Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition von Ohren, Jeffrey F, Chen, Huifen, Pavlovsky, Alexander, Whitehead, Christopher, Zhang, Erli, Kuffa, Peter, Yan, Chunhong, McConnell, Patrick, Spessard, Cindy, Banotai, Craig, Mueller, W Thomas, Delaney, Amy, Omer, Charles, Sebolt-Leopold, Judith, Dudley, David T, Leung, Iris K, Flamme, Cathlin, Warmus, Joseph, Kaufman, Michael, Barrett, Stephen, Tecle, Haile, Hasemann, Charles A

Volltext

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo von Sebolt-Leopold, Judith S., Dudley, David T., Herrera, Roman, Becelaere, Keri Van, Wiland, Amy, Gowan, Richard C., Tecle, Haile, Barrett, Stephen D., Bridges, Alexander, Przybranowski, Sally, Leopold, W.R., Saltiel, Alan R.

Volltext

The pharmacology of the novel and selective sigma ligand, PD 144418 von AKUNNE, H. C, WHETZEL, S. Z, WILEY, J. N, CORBIN, A. E, NINTEMAN, F. W, TECLE, H, PEI, Y, PUGSLEY, T. A, HEFFNER, T. G

Volltext

In vitro and in vivo evaluation of the subtype-selective muscarinic agonist PD 151832 von Jaen, J., Barrett, S., Brann, M., Callahan, M., Davis, R., Doyle, P., Eubanks, D., Lauffer, D., Lauffer, L., Lipinski, W., Moreland, D., Nelson, C., Raby, C., Schwarz, R., Spencer, C., Tecle, H.

Volltext

Synthesis and Sar of bulky 1-azabicyclo[2.2.1]-3-one oximes as muscarinic receptor subtype selective agonists von Tecle, H., Lauffer, D.J., Mirzadegan, T., Moos, W.H., Moreland, D.W., Pavia, M.R., Schwarz, R.D., Davis, R.E.

Volltext

CI-1017, a functionally M1-selective muscarinic agonist: design, synthesis, and preclinical pharmacology von Tecle, H, Schwarz, R.D, Barrett, S.D, Callahan, M.J, Caprathe, B.W, Davis, R.E, Doyle, P, Emmerling, M, Lauffer, D.J, Mirzadegan, T, Moreland, D.W, Lipiniski, W, Nelson, C, Raby, C, Spencer, C, Spiegel, K, Thomas, A.J, Jaen, J.C

Volltext

A rationale for the design and synthesis of m1 selective muscarinic agonists von Tecle, H., Mirzadegan, T., Moos, W.H., Moreland, D.W., Pavia, M.R., Schwarz, R.D., Davis, R.E.

Volltext

(±)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oximes: Potent muscarinic agonists von Tecle, H., Lauffer, D.J., Davis, R.E., Mirzadegan, T., Moreland, D.W., Schwan, R.D., Thomas, A.J., Raby, C., Eubanks, D., Brann, M.R., Jaen, J.C.

Volltext

Z-(±)-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl) oximes as potential m1-subtype selective muscarinic agonists von Tecle, H., Jaen, J.C., Augelli-Szafran, C., Barrett, S.D., Caprathe, B.W., Lauffer, D.J., Mirzadegan, T., Moos, W.H., Moreland, D.W., Pavia, M.R., Schwarz, R.D., Thomas, A.J., Davis, R.E.

Volltext

4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties von Jaen, Juan C, Wise, Lawrence D, Caprathe, Bradley W, Tecle, Haile, Bergmeier, Stephen, Humblet, Christine C, Heffner, Thomas G, Meltzer, Leonard T, Pugsley, Thomas A

Volltext

Design and Synthesis of m1-Selective Muscarinic Agonists:  (R)-(−)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3‘-Methoxyphenyl)-2-propynyl)- oxime Maleate (CI-1017), a Functionally... von Tecle, Haile, Barrett, Stephen D, Lauffer, David J, Augelli-Szafran, Corinne, Brann, Mark R, Callahan, Michael J, Caprathe, Bradley. W, Davis, Robert E, Doyle, Patricia D, Eubanks, David, Lipiniski, William, Mirzadegan, Tara, Moos, Walter H, Moreland, D. W, Nelson, Carrie B, Pavia, Michael R, Raby, Charlotte, Schwarz, Roy D, Spencer, Carolyn J, Thomas, Anthony J, Jaen, Juan C

Volltext

Effect of mutating aspart ate 103 to glutamate or asparagine in the Hm2 subtype on binding of agonists and antagonists of varied pKa and subtype selectivity von Spencer, C.J., Schwarz, R.D., Moreland, D.W., Thomas, A.J., Tecle, H.

Volltext

Effect of mutating aspart ate 103 to glutamate or asparagine in the Hm2 subtype on binding of agonists and antagonists of varied pK a and subtype selectivity von Spencer, C.J., Schwarz, R.D., Moreland, D.W., Thomas, A.J., Tecle, H.

Volltext

Mutations of aspartate 103 in the Hm2 receptor and alterations in receptor binding properties of muscarinic agonists von Schwarz, Roy D., Spencer, Carolyn J., Jaen, Juan C., Mirzadegan, Tara, Moreland, David, Tecle, Haile, Thomas, Anthony J.

Volltext

Characterization of muscarinic agonists in recombinant cell lines von Schwarz, Roy D., Davis, Robert E., Jaen, Juan C., Spencer, Carolyn J., Tecle, Haile, Thomas, Anthony J.

Volltext

Development of M1 subtype selective muscarinic agonists for Alzheimer's disease: Translation of in vitro selectivity into in vivo efficacy von Schwarz, R.D., Callahan, M.J., Davis, R.E., Jaen, J.C., Tecle, H.

Volltext

Molecular modeling studies of the m1 and m2 muscarinic receptors leading to the design of selective m1 agonists von Mirzadegan, T., Tecle, H., Lauffer, D.J., Humblet, C.

Volltext

Development of M1 subtype selective muscarinic agonists for Alzheimer's disease : Translation of in vitro selectivity into in vivo efficacy: Challenges and opportunities for develo... von SCHWARZ, R. D, CALLAHAN, M. J, DAVIS, R. E, JAEN, J. C, TECLE, H

Volltext

EFFICIENT SYNTHESIS OF EXO-1-AZABICYCLO[2.2.1]HEPTAN-3-OL von Barrett, Stephen D., Jaen, Juan C., Caprathe, Bradley W., Thomas, Anthony J., Tecle, Haile

Volltext

Aryleneyne 1-azabicyclo[2.2.1]heptan-3-one oximes: Potent muscarinic agonists von Tecle, H., Lauffer, D.J., Davis, R.E., Mirzadegan, T., Moreland, D.W., Schwarz, R.D., Thomas, A.J., Raby, C., Jaen, J.C.

Volltext