B. Melancon

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The succinct synthesis of AT13387, a clinically relevant Hsp90 inhibitor

Bruce J. Melancon, A. Bhardwaj, J. Kaur, 2019, Synthetic communications.

The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

Bruce J. Melancon, Z. Xiang, O. McManus, 2011, ACS chemical neuroscience.

Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α.

Bruce J. Melancon, B. LaFleur, A. Waterson, 2010, Nature chemical biology.

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Bruce J. Melancon, A. Christopoulos, C. Lindsley, 2012, Journal of medicinal chemistry.

Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Bruce J. Melancon, D. Sheffler, C. Lindsley, 2012, Bioorganic & medicinal chemistry letters.

Structural insights into HDAC6 tubulin deacetylation and its selective inhibition.

Bruce J. Melancon, M. Saito, P. Helquist, 2016, Nature chemical biology.

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.

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.

Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, D. Sheffler, 2013, Bioorganic & medicinal chemistry letters.

Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.

Craig W Lindsley, Bruce J. Melancon, Bruce J Melancon, 2013, Drug discovery today.

Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents

Bruce J. Melancon, J. Wess, N. Brandon, 2014, ACS chemical neuroscience.

Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model

C. Lindsley, P. Conn, C. Niswender, 2016, Neuropsychopharmacology.

Preview : Published ahead of advance online publication

C. Lindsley, P. Conn, C. Niswender, 2015 .

Allosteric modulation of the M 1 muscarinic acetylcholine receptor : improving cognition and a potential treatment for schizophrenia and Alzheimer ’ s disease

Bruce J. Melancon, C. Lindsley, Joseph D. Panarese, 2013 .

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.

Phosphodiesterase 10 A Regulates Alcohol and Saccharin Self-Administration in Rats

Robert L Barry, John C Gore, P Jeffrey Conn, 2014 .

Correction: A Structural Model for Binding of the Serine-Rich Repeat Adhesin GspB to Host Carbohydrate Receptors

Bruce J. Melancon, M. Tyska, T. Iverson, 2012, PLoS Pathogens.

A Structural Model for Binding of the Serine-Rich Repeat Adhesin GspB to Host Carbohydrate Receptors

Bruce J. Melancon, Matthew J. Tyska, Nicholas J. Ward, 2011, PLoS pathogens.

Development of a target-free high throughput screening platform for the discovery of anti-leishmanial compounds.

Bruce J. Melancon, M. Morales, D. Shoue, 2019, International journal of antimicrobial agents.

Identification of Positive Allosteric Modulators VU0155094 (ML397) and VU0422288 (ML396) Reveals New Insights into the Biology of Metabotropic Glutamate Receptor 7

Bruce J. Melancon, K. Gregory, Z. Xiang, 2014, ACS chemical neuroscience.

Inhibition of Histone Deacetylases 1, 2, and 3 Enhances Clearance of Cholesterol Accumulation in Niemann-Pick C1 Fibroblasts

Bruce J. Melancon, O. Wiest, F. Maxfield, 2021, ACS pharmacology & translational science.

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.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

C. Lindsley, P. Conn, C. Niswender, 2019, Bioorganic & medicinal chemistry letters.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

Bruce J. Melancon, Anna L. Blobaum, N. Brandon, 2017, ACS medicinal chemistry letters.

Influence of M1 muscarinic acetylcholine receptor activation on arousal and cognitive performance using electroencephalography and novel touchscreen cognition assessment (845.5)

J. Wess, Z. Xiang, C. Lindsley, 2014 .

mGlu1-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice

Bruce J. Melancon, C. Lindsley, C. Niswender, 2022, Neuropsychopharmacology.

Chromophore formation in resorcinarene solutions and the visual detection of mono- and oligosaccharides.

Bruce J. Melancon, R. Strongin, J. O. Escobedo, 2002, Journal of the American Chemical Society.

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.

Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.

Bruce J. Melancon, Z. Xiang, C. Lindsley, 2021, Bioorganic & medicinal chemistry letters.

mGlu1-mediated restoration of prefrontal cortex inhibitory signaling reverses social and cognitive deficits in an NMDA hypofunction model in mice

C. Lindsley, C. Niswender, D. Luessen, 2022, Neuropsychopharmacology.

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.

Julie L. Engers, Bruce J. Melancon, H. Hamm, 2014, Bioorganic & medicinal chemistry letters.

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.

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

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs.

Anna L. Blobaum, O. Boutaud, C. Lindsley, 2020, Bioorganic & medicinal chemistry letters.

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Alison R. Gregro, Julie L. Engers, Bruce J. Melancon, 2016, Bioorganic & medicinal chemistry letters.

2-Hydroxypropyl-β-cyclodextrin is the active component in a triple combination formulation for treatment of Niemann-Pick C1 disease.

Bruce J. Melancon, O. Wiest, F. Maxfield, 2019, Biochimica et biophysica acta. Molecular and cell biology of lipids.

Structural insights into HDAC6 tubulin deacetylation and its selective inhibition.

M. Saito, P. Helquist, P. Matthias, 2016, Nature chemical biology.

Progress toward the total synthesis of lucentamycin A: total synthesis and biological evaluation of 8-epi-lucentamycin A.

L. Marnett, C. Lindsley, R. Daniels, 2009, The Journal of organic chemistry.

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.

N. Brandon, C. Lindsley, P. Conn, 2017, ACS medicinal chemistry letters.

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

Stephen M. Damon, A. Deutch, J. Wess, 2014, Neuropsychopharmacology.

Structural basis of allosteric modulation of metabotropic glutamate receptor activation and desensitization

J. Meyerson, M. Filizola, Dagan C. Marx, 2023, bioRxiv.

VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.

Alison R. Gregro, Andrew S. Felts, N. Brandon, 2019, Bioorganic & medicinal chemistry letters.

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.

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

D. Sheffler, C. Lindsley, Margrith E. Mattmann, 2013, Bioorganic & medicinal chemistry letters.