Search Results - "ENGERS, Darren W"

Synthesis and structure–activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of Dorsomorphin: The discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe by Engers, Darren W., Frist, Audrey Y., Lindsley, Craig W., Hong, Charles C., Hopkins, Corey R.

“…A structure–activity relationship of the 3- and 6-positions of the pyrazolo[1,5-a]pyrimidine scaffold of the known BMP inhibitors dorsomorphin, 1, LDN-193189,…”
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Discovery, Structure–Activity Relationship, and Biological Characterization of a Novel Series of 6‑((1H‑Pyrazolo[4,3‑b]pyridin-3-yl)amino)-benzo[d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4) by Bollinger, Sean R, Engers, Darren W, Panarese, Joseph D, West, Mary, Engers, Julie L, Loch, Matthew T, Rodriguez, Alice L, Blobaum, Anna L, Jones, Carrie K, Thompson Gray, Analisa, Conn, P. Jeffrey, Lindsley, Craig W, Niswender, Colleen M, Hopkins, Corey R

“…This work describes the discovery and characterization of novel 6-(1H-pyrazolo­[4,3-b]­pyridin-3-yl)­amino-benzo­[d]­isothiazole-3-carboxamides as mGlu4 PAMs…”
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Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels by Raphemot, Rene, Rouhier, Matthew F, Swale, Daniel R, Days, Emily, Weaver, C David, Lovell, Kimberly M, Konkel, Leah C, Engers, Darren W, Bollinger, Sean R, Bollinger, Sean F, Hopkins, Corey, Piermarini, Peter M, Denton, Jerod S

“…Vector-borne diseases such as dengue fever and malaria, which are transmitted by infected female mosquitoes, affect nearly half of the world's population. The…”
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Challenges in the development of an M 4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs by Wood, Michael R, Noetzel, Meredith J, Poslusney, Michael S, Melancon, Bruce J, Tarr, James C, Lamsal, Atin, Chang, Sichen, Luscombe, Vincent B, Weiner, Rebecca L, Cho, Hyekyung P, Bubser, Michael, Jones, Carrie K, Niswender, Colleen M, Wood, Michael W, Engers, Darren W, Brandon, Nicholas J, Duggan, Mark E, Conn, P Jeffrey, Bridges, Thomas M, Lindsley, Craig W

“…This letter describes the chemical optimization of a novel series of M positive allosteric modulators (PAMs) based on a 5-amino-thieno[2,3-c]pyridazine core,…”
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Allosteric modulation of Class C GPCRs: a novel approach for the treatment of CNS disorders by Engers, Darren W., Lindsley, Craig W.

“…Allosteric modulation has emerged as an innovative pharmacological approach to selectively activate or inhibit several Class C GPCRs. Of the Class C GPCRs,…”
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Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia by Wood, Michael R., Noetzel, Meredith J., Melancon, Bruce J., Poslusney, Michael S., Nance, Kellie D., Hurtado, Miguel A., Luscombe, Vincent B., Weiner, Rebecca L., Rodriguez, Alice L., Lamsal, Atin, Chang, Sichen, Bubser, Michael, Blobaum, Anna L., Engers, Darren W., Niswender, Colleen M., Jones, Carrie K., Brandon, Nicholas J., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.

“…Herein, we report the structure–activity relationships within a series of potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4)…”
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Discovery of “Molecular Switches” within a Series of mGlu5 Allosteric Ligands Driven by a “Magic Methyl” Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype by Barbaro, Lisa, Rodriguez, Alice L, Blevins, Ashlyn N, Dickerson, Jonathan W, Billard, Natasha, Boutaud, Olivier, Rook, Jerri L, Niswender, Colleen M, Conn, P.Jeffrey, Engers, Darren W, Lindsley, Craig W

“…In the course of optimizing an M1 PAM chemotype, introduction of an ether moiety unexpectedly abolished M1 PAM activity while engendering a “molecular switch”…”
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Synthesis, SAR and Unanticipated Pharmacological Profiles of Analogues of the mGluR5 Ago‐potentiator ADX‐47273 by Engers, Darren W., Rodriguez, Alice L., Williams, Richard, Hammond, Alexis S., Venable, Daryl, Oluwatola, Oluwatomi, Sulikowski, Gary A., Conn, P. Jeffrey, Lindsley, Craig W.

“…An iterative analogue library synthesis strategy rapidly developed comprehensive SAR for the mGluR5 ago‐potentiator ADX‐47273. This effort identified key…”
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M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition by Moran, Sean P., Dickerson, Jonathan W., Cho, Hyekyung P., Xiang, Zixiu, Maksymetz, James, Remke, Daniel H., Lv, Xiaohui, Doyle, Catherine A., Rajan, Deepa H., Niswender, Colleen M., Engers, Darren W., Lindsley, Craig W., Rook, Jerri M., Conn, P. Jeffrey

“…Highly selective positive allosteric modulators (PAMs) of the M1 subtype of muscarinic acetylcholine receptor have emerged as an exciting new approach for…”
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M 1 -positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition by Moran, Sean P, Dickerson, Jonathan W, Cho, Hyekyung P, Xiang, Zixiu, Maksymetz, James, Remke, Daniel H, Lv, Xiaohui, Doyle, Catherine A, Rajan, Deepa H, Niswender, Colleen M, Engers, Darren W, Lindsley, Craig W, Rook, Jerri M, Conn, P Jeffrey

“…Highly selective positive allosteric modulators (PAMs) of the M subtype of muscarinic acetylcholine receptor have emerged as an exciting new approach for…”
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Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator by Mattmann, Margrith E., Yu, Haibo, Lin, Zhihong, Xu, Kaiping, Huang, Xiaofang, Long, Shunyou, Wu, Meng, McManus, Owen B., Engers, Darren W., Le, Uyen M., Li, Min, Lindsley, Craig W., Hopkins, Corey R.

“…A high-throughput screen utilizing a depolarization-triggered thallium influx through KCNQ1 channels was developed and used to screen the MLSMR collection of…”
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M1 Muscarinic Receptors Modulate Fear-Related Inputs to the Prefrontal Cortex: Implications for Novel Treatments of Posttraumatic Stress Disorder by Maksymetz, James, Joffe, Max E., Moran, Sean P., Stansley, Branden J., Li, Brianna, Temple, Kayla, Engers, Darren W., Lawrence, J. Josh, Lindsley, Craig W., Conn, P. Jeffrey

“…The prefrontal cortex (PFC) integrates information from multiple inputs to exert top-down control allowing for appropriate responses in a given context. In…”
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M 1 Muscarinic Receptors Modulate Fear-Related Inputs to the Prefrontal Cortex: Implications for Novel Treatments of Posttraumatic Stress Disorder by Maksymetz, James, Joffe, Max E, Moran, Sean P, Stansley, Branden J, Li, Brianna, Temple, Kayla, Engers, Darren W, Lawrence, J Josh, Lindsley, Craig W, Conn, P Jeffrey

“…The prefrontal cortex (PFC) integrates information from multiple inputs to exert top-down control allowing for appropriate responses in a given context. In…”
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An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria by Swale, Daniel R., Engers, Darren W., Bollinger, Sean R., Gross, Aaron, Inocente, Edna Alfaro, Days, Emily, Kanga, Fariba, Johnson, Reed M., Yang, Liu, Bloomquist, Jeffrey R., Hopkins, Corey R., Piermarini, Peter M., Denton, Jerod S.

“…Insecticide resistance is a growing threat to mosquito control programs around the world, thus creating the need to discover novel target sites and…”
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Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu 7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962) by Reed, Carson W, Yohn, Samantha E, Washecheck, Jordan P, Roenfanz, Hanna F, Quitalig, Marc C, Luscombe, Vincent B, Jenkins, Matthew T, Rodriguez, Alice L, Engers, Darren W, Blobaum, Anna L, Conn, P Jeffrey, Niswender, Colleen M, Lindsley, Craig W

“…Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu ) negative allosteric modulator (NAM)…”
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Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1 by Spearing, Paul K., Cho, Hyekyung P., Luscombe, Vincent B., Blobaum, Anna L., Boutaud, Olivier, Engers, Darren W., Rodriguez, Alice L., Niswender, Colleen M., Jeffrey Conn, P., Lindsley, Craig W., Bender, Aaron M.

“…[Display omitted] This Letter describes the synthesis and optimization of a series of heteroaryl-pyrrolidinone positive allosteric modulators (PAMs) of the…”
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Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063 by Kharade, Sujay V, Sanchez-Andres, Juan Vicente, Fulton, Mark G, Shelton, Elaine L, Blobaum, Anna L, Engers, Darren W, Hofmann, Christopher S, Dadi, Prasanna K, Lantier, Louise, Jacobson, David A, Lindsley, Craig W, Denton, Jerod S

“…Glucose-stimulated insulin secretion from pancreatic -cells is controlled by ATP-regulated potassium (K ) channels composed of Kir6.2 and sulfonylurea receptor…”
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Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 by Spearing, Paul K, Cho, Hyekyung P, Luscombe, Vincent B, Blobaum, Anna L, Boutaud, Olivier, Engers, Darren W, Rodriguez, Alice L, Niswender, Colleen M, Jeffrey Conn, P, Lindsley, Craig W, Bender, Aaron M

“…This Letter describes the synthesis and optimization of a series of heteroaryl-pyrrolidinone positive allosteric modulators (PAMs) of the muscarinic…”
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Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors by Engers, Darren W., Bollinger, Sean R., Felts, Andrew S., Vadukoot, Anish K., Williams, Charles H., Blobaum, Anna L., Lindsley, Craig W., Hong, Charles C., Hopkins, Corey R.

“…[Display omitted] The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2,…”
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Surveying heterocycles as amide bioisosteres within a series of mGlu 7 NAMs: Discovery of VU6019278 by Reed, Carson W, Washecheck, Jordan P, Quitlag, Marc C, Jenkins, Matthew T, Rodriguez, Alice L, Engers, Darren W, Blobaum, Anna L, Jeffrey Conn, P, Niswender, Colleen M, Lindsley, Craig W

“…This letter describes a diversity-oriented library approach to rapidly assess diverse heterocycles as bioisosteric replacements for a metabolically labile…”
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