Search Results - "Knighton, Daniel"

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth by Murray, Brion W, Guo, Chuangxing, Piraino, Joseph, Westwick, John K, Zhang, Cathy, Lamerdin, Jane, Dagostino, Eleanor, Knighton, Daniel, Loi, Cho-Ming, Zager, Michael, Kraynov, Eugenia, Popoff, Ian, Christensen, James G, Martinez, Ricardo, Kephart, Susan E, Marakovits, Joseph, Karlicek, Shannon, Bergqvist, Simon, Smeal, Tod

“…Despite abundant evidence that aberrant Rho-family GTPase activation contributes to most steps of cancer initiation and progression, there is a dearth of…”
Get full text

Discovery of Pyrroloaminopyrazoles as Novel PAK Inhibitors by Guo, Chuangxing, McAlpine, Indrawan, Zhang, Junhu, Knighton, Daniel D, Kephart, Susan, Johnson, M. Catherine, Li, Haitao, Bouzida, Djamal, Yang, Anle, Dong, Liming, Marakovits, Joseph, Tikhe, Jayashree, Richardson, Paul, Guo, Lisa C, Kania, Robert, Edwards, Martin P, Kraynov, Eugenia, Christensen, James, Piraino, Joseph, Lee, Joseph, Dagostino, Eleanor, Del-Carmen, Christine, Deng, Ya-Li, Smeal, Tod, Murray, Brion W

“…The P21-activated kinases (PAK) are emerging antitumor therapeutic targets. In this paper, we describe the discovery of potent PAK inhibitors guided by…”
Get full text

Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design by Cheng, Hengmiao, Li, Chunze, Bailey, Simon, Baxi, Sangita M, Goulet, Lance, Guo, Lisa, Hoffman, Jacqui, Jiang, Ying, Johnson, Theodore Otto, Johnson, Ted W, Knighton, Daniel R, Li, John, Liu, Kevin K.-C, Liu, Zhengyu, Marx, Matthew A, Walls, Marlena, Wells, Peter A, Yin, Min-Jean, Zhu, Jinjiang, Zientek, Michael

“…PI3K, AKT, and mTOR are key kinases from PI3K signaling pathway being extensively pursued to treat a variety of cancers in oncology. To search for a…”
Get full text

Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR by Le, Phuong T., Cheng, Hengmiao, Ninkovic, Sacha, Plewe, Michael, Huang, Xiaojun, Wang, Hai, Bagrodia, Shubha, Sun, Shaoxian, Knighton, Daniel R., LaFleur Rogers, Caroline M., Pannifer, Andrew, Greasley, Samantha, Dalvie, Deepak, Zhang, Eric

“…Lead optimization efforts that employed structure base drug design and physicochemical property based optimization leading to the discovery of a novel series…”
Get full text

Crystal structures of human calcineurin and the human FKBP12-FK506-calcineurin complex by Kissinger, Charles R, Parge, Hans E, Knighton, Daniel R, Lewis, Cristina T, Pelletier, Laura A, Tempczyk, Anna, Kalish, Vincent J, Tucker, Kathleen D, Showalter, Richard E, Moomaw, Ellen W, Gastinel, Louis N, Habuka, Noriyuki, Chen, Xinghai, Maldonado, Fausto, Barker, John E, Bacquet, Russell, Villafranca, J. Ernest

“…Calcineurin (CaN) is a calcium- and calmodulin-dependent protein serine/threonine phosphate which is critical for several important cellular processes,…”
Get full text

Structure of a Peptide Inhibitor Bound to the Catalytic Subunit of Cyclic Adenosine Monophosphate-Dependent Protein Kinase by Knighton, Daniel R., Zheng, Jianhua, Lynn F. Ten Eyck, Xuong, Nguyen-Huu, Taylor, Susan S., Sowadski, Janusz M.

“…The structure of a 20-amino acid peptide inhibitor bound to the catalytic subunit of cyclic AMP-dependent protein kinase, and its interactions with the enzyme,…”
Get full text

Crystal Structure of the Catalytic Subunit of Cyclic Adenosine Monophosphate-Dependent Protein Kinase by Knighton, Daniel R., Zheng, Jianhua, Lynn F. Ten Eyck, Ashford, Victor A., Xuong, Nguyen-Huu, Taylor, Susan S., Sowadski, Janusz M.

“…The crystal structure of the catalytic subunit of cyclic adenosine monophosphate--dependent protein kinase complexed with a 20-amino acid substrate analog…”
Get full text

Structural Basis of the Intrasteric Regulation of Myosin Light Chain Kinases by Knighton, Daniel R., Pearson, Richard B., Sowadski, Janusz M., Means, Anthony R., Lynn F. Ten Eyck, Taylor, Susan S., Kemp, Bruce E.

“…The smooth muscle myosin light chain kinase (smMLCK) catalytic core was modeled by using the crystallographic coordinates of the cyclic AMP-dependent protein…”
Get full text

Crystal structures of the myristylated catalytic subunit of cAMP‐dependent protein kinase reveal open and closed conformations by Zheng, Jianhua, Knighton, Daniel R., Taylor, Susan S., Xuong, Nguyen‐Huu, Sowadski, Janusz M., Eyck, Lynn F. Ten

“…Three crystal structures, representing two distinct conformational states, of the mammalian catalytic subunit of cAMP‐dependent protein kinase were solved…”
Get full text

Structural Features that Specify Tyrosine Kinase Activity Deduced from Homology Modeling of the Epidermal Growth Factor Receptor by Knighton, Daniel R., Cadena, Deborah L., Zheng, Jianhua, Lynn F. Ten Eyck, Taylor, Susan S., Sowadski, Janusz M., Gill, Gordon N.

“…To identify structural features that distinguish protein-tyrosine kinases from protein-serine kinases, a molecular model of the kinase domain of epidermal…”
Get full text

Structure of and kinetic channelling in bifunctional dihydrofolate reductase-thymidylate synthase by Knighton, Daniel R, Kan, Chen-Chen, Howland, Eleanor, Janson, Cheryl A, Hostomska, Zuzana, Welsh, Katherine M, Matthews, David A

“…The bifunctional enzyme dihydrofolate reductase-thymidylate synthase catalyses both the reductive methylation of 2'-deoxyuridylate and the subsequent reduction…”
Get full text

Structure-Based Design of Novel, Urea-Containing FKBP12 Inhibitors by Dragovich, Peter S, Barker, John E, French, Judy, Imbacuan, Michael, Kalish, Vincent J, Kissinger, Charles R, Knighton, Daniel R, Lewis, Cristina T, Moomaw, Ellen W, Parge, Hans E, Pelletier, Laura A. K, Prins, Thomas J, Showalter, Richard E, Tatlock, John H, Tucker, Kathleen D, Villafranca, J. Ernest

“…The structure-based design and subsequent chemical synthesis of novel, urea-containing FKBP12 inhibitors are described. These compounds are shown to disrupt…”
Get full text

Corrigendum to “Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR” [Bioorg. Med. Chem. Lett. 22 (2012) 5098–5103] by Le, Phuong T., Cheng, Hengmiao, Ninkovic, Sacha, Plewe, Michael, Huang, Xiaojun, Wang, Hai, Bagrodia, Shubha, Sun, Shaoxian, Knighton, Daniel R., LaFleur Rogers, Caroline M., Pannifer, Andrew, Greasley, Samantha, Dalvie, Deepak, Zhang, Eric

Get full text

Crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with magnesium-ATP and peptide inhibitor by Zheng, Jianhua, Knighton, Daniel R, Ten Eyck, Lynn F, Karlsson, Rolf, Xuong, N, Taylor, Susan S, Sowadski, Janusz M

Get full text

cAMP-Dependent Protein Kinase Defines a Family of Enzymes by Taylor, Susan S., Zheng, Jianhua, Radzioandzelm, Elzbieta, Knighton, Daniel R., Lynn F. Ten Eyck, Sowadski, Janusz M., Herberg, Friedrich W., Yonemoto, Wes M.

“…The structure of the recombinant mouse catalytic subunit of cAMP-dependent protein kinase is reviewed with particular emphasis on the overall features and…”
Get full text

Crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MgATP and peptide inhibitor by JIANHUA ZHENG, KNIGHTON, D. R, TEN EYCK, L. F, KARLSSON, R, NGUYEN-HUU XUONG, TAYLOR, S. S, SOWADSKI, J. M

“…The structure of a ternary complex of the catalytic subunit of cAMP-dependent protein kinase, MgATP, and a 20-residue inhibitor peptide was determined at a…”
Get full text

Abstract 5779: The discovery of the potent and selective PI3K/mTOR dual inhibitor PF-04691502 through structure-based drug design by Cheng, Henry, Bagrodia, Shubha, Bailey, Simon, Bhumalkar, Dilip, Dress, Klaus, Edwards, Martin, Gehring, Michael R., Guo, Lisa, Hoffman, Jacqui, Hu, Qiyue, Huang, Xiaojun, Johnson, Catherine, Johnson, Ted O., Kania, Robert, Knighton, Daniel R., Le, Phuong, Li, Haitao, Li, Samuel, Liu, Kevin, Liu, Zhengyu, Marx, Matthew A., Nambu, Mitch, Ninkovic, Sacha, Nowlin, Dawn, Pairish, Mason, Pannifer, Andrew, Plewe, Michael, Rodgers, Caroline, Smith, Graham, Sun, Shaoxian, Tran, Khanh, Wang, Hai, Zbieg, Jason, Zhu, Peter

“…Abstract The phosphatidylinositol 3-kinase (PI3K) signaling pathway plays crucial roles in cell growth, proliferation and survival. Genomic aberrations in the…”
Get full text

A template for the protein kinase family by Taylor, S S, Knighton, D R, Zheng, J, Sowadski, J M, Gibbs, C S, Zoller, M J

“…The crystal structure of the catalytic subunit of cAMP-dependent protein kinase, complexed with ATP and a 20-residue inhibitor peptide, is reviewed and…”
Get more information

Structural Framework for the Protein Kinase Family by Taylor, S S, Knighton, D R, Zheng, J, Ten Eyck, L F, Sowadski, J M

“…In this review, we have summarized the general structural features of the catalytic subunit of cAMP-dependent protein kinase, emphasizing those features that…”
Get full text

Electrostatic Channeling in the Bifunctional Enzyme Dihydrofolate Reductase-thymidylate Synthase by Elcock, Adrian H., Potter, Michael J., Matthews, David A., Knighton, Daniel R., McCammon, J.Andrew

“…The bifunctional enzyme dihydrofolate reductase-thymidylate synthase (DHFR-TS) carries out two distinct reactions, with the dihydrofolate produced by the…”
Get full text