Search Results - "WILLARD, DERRIL H"

Acyclic cyanamide-based inhibitors of cathepsin K by Barrett, David G., Deaton, David N., Hassell, Anne M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Payne, J. Alan, Shewchuk, Lisa M., Willard, Derril H., Wright, Lois L.

“…Conversion of the proline-derived cyanamide lead into an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large…”
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Melanocortin receptor-mediated mobilization of intracellular free calcium in HEK293 cells by MOUNTJOY, KATHLEEN G, KONG, PHILIP L, TAYLOR, JOHN A, WILLARD, DERRIL H, WILKISON, WILLIAM O

“…1 Research Centre for Developmental Medicine and Biology, Department of Paediatrics 2 School of Biological Sciences, University of Auckland, Auckland 1, New…”
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Design of Potent, Selective, and Orally Bioavailable Inhibitors of Cysteine Protease Cathepsin K by Tavares, Francis X, Boncek, Virginia, Deaton, David N, Hassell, Anne M, Long, Stacey T, Miller, Aaron B, Payne, Alan A, Miller, Larry R, Shewchuk, Lisa M, Wells-Knecht, Kevin, Willard, Derril H, Wright, Lois L, Zhou, Hui-Qiang

“…Osteoclast-mediated bone matrix resorption has been attributed to cathepsin K, a cysteine protease of the papain family that is abundantly and selectively…”
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Novel and potent cyclic cyanamide-based cathepsin K inhibitors by Deaton, David N., Hassell, Anne M., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Shewchuk, Lisa M., Tavares, Francis X., Willard, Derril H., Wright, Lois L.

“…Starting from a PDE IV inhibitor hit derived from high throughput screening of the compound collection, a key pyrrolidine cyanamide pharmacophore was…”
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Agouti structure and function: characterization of a potent .alpha.-melanocyte stimulating hormone receptor antagonist by Willard, Derril H, Bodnar, Wanda, Harris, Cole, Kiefer, Laura, Nichols, James S, Blanchard, Steven, Hoffman, Christine, Moyer, Mary, Burkhart, William

“…The murine agouti gene encodes for a novel 131 amino acid protein. The sequence includes a 22 residue putative secretion signal, an internal basic region, and…”
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Hydration Changes Implicated in the Remarkable Temperature-Dependent Membrane Permeation of Cyclosporin A by Augustijns, Patrick F, Brown, Stephen C, Willard, Derril H, Consler, Thomas G, Annaert, Pieter P, Hendren, R. Wayne, Bradshaw, Timothy P

“…Cyclosporin A is a cyclic peptide believed to exist as multiple conformers in aqueous solution. Two major conformations, distinguished by a single cis−trans…”
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Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors? by Adkison, Kim K., Barrett, David G., Deaton, David N., Gampe, Robert T., Hassell, Anne M., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Payne, J. Alan, Shewchuk, Lisa M., Wells-Knecht, Kevin J., Willard, Derril H., Wright, Lois L.

“…Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of…”
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Novel, potent P2–P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors by Barrett, David G., Catalano, John G., Deaton, David N., Hassell, Anne M., Long, Stacey T., Miller, Aaron B., Miller, Larry R., Ray, John A., Samano, Vicente, Shewchuk, Lisa M., Wells-Knecht, Kevin J., Willard, Derril H., Wright, Lois L.

“…Starting from a potent pantolactone ketoamide cathepsin K inhibitor derived from structural screening, conversion of the lactone scaffold to a pyrrolidine…”
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P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K by BARRETT, David G, BONCEK, Virginia M, PAYNE, J. Alan, RAY, John A, SAMANO, Vicente, SHEWCHUK, Lisa M, TAVARES, Francis X, WELLS-KNECHT, Kevin J, WILLARD, Derril H, WRIGHT, Lois L, ZHOU, Hui-Qiang Q, CATALANO, John G, DEATON, David N, HASSELL, Anne M, JURGENSEN, Cynthia H, LONG, Stacey T, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R

“…An orally bioavailable series of ketoamide-based cathepsin K inhibitors with good pharmacokinetic properties has been identified. Starting from a potent…”
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Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions by BARRETT, David G, CATALANO, John G, WRIGHT, Lois L, DEATON, David N, HASSELL, Anne M, LONG, Stacey T, MILLER, Aaron B, MILLER, Larry R, SHEWCHUK, Lisa M, WELLS-KNECHT, Kevin J, WILLARD, Derril H

“…A series of ketoamides were synthesized and evaluated for inhibitory activity against cathepsin K. Exploration of the interactions between achiral P(2)…”
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Exploration of the P1 SAR of aldehyde cathepsin K inhibitors by CATALANO, John G, DEATON, David N, FURFINE, Eric S, HASSELL, Annie M, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R, SHEWCHUK, Lisa M, WILLARD, Derril H, WRIGHT, Lois L

“…The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a…”
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Agouti Antagonism of Melanocortin-4 Receptor: Greater Effect with Desacetyl-α-Melanocyte-Stimulating Hormone (MSH) than withα -MSH by Mountjoy, Kathleen G, Willard, Derril H, Wilkison, William O

“…Desacetyl-α-MSH is more abundant than α-MSH in the brain, the fetus, human blood, and amniotic fluid, but there is little information on its ability to…”
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Solution Studies of Recombinant Human Stromal-Cell-Derived Factor-1 by Holmes, William D., Consler, Thomas G., Dallas, Walter S., Rocque, Warren J., Willard, Derril H.

“…Stromal-cell-derived factor-1 (SDF-1α) is an 8-kDa chemokine that is constitutively expressed in bone-marrow-derived stromal cells and has been identified as a…”
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Human Recombinant Phosphodiesterase 4B2B Binds (R)-Rolipram at a Single Site with Two Affinities by Rocque, Warren J, Tian, Gaochao, Wiseman, Jeffrey S, Holmes, William D, Zajac-Thompson, Irene, Willard, Derril H, Patel, Indravaden R, Wisely, G. Bruce, Clay, William C, Kadwell, Sue H, Hoffman, Christine R, Luther, Michael A

“…The interactions between (R)-rolipram and purified human recombinant low-K m, cAMP-specific phosphodiesterase (HSPDE4B2B) constructs were investigated using…”
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Mutations in the Carboxyl Terminus of the Agouti Protein Decrease Agouti Inhibition of Ligand Binding to the Melanocortin Receptors by Kiefer, Laura L, Ittoop, Olivia R. R, Bunce, Keith, Truesdale, Anne T, Willard, Derril H, Nichols, James S, Blanchard, Steven G, Mountjoy, Kathleen, Chen, Wen-Ji, Wilkison, William O

“…Several mutations that cause ectopic expression of the agouti gene result in obesity, hyperinsulinemia, and yellow coat color. A candidate pathway for agouti…”
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Detailed Characterization of a Purified Type 4 Phosphodiesterase, HSPDE4B2B: Differentiation of High- and Low-Affinity (R)-Rolipram Binding by Rocque, Warren J., Holmes, William D., Patel, Indravadan R., Dougherty, Robert W., Ittoop, Olivia, Overton, Laurie, Hoffman, Christine R., Wisely, G.Bruce, Willard, Derril H., Luther, Michael A.

“…We have overexpressed in a baculovirus expression system, and purified to >95% homogeneity, milligram quantities of a human recombinant rolipram-sensitive cAMP…”
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Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors by BORES, Eric E, DEATON, David N, WRIGHT, Lois L, HASSELL, Anne M, MCFADYEN, Robert B, MILLER, Aaron B, MILLER, Larry R, PAULICK, Margot G, SHEWCHUK, Lisa M, THOMPSON, James B, WILLARD, Derril H

“…The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites…”
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Replication-Associated Activities of Purified Human Papillomavirus Type 11 E1 Helicase by Rocque, Warren J., Porter, David J.T., Barnes, Julie A., Dixon, Eric P., Lobe, David C., Su, Jui-Lan, Willard, Derril H., Gaillard, Richard, Condreay, J.Patrick, Clay, William C., Hoffman, Christine R., Overton, Laurie K., Pahel, Greg, Kost, Thomas A., Phelps, William C.

“…Replication of human papillomavirus type11 (HPV11) requires both the E1 and the E2 proteins. E1 is structurally and functionally similar to SV40 large…”
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Product Release Is the Major Contributor tok cat for the Hepatitis C Virus Helicase-catalyzed Strand Separation of Short Duplex DNA by Porter, David J.T., Short, Steven A., Hanlon, Mary H., Preugschat, Frank, Wilson, Jeanne E., Willard, Derril H., Consler, Thomas G.

“…Hepatitis C virus (HCV) helicase catalyzes the ATP-dependent strand separation of duplex RNA and DNA containing a 3′ single-stranded tail. Equilibrium and…”
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Catalytic Activity of the SH2 Domain of Human pp60c-src; Evidence from NMR, Mass Spectrometry, Site-Directed Mutagenesis and Kinetic Studies for an Inherent Phosphatase Activity by Boerner, Renee J, Consler, Thomas G, Gampe, Robert T, Weigl, Debbra, Willard, Derril H, Davis, Donald G, Edison, Ann M, Loganzo, Frank, Kassel, D. B

“…During solution structural studies it was apparent that the human recombinant pp60c-src SH2 domain (srcSH2, residues 144-249) possessed an inherent phosphatase…”
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