Hyekyung P. Cho

发表

Cloning, Expression, and Nutritional Regulation of the Mammalian Δ-6 Desaturase*

Manabu T. Nakamura, S. Clarke, Hyekyung P. Cho, 1999, The Journal of Biological Chemistry.

Cdc14B depletion leads to centriole amplification, and its overexpression prevents unscheduled centriole duplication

Yi-Song Wang, Hyekyung P. Cho, Dabney K. Johnson, 2008, The Journal of cell biology.

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.

N. Brandon, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 2017, Bioorganic & medicinal chemistry letters.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

Jens Meiler, Raymond C. Stevens, Colleen M. Niswender, 2014, Science.

Phospholipase D1 is required for angiogenesis of intersegmental blood vessels in zebrafish.

H. Brown, Hyekyung P. Cho, T. Zhong, 2009, Developmental biology.

Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity

F. Dudek, K. Gregory, Z. Xiang, 2013, Biological Psychiatry.

Design and Synthesis of Systemically Active Metabotropic Glutamate Subtype-2 and -3 (mGlu2/3) Receptor Positive Allosteric Modulators (PAMs): Pharmacological Characterization and Assessment in a Rat Model of Cocaine Dependence

D. Sheffler, A. Der-Avakian, N. Cosford, 2014, Journal of medicinal chemistry.

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators

Andrew S. Felts, C. Lindsley, Hyekyung P. Cho, 2018, Molecular Pharmacology.

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, ACS chemical neuroscience.

Novel Allosteric Agonists of M1 Muscarinic Acetylcholine Receptors Induce Brain Region-Specific Responses That Correspond with Behavioral Effects in Animal Models

M. Foster Olive, J. Scott Daniels, P. Jeffrey Conn, 2012, The Journal of Neuroscience.

Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.

Sarah A. Scott, C. Lindsley, H. Brown, 2009, Nature chemical biology.

Metabolism and functions of highly unsaturated fatty acids: An update

Manabu T. Nakamura, S. Clarke, Hyekyung P. Cho, 2001, Lipids.

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators

Anna L. Blobaum, J. Cheer, C. Lindsley, 2018, Molecular Psychiatry.

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.

J. P. Kennedy, C. Lindsley, C. Hopkins, 2010, Bioorganic & medicinal chemistry letters.

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2017, Journal of medicinal chemistry.

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Brian A. Chauder, Bruce J. Melancon, D. Sheffler, 2012, Bioorganic & medicinal chemistry letters.

Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

D. Sheffler, C. Lindsley, C. Hopkins, 2013, Bioorganic & medicinal chemistry letters.

Functional impact of allosteric agonist activity of selective positive allosteric modulators of mGlu 5 in regulating CNS function

H. Lavreysen, Z. Xiang, C. Lindsley, 2011 .

Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.

S. P. Moran, Anna L. Blobaum, C. Lindsley, 2016, ACS chemical neuroscience.

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2015, Bioorganic & medicinal chemistry letters.

Discovery, Synthesis and Characterization of a Highly Muscarinic Acetylcholine Receptor (mAChR)‐Selective M5‐Orthosteric Antagonist, VU0488130 (ML381): A Novel Molecular Probe

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, ChemMedChem.

Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

D. Sheffler, C. Lindsley, Hyekyung P. Cho, 2011, Bioorganic & medicinal chemistry letters.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2015, Bioorganic & medicinal chemistry letters.

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.

J. P. Kennedy, C. Lindsley, C. Hopkins, 2010, Bioorganic & medicinal chemistry letters.

Huixian Wu Bound to an Allosteric Modulator Structure of a Class C GPCR Metabotropic Glutamate Receptor

R. Stevens, K. Gregory, V. Katritch, 2014 .

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

Andrew S. Felts, Anna L. Blobaum, C. Lindsley, 2018, Journal of medicinal chemistry.

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core.

Julie L. Engers, Andrew S. Felts, Anna L. Blobaum, 2017, ACS medicinal chemistry letters.

Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2016, Bioorganic & medicinal chemistry letters.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2016, Bioorganic & medicinal chemistry letters.

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2016, Bioorganic & medicinal chemistry letters.

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics

Anna L. Blobaum, Z. Xiang, C. Lindsley, 2015, Journal of medicinal chemistry.

M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition

S. P. Moran, Z. Xiang, C. Lindsley, 2018, Neuropsychopharmacology.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Bruce J. Melancon, N. Brandon, C. Lindsley, 2017, Bioorganic & medicinal chemistry letters.

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.

Andrew S. Felts, Anna L. Blobaum, N. Schnetz-Boutaud, 2022, Journal of medicinal chemistry.

A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.

S. P. Moran, Anna L. Blobaum, C. Lindsley, 2018, ACS chemical neuroscience.

PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems.

S. P. Moran, C. Lindsley, Hyekyung P. Cho, 2018, ACS chemical neuroscience.

Sterol Regulatory Element Binding Protein-1 Expression Is Suppressed by Dietary Polyunsaturated Fatty Acids

Manabu T. Nakamura, S. Clarke, Hyekyung P. Cho, 1999, The Journal of Biological Chemistry.

Synthesis and Biological Evaluation of Cremastrine and an Unnatural Analogue.

C. Lindsley, Hyekyung P. Cho, O. Fadeyi, 2012, Tetrahedron letters.

Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function

H. Lavreysen, Z. Xiang, C. Lindsley, 2012, Molecular Pharmacology.

Regulation of Hepatic Δ-6 Desaturase Expression and Its Role in the Polyunsaturated Fatty Acid Inhibition of Fatty Acid Synthase Gene Expression in Mice

Manabu T. Nakamura, S. Clarke, Hyekyung P. Cho, 2000 .

The Dual-Specificity Phosphatase CDC14B Bundles and Stabilizes Microtubules

Yi-Song Wang, M. Tyers, Hyekyung P. Cho, 2005, Molecular and Cellular Biology.

Cloning, Expression, and Fatty Acid Regulation of the Human Δ-5 Desaturase*

Manabu T. Nakamura, S. Clarke, Hyekyung P. Cho, 1999, The Journal of Biological Chemistry.

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

Anna L. Blobaum, D. Sheffler, C. Lindsley, 2012, ACS chemical neuroscience.

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.

Julie L. Engers, Anna L. Blobaum, C. Lindsley, 2017, ACS chemical neuroscience.

Regulation of Phospholipase D Activity and Phosphatidic Acid Production after Purinergic (P2Y6) Receptor Stimulation*

Sarah A. Scott, C. Lindsley, H. Brown, 2013, The Journal of Biological Chemistry.

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2013, Bioorganic & medicinal chemistry letters.

Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

Julie L. Engers, C. Lindsley, Hyekyung P. Cho, 2021, ACS pharmacology & translational science.

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

D. Sheffler, Z. Xiang, C. Lindsley, 2011, Bioorganic & medicinal chemistry letters.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Peter Chase, P Jeffrey Conn, Craig W Lindsley, 2013, Journal of medicinal chemistry.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Alice E. Berizzi, C. Langmead, P. Sexton, 2018, ACS chemical neuroscience.

Development of a Highly Potent, Novel M5 Positive Allosteric Modulator (PAM) Demonstrating CNS Exposure: 1-((1H-Indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380)

C. Lindsley, Hyekyung P. Cho, P. Conn, 2014, Journal of medicinal chemistry.

N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.

Andrew S. Felts, C. Lindsley, Hyekyung P. Cho, 2013, Bioorganic & medicinal chemistry letters.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Alison R. Gregro, Andrew S. Felts, N. Schnetz-Boutaud, 2019, Bioorganic & medicinal chemistry letters.

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & medicinal chemistry letters.

Discovery of a Novel Class of Heteroaryl-Pyrrolidinones as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1.

Anna L. Blobaum, O. Boutaud, C. Lindsley, 2021, Bioorganic & medicinal chemistry letters.

The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.

Anna L. Blobaum, C. Lindsley, Hyekyung P. Cho, 2018, Bioorganic & medicinal chemistry letters.

Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics

C. Lindsley, C. Hopkins, Hyekyung P. Cho, 2014, ACS chemical biology.

Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & Medicinal Chemistry Letters.

Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.

C. Lindsley, Hyekyung P. Cho, P. Conn, 2017, Bioorganic & medicinal chemistry letters.

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

R. Stevens, K. Gregory, V. Katritch, 2014, Science.

Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function

H. Lavreysen, C. Lindsley, Hyekyung P. Cho, 2012, Molecular Pharmacology.

Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.

O. Boutaud, C. Lindsley, Joshua A. Bauer, 2023, Bioorganic & medicinal chemistry letters.

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators

J. Cheer, C. Lindsley, Hyekyung P. Cho, 2018, Molecular Psychiatry.