Search Results - "Gallop, Mark A"

Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction by Simonetta, Kyle R., Taygerly, Joshua, Boyle, Kathleen, Basham, Stephen E., Padovani, Chris, Lou, Yan, Cummins, Thomas J., Yung, Stephanie L., von Soly, Szerenke Kiss, Kayser, Frank, Kuriyan, John, Rape, Michael, Cardozo, Mario, Gallop, Mark A., Bence, Neil F., Barsanti, Paul A., Saha, Anjanabha

“…Protein–protein interactions (PPIs) governing the recognition of substrates by E3 ubiquitin ligases are critical to cellular function. There is significant…”
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Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen by Lal, Ritu, Sukbuntherng, Juthamas, Tai, Ezra H L, Upadhyay, Shubhra, Yao, Fenmei, Warren, Mark S, Luo, Wendy, Bu, Lin, Nguyen, Son, Zamora, Jeanelle, Peng, Ge, Dias, Tracy, Bao, Ying, Ludwikow, Maria, Phan, Thu, Scheuerman, Randall A, Yan, Hui, Gao, Mark, Wu, Quincey Q, Annamalai, Thamil, Raillard, Stephen P, Koller, Kerry, Gallop, Mark A, Cundy, Kenneth C

“…Baclofen is a racemic GABA(B) receptor agonist that has a number of significant pharmacokinetic limitations, including a narrow window of absorption in the…”
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XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys by Cundy, Kenneth C, Annamalai, Thamil, Bu, Lin, De Vera, Josephine, Estrela, Jenny, Luo, Wendy, Shirsat, Payal, Torneros, Allan, Yao, Fenmei, Zou, Joan, Barrett, Ronald W, Gallop, Mark A

“…The absorption of gabapentin (Neurontin) is dose-dependent and variable between patients. Rapid clearance of the drug necessitates dosing three or more times…”
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XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters by Cundy, Kenneth C, Branch, Russell, Chernov-Rogan, Tania, Dias, Tracy, Estrada, Toño, Hold, Karin, Koller, Kerry, Liu, Xiaoli, Mann, Adam, Panuwat, Matt, Raillard, Stephen P, Upadhyay, Shubhra, Wu, Quincey Q, Xiang, Jia-Ning, Yan, Hui, Zerangue, Noa, Zhou, Cindy X, Barrett, Ronald W, Gallop, Mark A

“…Gabapentin is thought to be absorbed from the intestine of humans and animals by a low-capacity solute transporter localized in the upper small intestine…”
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Orally Absorbed Derivatives of the β‑Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs by Gordon, Eric M, Duncton, Matthew A. J, Gallop, Mark A

“…Only one FDA-approved β-lactamase inhibitor has ever been orally available: clavulanic acid, approved in 1984. Avibactam, approved by FDA in 2015, is the first…”
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Applications of Combinatorial Technologies to Drug Discovery. 2. Combinatorial Organic Synthesis, Library Screening Strategies, and Future Directions by Gordon, Eric M, Barrett, Ronald W, Dower, William J, Fodor, Stephen P. A, Gallop, Mark A

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Applications of Combinatorial Technologies to Drug Discovery. 1. Background and Peptide Combinatorial Libraries by Gallop, Mark A, Barrett, Ronald W, Dower, William J, Fodor, Stephen P. A, Gordon, Eric M

“…Recent trends in the search for novel pharmacological agents have focused on the preparation of "chemical libraries" as potential sources of new leads for drug…”
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Acamprosate Produces Its Anti-Relapse Effects Via Calcium by SPANAGEL, Rainer, VENGELIENE, Valentina, JANDELEIT, Bernd, FISCHER, Wolf-Nicolas, GRINDSTAFF, Kent, XUEXIANG ZHANG, GALLOP, Mark A, KRSTEW, Elena V, LAWRENCE, Andrew J, KIEFER, Falk

“…Alcoholism is one of the most prevalent neuropsychiatric diseases, having an enormous health and socioeconomic impact. Along with a few other medications,…”
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Combinatorial Organic Synthesis of Highly Functionalized Pyrrolidines: Identification of a Potent Angiotensin Converting Enzyme Inhibitor from a Mercaptoacyl Proline Library by Murphy, Martin M, Schullek, John R, Gordon, Eric M, Gallop, Mark A

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Solid-Phase Synthesis of 3,5-Disubstituted 2,3-Dihydro-1,5-benzothiazepin-4(5H)-ones by Schwarz, Matthias K, Tumelty, David, Gallop, Mark A

“…A solid-phase route affording novel 3,5-disubstituted 1,5-benzothiazepin-4(5H)-ones in optically pure form has been enabled. SNAr reaction of polymer-bound…”
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Stereoselective Solid-Phase Synthesis of a Triaza Tricyclic Ring System:  A New Chemotype for Lead Discovery by Peng, Ge, Sohn, Amy, Gallop, Mark A

“…Sequential pyrrolidine and hydantoin ring-forming reactions have been applied in the stereoselective solid-phase synthesis of a conformationally constrained,…”
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Discovery of a novel potent GABA(B) receptor agonist by Xu, Feng, Peng, Ge, Phan, Thu, Dilip, Usha, Chen, Jian Lu, Chernov-Rogan, Tania, Zhang, Xuexiang, Grindstaff, Kent, Annamalai, Thamil, Koller, Kerry, Gallop, Mark A, Wustrow, David J

“…Structure-activity studies have led to a discovery of 3-(4-pyridyl)methyl ether derivative 9d that has 25- to 50-fold greater functional potency than…”
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Strategies for the Synthesis and Screening of Glycoconjugates. 1. A Library of Glycosylamines by Vetter, Dirk, Gallop, Mark A

“…A simple one-step procedure is found to be highly effective for the "functionalization" of glycodiversity. This study encompasses 50 unprotected mono- and…”
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Discovery of a novel potent GABAB receptor agonist by Xu, Feng, Peng, Ge, Phan, Thu, Dilip, Usha, Chen, Jian Lu, Chernov-Rogan, Tania, Zhang, Xuexiang, Grindstaff, Kent, Annamalai, Thamil, Koller, Kerry, Gallop, Mark A, Wustrow, David J

“…Structure–activity studies have led to a discovery of 3-(4-pyridyl)methyl ether derivative 9d that has 25- to 50-fold greater functional potency than…”
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New methods for analyzing compounds on polymeric supports by Gallop, Mark A, Fitch, William L

“…Beyond specialized applications in peptide and oligonucleotide synthesis, widespread utilization of solid-phase methods in organic chemistry has been hampered…”
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Solid-Supported Combinatorial Synthesis of Structurally Diverse β-Lactams by Ruhland, Beatrice, Bhandari, Ashok, Gordon, Eric M, Gallop, Mark A

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Solid-Phase Synthesis of 4-Arylazetidin-2-ones via Suzuki and Heck Cross-Coupling Reactions by Ruhland, Beatrice, Bombrun, Agnes, Gallop, Mark A

“…Application of the Suzuki and the Heck cross-coupling reactions for efficient synthesis of diverse biaryl- and styryl-substituted β-lactams on solid support…”
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Validation of tele-otology to diagnose ear disease in children by Eikelboom, Robert H., Mbao, Mathew N., Coates, Harvey L., Atlas, Marcus D., Gallop, Mark A.

“…To determine if digitised still eardrum images, with a clinical history, and audiometry and tympanometry data provide sufficient information to an ear…”
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Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters by Bhat, Laxminarayan, Jandeleit, Bernd, Dias, Tracy M., Moors, Tristen L., Gallop, Mark A.

“…A series of novel C2–C3 annulated steroidal pyrazoles was synthesized as substrates for bile acid transporters. The pyrazoles were conjugated with drugs and…”
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A face-capping bonding mode for benzene in triosmium carbonyl cluster complexes by Gallop, Mark A, Gomez-Sal, M. Pilar, Housecroft, Catherine E, Johnson, Brian F. G, Lewis, Jack, Owen, Steven M, Raithby, Paul R, Wright, Anthony H

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