Search Results - "Hedrick, Michael P."

A Simple, High-Resolution Method for Establishing DNA Binding Affinity and Sequence Selectivity by Boger, Dale L, Fink, Brian E, Brunette, Steven R, Tse, Winston C, Hedrick, Michael P

“…Full details of the development of a simple, nondestructive, and high-throughput method for establishing DNA binding affinity and sequence selectivity are…”
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Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase by Stanford, Stephanie M, Aleshin, Alexander E, Zhang, Vida, Ardecky, Robert J, Hedrick, Michael P, Zou, Jiwen, Ganji, Santhi R, Bliss, Matthew R, Yamamoto, Fusayo, Bobkov, Andrey A, Kiselar, Janna, Liu, Yingge, Cadwell, Gregory W, Khare, Shilpi, Yu, Jinghua, Barquilla, Antonio, Chung, Thomas D Y, Mustelin, Tomas, Schenk, Simon, Bankston, Laurie A, Liddington, Robert C, Pinkerton, Anthony B, Bottini, Nunzio

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Development and use of a high-throughput screen to identify novel modulators of the corticotropin releasing factor binding protein by Haass-Koffler, Carolina L., Francis, T. Chase, Gandhi, Pauravi, Patel, Reesha, Naemuddin, Mohammad, Nielsen, Carsten K., Bartlett, Selena E., Bonci, Antonello, Vasile, Stefan, Hood, Becky L., Suyama, Eigo, Hedrick, Michael P., Smith, Layton H., Limpert, Allison S., Roberto, Marisa, Cosford, Nicholas D.P., Sheffler, Douglas J.

“…Stress responses are believed to involve corticotropin releasing factor (CRF), its two cognate receptors (CRF1 and CRF2), and the CRF-binding protein (CRFBP)…”
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Exceptionally Potent Inhibitors of Fatty Acid Amide Hydrolase: The Enzyme Responsible for Degradation of Endogenous Oleamide and Anandamide by Boger, Dale L., Sato, Haruhiko, Lerner, Aaron E., Hedrick, Michael P., Fecik, Robert A., Miyauchi, Hiroshi, Wilkie, Gordon D., Austin, Bryce J., Patricelli, Matthew P., Cravatt, Benjamin F.

“…The development of exceptionally potent inhibitors of fatty acid amide hydrolase (FAAH), the enzyme responsible for the degradation of oleamide (an endogenous…”
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β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors by Slosky, Lauren M., Bai, Yushi, Toth, Krisztian, Ray, Caroline, Rochelle, Lauren K., Badea, Alexandra, Chandrasekhar, Rahul, Pogorelov, Vladimir M., Abraham, Dennis M., Atluri, Namratha, Peddibhotla, Satyamaheshwar, Hedrick, Michael P., Hershberger, Paul, Maloney, Patrick, Yuan, Hong, Li, Zibo, Wetsel, William C., Pinkerton, Anthony B., Barak, Lawrence S., Caron, Marc G.

“…Small molecule neurotensin receptor 1 (NTSR1) agonists have been pursued for more than 40 years as potential therapeutics for psychiatric disorders, including…”
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Total Synthesis of Ningalin B Utilizing a Heterocyclic Azadiene Diels−Alder Reaction and Discovery of a New Class of Potent Multidrug Resistant (MDR) Reversal Agents by Boger, Dale L, Soenen, Danielle R, Boyce, Christopher W, Hedrick, Michael P, Jin, Qing

“…A concise, efficient approach to the total synthesis of ningalin B (1) based on a heterocyclic azadiene Diels−Alder strategy (1,2,4,5-tetrazine → 1,2-diazine →…”
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An Optimized Dihydrodibenzothiazepine Lead Compound (SBI-0797750) as a Potent and Selective Inhibitor of Plasmodium falciparum and P. vivax Glucose 6-Phosphate Dehydrogenase 6-Phosphogluconolactonase by Berneburg, Isabell, Peddibhotla, Satyamaheshwar, Heimsch, Kim C, Haeussler, Kristina, Maloney, Patrick, Gosalia, Palak, Preuss, Janina, Rahbari, Mahsa, Skorokhod, Oleksii, Valente, Elena, Ulliers, Daniela, Simula, Luigi Felice, Buchholz, Kathrin, Hedrick, Michael P, Hershberger, Paul, Chung, Thomas D Y, Jackson, Michael R, Schwarzer, Evelin, Rahlfs, Stefan, Bode, Lars, Becker, Katja, Pinkerton, Anthony B

“…In , the first two and rate-limiting enzymes of the pentose phosphate pathway, glucose 6-phosphate dehydrogenase (G6PD) and the 6-phosphogluconolactonase, are…”
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Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase by Stanford, Stephanie M, Diaz, Michael A, Ardecky, Robert J, Zou, Jiwen, Roosild, Tarmo, Holmes, Zachary J, Nguyen, Tiffany P, Hedrick, Michael P, Rodiles, Socorro, Guan, April, Grotegut, Stefan, Santelli, Eugenio, Chung, Thomas D. Y, Jackson, Michael R, Bottini, Nunzio, Pinkerton, Anthony B

“…Obesity-associated insulin resistance plays a central role in the pathogenesis of type 2 diabetes. A promising approach to decrease insulin resistance in…”
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Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase by Stanford, Stephanie M, Aleshin, Alexander E, Zhang, Vida, Ardecky, Robert J, Hedrick, Michael P, Zou, Jiwen, Ganji, Santhi R, Bliss, Matthew R, Yamamoto, Fusayo, Bobkov, Andrey A, Kiselar, Janna, Liu, Yingge, Cadwell, Gregory W, Khare, Shilpi, Yu, Jinghua, Barquilla, Antonio, Chung, Thomas D Y, Mustelin, Tomas, Schenk, Simon, Bankston, Laurie A, Liddington, Robert C, Pinkerton, Anthony B, Bottini, Nunzio

“…The generation of low-molecular-weight protein tyrosine phosphatase (LMPTP) knockout mice combined with the identification of a small-molecule uncompetitive…”
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Discovery of β‑Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators by Pinkerton, Anthony B, Peddibhotla, Satyamaheshwar, Yamamoto, Fusayo, Slosky, Lauren M, Bai, Yushi, Maloney, Patrick, Hershberger, Paul, Hedrick, Michael P, Falter, Bekhi, Ardecky, Robert J, Smith, Layton H, Chung, Thomas D. Y, Jackson, Michael R, Caron, Marc G, Barak, Lawrence S

“…Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator…”
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Evidence That the DNA Endonuclease ARTEMIS also Has Intrinsic 5′-Exonuclease Activity by Li, Sicong, Chang, Howard H., Niewolik, Doris, Hedrick, Michael P., Pinkerton, Anthony B., Hassig, Christian A., Schwarz, Klaus, Lieber, Michael R.

“…ARTEMIS is a member of the metallo-β-lactamase protein family. ARTEMIS has endonuclease activity at DNA hairpins and at 5′- and 3′-DNA overhangs of duplex DNA,…”
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Discovery, Synthesis, and Optimization of Diarylisoxazole-3-carboxamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore by Roy, Sudeshna, Šileikytė, Justina, Schiavone, Marco, Neuenswander, Benjamin, Argenton, Francesco, Aubé, Jeffrey, Hedrick, Michael P., Chung, Thomas D. Y., Forte, Michael A., Bernardi, Paolo, Schoenen, Frank J.

“…The mitochondrial permeability transition pore (mtPTP) is a Ca2+‐requiring mega‐channel which, under pathological conditions, leads to the deregulated release…”
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N-Phenylbenzamides as Potent Inhibitors of the Mitochondrial Permeability Transition Pore by Roy, Sudeshna, Šileikytė, Justina, Neuenswander, Benjamin, Hedrick, Michael P., Chung, Thomas D. Y., Aubé, Jeffrey, Schoenen, Frank J., Forte, Michael A., Bernardi, Paolo

“…Persistent opening of the mitochondrial permeability transition pore (PTP), an inner membrane channel, leads to mitochondrial dysfunction and renders the PTP a…”
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Discovery of a Potent, Selective, and Efficacious Class of Reversible α-Ketoheterocycle Inhibitors of Fatty Acid Amide Hydrolase Effective as Analgesics by Boger, Dale L, Miyauchi, Hiroshi, Du, Wu, Hardouin, Christophe, Fecik, Robert A, Cheng, Heng, Hwang, Inkyu, Hedrick, Michael P, Leung, Donmienne, Acevedo, Orlando, Guimarães, Cristiano R. W, Jorgensen, William L, Cravatt, Benjamin F

“…Fatty acid amide hydrolase (FAAH) degrades neuromodulating fatty acid amides including anandamide (endogenous cannabinoid agonist) and oleamide (sleep-inducing…”
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Discovery of a Plasmodium falciparum Glucose-6-phosphate Dehydrogenase 6‑phosphogluconolactonase Inhibitor (R,Z)‑N‑((1-Ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro‑2H‑benzo[b][1,4]thiazine-6-carboxamide (ML276) That Reduces Parasite Growth in Vitro by Preuss, Janina, Maloney, Patrick, Peddibhotla, Satyamaheshwar, Hedrick, Michael P, Hershberger, Paul, Gosalia, Palak, Milewski, Monika, Li, Yujie Linda, Sugarman, Eliot, Hood, Becky, Suyama, Eigo, Nguyen, Kevin, Vasile, Stefan, Sergienko, Eduard, Mangravita-Novo, Arianna, Vicchiarelli, Michael, McAnally, Danielle, Smith, Layton H, Roth, Gregory P, Diwan, Jena, Chung, Thomas D.Y, Jortzik, Esther, Rahlfs, Stefan, Becker, Katja, Pinkerton, Anthony B, Bode, Lars

“…A high-throughput screen of the NIH’s MLSMR collection of ∼340000 compounds was undertaken to identify compounds that inhibit Plasmodium falciparum…”
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Connecting proteins with drug-like compounds: Open source drug discovery workflows with BindingDB and KNIME by Nicola, George, Berthold, Michael R, Hedrick, Michael P, Gilson, Michael K

“…Today's large, public databases of protein-small molecule interaction data are creating important new opportunities for data mining and integration. At the…”
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Imidazole-derived agonists for the neurotensin 1 receptor by Hershberger, Paul M, Hedrick, Michael P, Peddibhotla, Satyamaheshwar, Mangravita-Novo, Arianna, Gosalia, Palak, Li, Yujie, Gray, Wilson, Vicchiarelli, Michael, Smith, Layton H, Chung, Thomas D Y, Thomas, James B, Caron, Marc G, Pinkerton, Anthony B, Barak, Lawrence S, Roth, Gregory P

“…A scaffold-hop program seeking full agonists of the neurotensin-1 (NTR1) receptor identified the probe molecule ML301 (1) and associated analogs, including its…”
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Total Synthesis of Distamycin A and 2640 Analogues:  A Solution-Phase Combinatorial Approach to the Discovery of New, Bioactive DNA Binding Agents and Development of a Rapid, High-Throughput Screen for Determining Relative DNA Binding Affinity or DNA Binding Sequence Selectivity by Boger, Dale L, Fink, Brian E, Hedrick, Michael P

“…The development of a solution-phase synthesis of distamycin A and its extension to the preparation of 2640 analogues are described. Thus, solution-phase…”
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Discovery of ML314, a Brain Penetrant Nonpeptidic β‑Arrestin Biased Agonist of the Neurotensin NTR1 Receptor by Peddibhotla, Satyamaheshwar, Hedrick, Michael P, Hershberger, Paul, Maloney, Patrick R, Li, Yujie, Milewski, Monika, Gosalia, Palak, Gray, Wilson, Mehta, Alka, Sugarman, Eliot, Hood, Becky, Suyama, Eigo, Nguyen, Kevin, Heynen-Genel, Susanne, Vasile, Stefan, Salaniwal, Sumeet, Stonich, Derek, Su, Ying, Mangravita-Novo, Arianna, Vicchiarelli, Michael, Roth, Gregory P, Smith, Layton H, Chung, Thomas D. Y, Hanson, Glen R, Thomas, James B, Caron, Marc G, Barak, Lawrence S, Pinkerton, Anthony B

“…The neurotensin 1 receptor (NTR1) is an important therapeutic target for a range of disease states including addiction. A high-throughput screening campaign,…”
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Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy by Frankowski, Kevin J, Hedrick, Michael P, Gosalia, Palak, Li, Kelin, Shi, Shenghua, Whipple, David, Ghosh, Partha, Prisinzano, Thomas E, Schoenen, Frank J, Su, Ying, Vasile, S, Sergienko, Eduard, Gray, Wilson, Hariharan, Santosh, Milan, Loribelle, Heynen-Genel, Susanne, Mangravita-Novo, Arianna, Vicchiarelli, Michael, Smith, Layton H, Streicher, John M, Caron, Marc G, Barak, Lawrence S, Bohn, Laura M, Chung, Thomas D. Y, Aubé, Jeffrey

“…Herein we present the outcome of a high throughput screening (HTS) campaign-based strategy for the rapid identification and optimization of selective and…”
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