Search Results - "WENTLAND, MARK"

Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities by Porter, Donald C, Farmaki, Elena, Altilia, Serena, Schools, Gary P, West, Deborah K, Chen, Mengqian, Chang, Bey-Dih, Puzyrev, Anatoliy T, Lim, Chang-uk, Rokow-Kittell, Rebecca, Friedhoff, Lawrence T, Papavassiliou, Athanasios G, Kalurupalle, Swathi, Hurteau, Gregory, Shi, Jun, Baran, Phil S, Gyorffy, Balazs, Wentland, Mark P, Broude, Eugenia V, Kiaris, Hippokratis, Roninson, Igor B

“…Conventional chemotherapy not only kills tumor cells but also changes gene expression in treatment-damaged tissues, inducing production of multiple…”
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Syntheses of novel high affinity ligands for opioid receptors by Wentland, Mark P., Lou, Rongliang, Lu, Qun, Bu, Yigong, Denhardt, Christoph, Jin, Jin, Ganorkar, Rakesh, VanAlstine, Melissa A., Guo, Chengyun, Cohen, Dana J., Bidlack, Jean M.

“…High binding affinity [ K i values (μ) = 0.072–1.3 nM] to opioid receptors is seen in a novel series of 3-desoxy-3-carboxamido-4-hydroxymorphinans where the…”
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Antinociceptive activity of CC44, a biotinylated improgan congener by Hoerbelt, Paul, Nalwalk, Julia W., Phillips, James G., Wentland, Mark P., Shan, Zhixing, Hough, Lindsay B.

“…Improgan, a non-opioid, antinociceptive drug, activates descending analgesic circuits following brain administration, but the improgan receptor remains…”
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Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling by Ding, Xinxin, Hough, Lindsay B, Conroy, Jennie L, Fang, Cheng, Gu, Jun, Zeitlin, Scott O, Yang, Weizhu, Yang, Jun, VanAlstine, Melissa A, Nalwalk, Julia W, Albrecht, Phillip J, Mazurkiewicz, Joseph E, Snyder-Keller, Abigail, Shan, Zhixing, Zhang, Shao-Zhong, Wentland, Mark P, Behr, Melissa, Knapp, Brian I, Bidlack, Jean M, Zuiderveld, Obbe P, Leurs, Rob

“…To assess the importance of brain cytochrome P450 (P450) activity in μ opioid analgesic action, we generated a mutant mouse with brain neuron-specific…”
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Syntheses and opioid receptor binding properties of carboxamido-substituted opioids by Wentland, Mark P., Lou, Rongliang, Lu, Qun, Bu, Yigong, VanAlstine, Melissa A., Cohen, Dana J., Bidlack, Jean M.

“…A series of 15 novel opioid derivatives were made where the prototypic phenolic-OH group of traditional opioids was replaced by a carboxamido (CONH 2) group. A…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: Oxygenated N-(2-[1,1′-biphenyl]-4-ylethyl) analogues of 8-CAC by Wentland, Mark P., Jo, Sunjin, Gargano, Joseph M., VanAlstine, Melissa A., Cohen, Dana J., Bidlack, Jean M.

“…N-[2-(4′-methoxy[1,1′-biphenyl]-4-yl)ethyl]-8-CAC (1) is a high affinity (Ki=0.084nM) ligand for the μ opioid receptor and served as the lead compound for this…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors by VanAlstine, Melissa A., Wentland, Mark P., Alvarez, Juan, Cao, Qing, Cohen, Dana J., Knapp, Brian I., Bidlack, Jean M.

“…Derivatives of the lead compound N-BPE-8-CAC (1) where each CH of the biphenyl group was individually replaced by N were prepared in hopes of identifying high…”
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Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic by Hough, Lindsay B., Nalwalk, Julia W., Yang, Jun, Conroy, Jennie L., VanAlstine, Melissa A., Yang, Weizhu, Gargano, Joseph, Shan, Zhixing, Zhang, Shao-Zhong, Wentland, Mark P., Phillips, James G., Knapp, Brian I., Bidlack, Jean M., Zuiderveld, Obbe P., Leurs, Rob, Ding, Xinxin

“…The search for the mechanism of action of improgan (a nonopioid analgesic) led to the recent discovery of CC12, a compound that blocks improgan…”
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Redefining the Structure−Activity Relationships of 2,6-Methano-3-benzazocines. 4. Opioid Receptor Binding Properties of 8-[N-(4‘-phenyl)-phenethyl)carboxamido] Analogues of Cyclazocine and Ethylketocycalzocine by Wentland, Mark P, VanAlstine, Melissa, Kucejko, Robert, Lou, Rongliang, Cohen, Dana J, Parkhill, Amy L, Bidlack, Jean M

“…The synthesis and evaluation of a series of aryl-containing N-monosubstituted analogues of the lead compound 8-carboxamidocyclazocine were performed to probe a…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine by Wentland, Mark P., Sun, Xufeng, Cohen, Dana J., Bidlack, Jean M.

“…Novel 7,8- and 8,9-fused-heterocyclic variants of 8-carboxamidocyclazocine have high affinity for opioid receptors. A series of 7,8- and 8,9-fused…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4′-phenyl)-phenethyl) analogues of 8-CAC by VanAlstine, Melissa A., Wentland, Mark P., Cohen, Dana J., Bidlack, Jean M.

“…Novel analogues of 8-carboxamidocyclazocine have very high affinity for opioid receptors. A series of aryl-containing N-monosubstituted analogues of the lead…”
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10-Ketomorphinan and 3-Substituted-3-desoxymorphinan Analogues as Mixed κ and μ Opioid Ligands:  Synthesis and Biological Evaluation of Their Binding Affinity at Opioid Receptors by Zhang, Ao, Xiong, Wennan, Bidlack, Jean M, Hilbert, James E, Knapp, Brian I, Wentland, Mark P, Neumeyer, John L

“…A series of 10-ketomorphinan analogues were synthesized, and their binding affinity at all three opioid receptors was investigated. In most cases, high…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 7: Syntheses and opioid receptor properties of cyclic variants of cyclazocine by Wentland, Mark P., Lu, Qun, Ganorkar, Rakesh, Zhang, Shao-Zhong, Jo, Sunjin, Cohen, Dana J., Bidlack, Jean M.

“…Members of a novel series of 7,8- and 8,9-fused triazole and imidazole analogues of cyclazocine display very high affinity for opioid receptors. A series of…”
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Synthesis and opioid receptor binding properties of a highly potent 4-hydroxy analogue of naltrexone by Wentland, Mark P., Lu, Qun, Lou, Rongliang, Bu, Yigong, Knapp, Brian I., Bidlack, Jean M.

“…Novel analogue 5 of naltrexone displays very high affinity for opioid receptors with K i values of 0.052 nM, 2.6 nM and 0.23 nM for μ, δ and κ, respectively…”
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Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition by Yang, Jun, VanAlstine, Melissa A, Phillips, James G, Wentland, Mark P, Hough, Lindsay B

“…Cytochrome P450 (CYP)-mediated epoxidation of arachidonic acid (AA) contributes to important biological functions, including the pain-relieving responses…”
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Kappa-opioid receptor ligands inhibit cocaine-induced HIV-1 expression in microglial cells by Gekker, Genya, Hu, Shuxian, Wentland, Mark P, Bidlack, Jean M, Lokensgard, James R, Peterson, Phillip K

“…Cocaine abuse has been implicated as a cofactor in human immunodeficiency virus (HIV)-1-associated dementia (HAD). In this study, we tested the hypothesis that…”
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CC12, a high-affinity ligand for [3H]cimetidine binding, is an improgan antagonist by Hough, Lindsay B., Nalwalk, Julia W., Phillips, James G., Kern, Brian, Shan, Zhixing, Wentland, Mark P., de Esch, Iwan J.P., Janssen, Elwin, Barr, Travis, Stadel, Rebecca

“…Improgan, a chemical congener of cimetidine, is a highly effective non-opioid analgesic when injected into the CNS. Despite extensive characterization, neither…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 3: 8-Thiocarboxamido and 8-thioformamido derivatives of cyclazocine by Wentland, Mark P., Sun, Xufeng, Bu, Yigong, Lou, Rongliang, Cohen, Dana J., Bidlack, Jean M.

“…8-Thiocarboxamido and 8-thioformamido analogues of cyclazocine show high binding affinity for opioid receptors. 8-Position variants of cyclazocine have been…”
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96-Well Plate Colorimetric Assay for Ki Determination of (+/-)-2-Benzylsuccinic Acid, an Inhibitor of Carboxypeptidase A: A Laboratory Experiment in Drug Discovery by Wentland, Mark P, Raza, Shaan, Gao, Yingtong

“…A new 96-well microplate bioassay has been developed for students to learn and practice biotechnologies that researchers use to discover therapeutics. This…”
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8-Carboxamidocyclazocine: a long-acting, novel benzomorphan by Bidlack, Jean M, Cohen, Dana J, McLaughlin, Jay P, Lou, Rongliang, Ye, Yingchun, Wentland, Mark P

“…To obtain benzomorphans with a longer duration of action that may be potential therapeutics for treating cocaine abuse, 8-carboxamidocyclazocine was…”
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