Search Results - "MILLER, Larry R"

Ketoamide-Based Inhibitors of Cysteine Protease, Cathepsin K:  P3 Modifications by Tavares, Francis X, Deaton, David N, Miller, Larry R, Wright, Lois L

“…Osteoporosis is a disease characterized by skeletal fragility. Cathepsin K, a lysosomal cysteine protease, has been implicated in the osteoclast mediated bone…”
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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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Potent and Selective Ketoamide-Based Inhibitors of Cysteine Protease, Cathepsin K by Tavares, Francis X, Deaton, David N, Miller, Aaron B, Miller, Larry R, Wright, Lois L, Zhou, Hui-Qiang

“…Cathepsin K, a lysosomal cysteine protease of the papain superfamily, is abundantly and selectively expressed in osteoclasts, suggesting that this enzyme is…”
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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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Ketoheterocycle-based inhibitors of cathepsin K: A novel entry into the synthesis of peptidic ketoheterocycles by Tavares, Francis X., Deaton, David N., Miller, Aaron B., Miller, Larry R., Wright, Lois L.

“…Ketoheterocyclic inhibitors of cathepsin K have been disclosed. SAR of potency enhancing P 2–P 3 groups coupled with ketoheterocyclic warheads to provide…”
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Acyclic, orally bioavailable ketone-based cathepsin K inhibitors by Barrett, David G., Catalano, John G., Deaton, David N., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Samano, Vicente, Tavares, Francis X., Wells-Knecht, Kevin J., Wright, Lois L., Zhou, Hui-Qiang Q.

“…Starting from a potent ketone-based inhibitor with poor drug properties, incorporation of P 2–P 3 elements from a ketoamide-based inhibitor led to the…”
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Design of small molecule ketoamide-based inhibitors of cathepsin K by Catalano, John G., Deaton, David N., Long, Stacey T., McFadyen, Robert B., Miller, Larry R., Payne, J.Alan, Wells-Knecht, Kevin J., Wright, Lois L.

“…A novel series of ketoamide-based inhibitors of cathepsin K has been identified. Modifications to P 2 and P 3 elements were crucial to enhancing inhibitory…”
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A structural screening approach to ketoamide-based inhibitors of cathepsin K by Barrett, David G., Catalano, John G., Deaton, David N., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., Wells-Knecht, Kevin J., Wright, Lois L.

“…Several novel ketoamide-based inhibitors of cathepsin K have been identified. Starting from a modestly potent inhibitor, structural screening of P 2 elements…”
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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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Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K by Barrett, David G., Catalano, John G., Deaton, David N., Long, Stacey T., Miller, Larry R., Tavares, Francis X., Wells-Knecht, Kevin J., Wright, Lois L., Zhou, Hui-Qiang Q.

“…An orally available series of ketoamide-based inhibitors of cathepsin K has been identified. Starting from a potent inhibitor with poor oral bioavailability,…”
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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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Impact of an extract from the bran layer of rice on the nutrition of lactating mothers and growth of their exclusively breastfed infants: a longitudinal study by Sanchez, Guillermo E., Sullivan, Glenn H., Miller, Larry R.

“…Background: The nutritional composition of the bran layer of rice (RB), a globally available product of the rice milling process, has attracted attention as a…”
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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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RoBo-1, a Novel Member of the Urokinase Plasminogen Activator Receptor/CD59/Ly-6/Snake Toxin Family Selectively Expressed in Rat Bone and Growth Plate Cartilage by Noel, L S, Champion, B R, Holley, C L, Simmons, C J, Morris, D C, Payne, J A, Lean, J M, Chambers, T J, Zaman, G, Lanyon, L E, Suva, L J, Miller, L R

“…Using differential display polymerase chain reaction, we cloned a novel cDNA named RoBo-1 from rat tibia. RoBo-1 is abundantly expressed in bone, including the…”
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An immunohistochemical study of perianal Paget's disease. Possible origins and clinical implications by Miller, L R, McCunniff, A J, Randall, M E

“…The histogenesis of perianal Paget's disease is controversial. A clinical and pathologic study was done of a patient with a history of adenocarcinoma of the…”
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P 2–P 3 conformationally constrained ketoamide-based inhibitors of cathepsin K by Barrett, David G., Boncek, Virginia M., Catalano, John G., Deaton, David N., Hassell, Anne M., Jurgensen, Cynthia H., Long, Stacey T., McFadyen, Robert B., Miller, Aaron B., Miller, Larry R., 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.

“…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 P 2–P 3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P 1′, P 1, and/or P 3 substitutions by Barrett, David G., Catalano, John G., 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., Wright, Lois L.

“…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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