosteric Modulator (PAM) Lead. Part I. Development of the first highly selective M(5) PAM

Por Bridges, Thomas M., Kennedy, J. Phillip, Cho, Hyekyung P., Breininger, Micah L., Gentry, Patrick R., Hopkins, Corey R., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

In Vivo Structure Activity Relationship Study of Dorsomorphin Analogs Identifies Selective VEGF and BMP Inhibitors

Por Hao, Jijun, Ho, Joshua N., Lewis, Jana A., Karim, Kaleh A., Daniels, R. Nathan, Gentry, Patrick R., Hopkins, Corey R., Lindsley, Craig W., Hong, Charles C.
Publicado em 2010

Synthesis and Structure–Activity Relationships of Allosteric Potentiators of the M(4) Muscarinic Acetylcholine Receptor

Por Kennedy, J. Phillip, Bridges, Thomas M., Gentry, Patrick R., Brogan, John T., Kane, Alexander S., Jones, Carrie K., Brady, Ashley E., Shirey, Jana K., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Por Engers, Darren W., Gentry, Patrick R., Williams, Richard, Bolinger, Julie L., Weaver, C. David, Menon, Usha N., Conn, P. Jeffrey, Lindsley, Craig W., Niswender, Colleen M., Hopkins, Corey R.
Publicado em 2010

M(5) Receptor Activation Produces Opposing Physiological Outcomes in Dopamine Neurons Depending on the Receptor's Location

Por Foster, Daniel J., Gentry, Patrick R., Lizardi-Ortiz, Jose E., Bridges, Thomas M., Wood, Michael R., Niswender, Colleen M., Sulzer, David, Lindsley, Craig W., Xiang, Zixiu, Conn, P. Jeffrey
Publicado em 2014

Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isati...

Por Bridges, Thomas M., Marlo, Joy E., Niswender, Colleen M., Jones, Carrie K., Jadhav, Satyawan B., Gentry, Patrick R., Plumley, Hyekyung C., Weaver, C. David, Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2009

Further optimization of the M(5) NAM MLPCN probe ML375: Tactics and challenges

Por Kurata, Haruto, Gentry, Patrick R., Kokubo, Masaya, Cho, Hyekyung P., Bridges, Thomas M., Niswender, Colleen M., Byers, Frank W., Wood, Michael R., Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W.
Publicado no Bioorg Med Chem Lett (2014)

Spirocyclic replacements for the isatin in the highly selective, muscarinic M(1) PAM ML137: the continued optimization of an MLPCN probe molecule

Por Poslusney, Michael S., Melancon, Bruce J., Gentry, Patrick R., Sheffler, Douglas J., Bridges, Thomas M., Utley, Thomas J., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Wood, Michael R.
Publicado em 2013

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I. Exploration of alternative benzyl and privileged structure moieties

Por Bridges, Thomas M., Brady, Ashley E., Kennedy, J. Phillip, Daniels, R. Nathan, Miller, Nicole R., Kim, Kwango, Breininger, Micah L., Gentry, Patrick R., Brogan, John T., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2008

Development of a Highly Potent, Novel M(5) Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piper...

Por Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Noetzel, Meredith J., Cho, Hyekyung P., Lamsal, Atin, Smith, Emery, Chase, Peter, Hodder, Peter S., Niswender, Colleen M., Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W., Wood, Michael R.
Publicado em 2014

Centrally Active Allosteric Potentiators of the M(4) Muscarinic Acetylcholine Receptor Reverse Amphetamine-Induced Hyperlocomotor Activity in Rats

Por Brady, Ashley E., Jones, Carrie K., Bridges, Thomas M., Kennedy, J. Phillip, Thompson, Analisa D., Heiman, Justin U., Breininger, Micah L., Gentry, Patrick R., Yin, Huiyong, Jadhav, Satyawan B., Shirey, Jana K., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2008

Isatin replacements applied to the highly selective, muscarinic M(1) PAM ML137: Continued optimization of an MLPCN probe molecule

Por Melancon, Bruce J., Poslusney, Michael S., Gentry, Patrick R., Tarr, James C., Sheffler, Douglas J., Mattmann, Margrith E., Bridges, Thomas M., Utley, Thomas J., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W., Wood, Michael R.
Publicado em 2012

Discovery of the first M(5)-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-...

Por Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Kett, Nathan R., Harp, Joel M., Cho, Hyekyung P., Smith, Emery, Chase, Peter, Hodder, Peter S., Niswender, Colleen M., Daniels, J. Scott, Conn, P. Jeffrey, Wood, Michael R., Lindsley, Craig W.
Publicado em 2013

Discovery of (S)-2-Cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): A Novel, CNS Penetrant Glucagon-Like Pep...

Por Morris, Lindsey C., Nance, Kellie D., Gentry, Patrick R., Days, Emily L., Weaver, C. David, Niswender, Colleen M., Thompson, Analisa D., Jones, Carrie K., Locuson, Chuck W., Morrison, Ryan D., Daniels, J. Scott, Niswender, Kevin D., Lindsley, Craig W.
Publicado no J Med Chem (2014)

Discovery, synthesis and characterization of a highly mAChR selective M(5) orthosteric antagonist, VU0488130 (ML381): a novel molecular probe

Por Gentry, Patrick R., Kokubo, Masaya, Bridges, Thomas M., Cho, Hyekyung P., Smith, Emery, Chase, Peter, Hodder, Peter S., Utley, Thomas J., Rajapakse, Anuruddha, Byers, Frank, Niswender, Colleen M., Morrison, Ryan D., Daniels, J. Scott, Wood, Michael R., Conn, P. Jeffrey, Lindsley, Craig W.
Publicado em 2014

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

Por Gogliotti, Rocco D., Engers, Darren W., Garcia-Barrantes, Pedro M., Panarese, Joseph D., Gentry, Patrick R., Blobaum, Anna L., Morrison, Ryan D., Daniels, J. Scott, Thompson, Analisa D., Jones, Carrie K., Conn, P. Jeffrey, Niswender, Colleen M., Lindsley, Craig W., Hopkins, Corey R.
Publicado no Bioorg Med Chem Lett (2016)