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LoGrasso, Philip
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LoGrasso, Philip

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Positions

  • 2005 - Senior Scientific Director, Discovery Biology, Translational Research Institute , Scripps Research
  • Research Fellow, Merck & Co., Inc.
  • Program Director, National Institute of General Medical Sciences, National Institutes of Health
  • Director of Preclinical Research and Development, Avera Pharmaceuticals
  • 2007 - 2017 Professor, Molecular Therapeutics , Scripps Research
  • 2005 - 2017 Professor (Joint Appointment), Metabolism and Aging , Scripps Research
Dr. Philip LoGrasso studies structure function relationships of enzymes for drug discovery and development.

Research Areas research areas

  • Drug Discovery (UMLS)
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Publications

recent publications

  • academic article

    • Grassi, D., Howard, S., Zhou, M., Diaz-Perez, N., Urban, N. T., Guerrero-Given, D., Kamasawa, N., Volpicelli-Daley, L. A., LoGrasso, P., Lasmezas, C. I. Identification of a highly neurotoxic α-synuclein species inducing mitochondrial damage and mitophagy in Parkinson's disease Proceedings of the National Academy of Sciences of the United States of America  2018 115:E2634-E2643  DOI:10.1073/pnas.1713849115  PMID:29487216
    • Gao, S., Howard, S., Lograsso, P. V. Pharmacological inhibition of c-Jun N-terminal Kinase reduces food intake and sensitizes leptin's anorectic signaling actions Scientific Reports  2017 7  DOI:10.1038/srep41795  PMID:28165482  PMCID:PMC5292945
    • Feng, Y. B., Lograsso, P. V., Defert, O., Li, R. Rho kinase (ROCK) inhibitors and their therapeutic potential Journal of Medicinal Chemistry  2016 59:2269-2300  DOI:10.1021/acs.jmedchem.5b00683  PMID:26486225
    • Iqbal, S., Howard, S., Lograsso, P. V. Serum- and glucocorticoid-inducible kinase 1 confers protection in cell-based and in in vivo neurotoxin models via the c-Jun N-terminal kinase signaling pathway Molecular and Cellular Biology  2015 35:1992-2006  DOI:10.1128/mcb.01510-14  PMID:25825522
    • Zheng, K., Park, C. M., Iqbal, S., Hernandez, P., Park, H., Lograsso, P. V., Feng, Y. Pyridopyrimidinone derivatives as potent and selective c-jun N-terminal kinase (JNK) inhibitors ACS Medicinal Chemistry Letters  2015 6:413-418  DOI:10.1021/ml500474d  PMID:25893042  PMCID:PMC4394340
    • Yin, Y., Zheng, K., Eid, N., Howard, S., Jeong, J. H., Yi, F., Guo, J., Park, C. M., Bibian, M., Wu, W., Hernandez, P., Park, H., et al. Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors Journal of Medicinal Chemistry  2015 58:1846-1861  DOI:10.1021/jm501680m  PMID:25621531  PMCID:PMC4349585
    • Park, H., Iqbal, S., Hernandez, P., Mora, R., Zheng, K., Feng, Y., LoGrasso, P. Structural basis and biological consequences for JNK2/3 isoform selective aminopyrazoles Scientific Reports  2015 5  DOI:10.1038/srep08047  PMID:25623238  PMCID:PMC4306959
    • Zheng, K., Iqbal, S., Hernandez, P., Park, H., Lograsso, P. V., Feng, Y. Design and synthesis of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole derivatives Journal of Medicinal Chemistry  2014 57:10013-10030  DOI:10.1021/jm501256y  PMID:25393557  PMCID:PMC4266361
    • Feng, Y., Lograsso, P. V. Rho kinase inhibitors: a patent review (2012-2013) Expert Opinion on Therapeutic Patents  2014 24:295-307  DOI:10.1517/13543776.2014.863279  PMID:24283930
    • He, Y., Duckett, D., Chen, W., Ling, Y. Y., Cameron, M. D., Lin, L., Ruiz, C. H., Lograsso, P. V., Kamenecka, T. M., Koenig, M. Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors Bioorganic & Medicinal Chemistry Letters  2014 24:161-164  DOI:10.1016/j.bmcl.2013.11.052  PMID:24332487  PMCID:PMC4540177
    • Feng, Y. B., Chambers, J. W., Iqbal, S., Koenig, M., Park, H., Cherry, L., Hernandez, P., Figuera-Losada, M., Lograsso, P. V. A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases ACS Chemical Biology  2013 8:1747-1754  DOI:10.1021/cb3006165  PMID:23751758  PMCID:PMC3759981
    • Feng, Y., Chambers, J. W., Iqbal, S., Koenig, M., Park, H., Cherry, L., Hernandez, P., Figuera-Losada, M., Lograsso, P. V. A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases ACS Chemical Biology  2013 8:1747-1754  DOI:10.1021/cb3006165  PMID:23751758  PMCID:PMC3759981
    • Yin, Y., Lin, L., Ruiz, C., Khan, S., Cameron, M. D., Grant, W., Pocas, J., Eid, N., Park, H., Schroter, T., Lograsso, P. V., Feng, Y. Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors Journal of Medicinal Chemistry  2013 56:3568-3581  DOI:10.1021/jm400062r  PMID:23570561
    • Chowdhury, S., Chen, Y. T., Fang, X. G., Grant, W., Pocas, J., Cameron, M. D., Ruiz, C., Lin, L., Park, H., Schroter, T., Bannister, T. D., LoGrasso, P. V., et al. Amino acid derived quinazolines as Rock/PKA inhibitors Bioorganic & Medicinal Chemistry Letters  2013 23:1592-1599  DOI:10.1016/j.bmcl.2013.01.109  PMID:23416002
    • Chambers, J. W., Pachori, A., Howard, S., Iqbal, S., LoGrasso, P. V. Inhibition of JNK mitochondrial localization and signaling is protective against ischemia/reperfusion injury in rats Journal of Biological Chemistry  2013 288:4000-4011  DOI:10.1074/jbc.M112.406777  PMID:23258542  PMCID:PMC3567652
    • Chambers, J. W., Howard, S., LoGrasso, P. V. Blocking c-jun n-terminal kinase (jnk) translocation to the mitochondria prevents 6-hydroxydopamine-induced toxicity in vitro and in vivo Journal of Biological Chemistry  2013 288:1079-1087  DOI:10.1074/jbc.M112.421354  PMID:23184940  PMCID:PMC3542993
    • Jeso, V., Iqbal, S., Hernandez, P., Cameron, M. D., Park, H., Lograsso, P. V., Micalizio, G. C. Synthesis of benzoquinone ansamycin-inspired macrocyclic lactams from shikimic acid Angewandte Chemie-International Edition  2013 52:4800-4804  DOI:10.1002/anie.201301323  PMID:23554224
    • Laughlin, J. D., Nwachukwu, J. C., Figuera-Losada, M., Cherry, L., Nettles, K. W., LoGrasso, P. V. Structural mechanisms of allostery and autoinhibition in JNK family kinases Structure  2012 20:2174-2184  DOI:10.1016/j.str.2012.09.021  PMID:23142346  PMCID:PMC3589125
    • Boregowda, S. V., Krishnappa, V., Chambers, J. W., Lograsso, P. V., Lai, W. T., Ortiz, L. A., Phinney, D. G. Atmospheric oxygen inhibits growth and differentiation of marrow-derived mouse mesenchymal stem cells via a p53-dependent mechanism: Implications for long-term culture expansion Stem Cells  2012 30:975-987  DOI:10.1002/stem.1069  PMID:22367737  PMCID:PMC3683654
    • Figuera-Losada, M., LoGrasso, P. V. Enzyme kinetics and interaction studies for human jnk1 beta 1 and substrates activating transcription factor 2 (atf2) and c-jun n-terminal kinase (c-jun) Journal of Biological Chemistry  2012 287:13291-13302  DOI:10.1074/jbc.M111.323766  PMID:22351776  PMCID:PMC3339953
    • Zhang, T., Inesta-Vaquera, F., Niepel, M., Zhang, J. M., Ficarro, S. B., Machleidt, T., Xie, T., Marto, J. A., Kim, N., Sim, T., Laughlin, J. D., Park, H., et al. Discovery of potent and selective covalent inhibitors of JNK Chemistry & Biology  2012 19:140-154  DOI:10.1016/j.chembiol.2011.11.010  PMID:22284361  PMCID:PMC3270411
    • Sessions, E. H., Chowdhury, S., Yin, Y., Pocas, J. R., Grant, W., Schroter, T., Lin, L., Ruiz, C., Cameron, M. D., LoGrasso, P., Bannister, T. D., Feng, Y. B. Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II) Bioorganic & Medicinal Chemistry Letters  2011 21:7113-7118  DOI:10.1016/j.bmcl.2011.09.084  PMID:22018789
    • Chowdhury, S., Sessions, E. H., Pocas, J. R., Grant, W., Schroter, T., Lin, L., Ruiz, C., Cameron, M. D., Schurer, S., LoGrasso, P., Bannister, T. D., Feng, Y. B. Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I) Bioorganic & Medicinal Chemistry Letters  2011 21:7107-7112  DOI:10.1016/j.bmcl.2011.09.083  PMID:22004718
    • Jeso, V., Cherry, L., Macklin, T. K., Pan, S. C., LoGrasso, P. V., Micalizio, G. C. Convergent synthesis and discovery of a natural product-inspired paralog-selective Hsp90 inhibitor Organic Letters  2011 13:5108-5111  DOI:10.1021/ol2019828  PMID:21866939
    • Chambers, J. W., Cherry, L., Laughlin, J. D., Figuera-Losada, M., LoGrasso, P. V. Selective inhibition of mitochondrial jnk signaling achieved using peptide mimicry of the sab kinase interacting motif-1 (kim1) ACS Chemical Biology  2011 6:808-818  DOI:10.1021/cb200062a  PMID:21563797  PMCID:PMC3158843
    • Chambers, J. W., LoGrasso, P. V. Mitochondrial c-jun n-terminal kinase (jnk) signaling initiates physiological changes resulting in amplification of reactive oxygen species generation Journal of Biological Chemistry  2011 286:16052-16062  DOI:10.1074/jbc.M111.223602  PMID:21454558  PMCID:PMC3091214
    • Noel, R., Shin, Y., Song, X. Y., He, Y. J., Koenig, M., Chen, W. M., Ling, Y. Y., Lin, L., Ruiz, C. H., LoGrasso, P., Cameron, M. D., Duckett, D. R., et al. Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2011 21:2732-2735  DOI:10.1016/j.bmcl.2010.11.104  PMID:21185177  PMCID:PMC3081976
    • Crocker, C. E., Khan, S., Cameron, M. D., Robertson, H. A., Robertson, G. S., LoGrasso, P. JNK inhibition protects dopamine neurons and provides behavioral improvement in a rat 6-hydroxydopamine model of Parkinson's Disease ACS Chemical Neuroscience  2011 2:207-212  DOI:10.1021/cn1001107  PMID:21666838  PMCID:PMC3110072
    • Chambers, J. W., Pachori, A., Howard, S., Ganno, M., Hansen, D., Song, X. Y., Kamenecka, T., Duckett, D., Chen, W. M., Ling, Y. Y., Cherry, L., Cameron, M. D. Small molecule c-jun-N-terminal Kinase (JNK) inhibitors protect dopaminergic neurons in a model of Parkinson's Disease ACS Chemical Neuroscience  2011 2:198-206  DOI:10.1021/cn100109k  PMID:21666839  PMCID:PMC3110074
    • He, Y. J., Kamenecka, T. M., Shin, Y. S., Song, X. Y., Jiang, R., Noel, R., Duckett, D., Chen, W. M., Ling, Y. Y., Cameron, M. D., Lin, L., Khan, S., et al. Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors Bioorganic & Medicinal Chemistry Letters  2011 21:1719-1723  DOI:10.1016/j.bmcl.2011.01.079  PMID:21316221  PMCID:PMC3052630
    • Fang, X. A., Chen, Y. T., Sessions, E. H., Chowdhury, S., Vojkovsky, T., Yin, Y., Pocas, J. R., Grant, W., Schroter, T., Lin, L., Ruiz, C., Cameron, M. D., et al. Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2011 21:1844-1848  DOI:10.1016/j.bmcl.2011.01.039  PMID:21349713
    • Chen, Y. T., Vojkovsky, T., Fang, X. G., Pocas, J. R., Grant, W., Handy, A. M. W., Schroter, T., LoGrasso, P., Bannister, T. D., Fang, Y. B. Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors MedChemComm  2011 2:73-75  DOI:10.1039/c0md00194e
    • Fang, X. G., Yin, Y., Chen, Y. T., Yao, L., Wang, B., Cameron, M. D., Lin, L., Khan, S., Ruiz, C., Schroter, T., Grant, W., Weiser, A., et al. Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors Journal of Medicinal Chemistry  2010 53:5727-5737  DOI:10.1021/jm100579r  PMID:20684608
    • Yin, Y., Cameron, M. D., Lin, L., Khan, S., Schroter, T., Grant, W., Pocas, J., Chen, Y. T., Schurer, S., Pachori, A., LoGrasso, P., Feng, Y. B. Discovery of potent and selective urea-based ROCK inhibitors and their effects on intraocular pressure in rats ACS Medicinal Chemistry Letters  2010 1:175-179  DOI:10.1021/ml1000382  PMID:24900192  PMCID:PMC4007833
    • Sessions, E. H., Smolinski, M., Wang, B., Frackowiak, B., Chowdhury, S., Yin, Y., Chen, Y. T., Ruiz, C., Lin, L., Pocas, J., Schroter, T., Cameron, M. D., et al. The development of benzimidazoles as selective Rho kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2010 20:1939-1943  DOI:10.1016/j.bmcl.2010.01.124  PMID:20167489
    • Kamenecka, T., Jiang, R., Song, X. Y., Duckett, D., Chen, W. M., Ling, Y. Y., Habel, J., Laughlin, J. D., Chambers, J., Figuera-Losada, M., Cameron, M. D., Lin, L., et al. Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors Journal of Medicinal Chemistry  2010 53:419-431  DOI:10.1021/jm901351f  PMID:19947601  PMCID:PMC2804074
    • Yin, Y., Lin, L., Ruiz, C., Cameron, M. D., Pocas, J., Grant, W., Schroter, T., Chen, W. M., Duckett, D., Schurer, S., LoGrasso, P., Feng, Y. B. Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors Bioorganic & Medicinal Chemistry Letters  2009 19:6686-6690  DOI:10.1016/j.bmcl.2009.09.115  PMID:19837589
    • Shin, Y. S., Chen, W. M., Habel, J., Duckett, D., Ling, Y. Y., Koenig, M., He, Y. J., Vojkovsky, T., LoGrasso, P., Kamenecka, T. M. Synthesis and sar of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors Bioorganic & Medicinal Chemistry Letters  2009 19:3344-3347  DOI:10.1016/j.bmcl.2009.03.086  PMID:19433357  PMCID:PMC2737472
    • Kamenecka, T., Habel, J., Duckett, D., Chen, W. M., Ling, Y. Y., Frackowiak, B., Jiang, R., Shin, Y. S., Song, X. Y., LoGrasso, P. Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-jun N-terminal kinase 3 (JNK3) over p38 Journal of Biological Chemistry  2009 284:12853-12861  DOI:10.1074/jbc.M809430200  PMID:19261605  PMCID:PMC2676016
    • LoGrasso, P. V., Feng, Y. B. Rho kinase (ROCK) inhibitors and their application to inflammatory disorders Current Topics in Medicinal Chemistry  2009 9:704-723  DOI:10.2174/156802609789044452  PMID:19689376
    • Sessions, E. H., Yin, Y., Bannister, T. D., Weiser, A., Griffin, E., Pocas, J., Cameron, M. D., Ruiz, C., Lin, L., Schurer, S. C., Schroter, T., LoGrasso, P., et al. Benzimidazole- and benzoxazole-based inhibitors of Rho kinase Bioorganic & Medicinal Chemistry Letters  2008 18:6390-6393  DOI:10.1016/j.bmcl.2008.10.095  PMID:18996009
    • Chen, Y. T., Bannister, T. D., Weiser, A., Griffin, E., Lin, L., Ruiz, C., Cameron, M. D., Schurer, S., Duckett, D., Schroter, T., LoGrasso, P., Feng, Y. B. Chroman-3-amides as potent Rho kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2008 18:6406-6409  DOI:10.1016/j.bmcl.2008.10.080  PMID:18990570
    • Feng, Y. B., Yin, Y., Weiser, A., Griffin, E., Cameron, M. D., Lin, L., Ruiz, C., Schurer, S. C., Inoue, T., Rao, P. V., Schroter, T., LoGrasso, P. Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors Journal of Medicinal Chemistry  2008 51:6642-6645  DOI:10.1021/jm800986w  PMID:18834107  PMCID:PMC3708311
    • Schroter, T., Griffin, E., Weiser, A., Feng, Y. B., LoGrasso, P. Detection of myosin light chain phosphorylation - a cell-based assay for screening rho-kinase inhibitors Biochemical and Biophysical Research Communications  2008 374:356-360  DOI:10.1016/j.bbrc.2008.07.028  PMID:18638453
    • Ember, B., LoGrasso, P. Mechanistic characterization for c-jun-n-terminal kinase 1 alpha 1 Archives of Biochemistry and Biophysics  2008 477:324-329  DOI:10.1016/j.abb.2008.06.001  PMID:18559253
    • LoGrasso, P., Kamenecka, T. Inhibitors of c-jun-n-terminal kinase (jnk) Mini-Reviews in Medicinal Chemistry  2008 8:755-766  DOI:10.2174/138955708784912120  PMID:18673131
    • Ember, B., Kamenecka, T., LoGrasso, P. Kinetic mechanism and inhibitor characterization for c-jun-N-terminal kinase 3 alpha 1 Biochemistry  2008 47:3076-3084  DOI:10.1021/bi701852z  PMID:18269248
    • Schroeter, T., Minond, D., Weiser, A., Dao, C., Habel, J., Spicer, T., Chase, P., Baillargeon, P., Scampavia, L., Schuerer, S., Chung, C., Mader, C., et al. Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of Rho-kinase II (ROCK-II) Journal of Biomolecular Screening  2008 13:17-28  DOI:10.1177/1087057107310806  PMID:18227223
    • Jiang, R., Duckett, D., Chen, W., Habel, J., Ling, Y. Y., LoGrasso, P., Kamenecka, T. M. 3,5-disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors Bioorganic & Medicinal Chemistry Letters  2007 17:6378-6382  DOI:10.1016/j.bmcl.2007.08.054  PMID:17911023
    • Feng, Y. B., Cameron, M. D., Frackowiak, B., Griffin, E., Lin, L., Ruiz, C., Schroter, T., LoGrasso, P. Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II Bioorganic & Medicinal Chemistry Letters  2007 17:2355-2360  DOI:10.1016/j.bmcl.2006.12.043  PMID:17368019
    • Rech, J. C., Yato, M., Duckett, D., Ember, B., LoGrasso, P. V., Bergman, R. G., Ellman, J. A. Synthesis of potent bicyclic bisarylimidazole c-jun N-terminal kinase inhibitors by catalytic C-H bond activation Journal of the American Chemical Society  2007 129:490-491  DOI:10.1021/ja0676004  PMID:17227002  PMCID:PMC2556147
    • Zhang, W. X., Wang, R. X., Wisniewski, D., Marcy, A. I., LoGrasso, P., Lisnock, J. M., Cummings, R. T., Thompson, J. E. Time-resolved Förster resonance energy transfer assays for the binding of nucleotide and protein substrates to p38 alpha protein kinase Analytical Biochemistry  2005 343:76-83  DOI:10.1016/j.ab.2005.05.011  PMID:15979553
    • Fricker, M., LoGrasso, P., Ellis, S., Wilkie, N., Hunt, P., Pollack, S. J. Substituting c-jun n-terminal kinase-3 (jnk3) atp-binding site amino acid residues with their p38 counterparts affects binding of jnk- and p38-selective inhibitors Archives of Biochemistry and Biophysics  2005 438:195-205  DOI:10.1016/j.abb.2005.04.013  PMID:15907786
    • LoGrasso, P., McKelvy, J. Advances in pain therapeutics Current Opinion in Chemical Biology  2003 7:452-456  DOI:10.1016/s1367-5931(03)00078-4  PMID:12941418
    • Scapin, G., Patel, S. B., Lisnock, J., Becker, J. W., LoGrasso, P. V. The structure of jnk3 in complex with small molecule inhibitors: Structural basis for potency and selectivity Chemistry & Biology  2003 10:705-712  DOI:10.1016/s1074-5521(03)00159-5  PMID:12954329
    • Trauger, J. W., Jiang, A., Stearns, B. A., LoGrasso, P. V. Kinetics of allopregnanolone formation catalyzed by human 3 alpha-hydroxysteroid dehydrogenase type iii (akrlc2) Biochemistry  2002 41:13451-13459  DOI:10.1021/bi026109w  PMID:12416991
    • Turner, M. S., Lin, F. F., Trauger, J. W., Stephens, J., LoGrasso, P. Characterization and purification of truncated human rho-kinase ii expressed in sf-21 cells Archives of Biochemistry and Biophysics  2002 405:13-20  DOI:10.1016/s0003-9861(02)00249-7  PMID:12176052
    • Trauger, J. W., Lin, F. F., Turner, M. S., Stephens, J., LoGrasso, P. V. Kinetic mechanism for human rho-kinase ii (rock-ii) Biochemistry  2002 41:8948-8953  DOI:10.1021/bi0258243  PMID:12102637
    • Harper, S. J., LoGrasso, P. Inhibitors of the JNK signaling pathway Drugs of the Future  2001 26:957-973  DOI:10.1358/dof.2001.026.10.858715
    • Harper, S. J., LoGrasso, P. Signalling for survival and death in neurones - the role of stress-activated kinases, jnk and p38 Cellular Signalling  2001 13:299-310  DOI:10.1016/s0898-6568(01)00148-6  PMID:11369511
    • Hawkins, J., Zheng, S., Frantz, B., LoGrasso, P. P38 map kinase substrate specificity differs greatly for protein and peptide substrates Archives of Biochemistry and Biophysics  2000 382:310-313  DOI:10.1006/abbi.2000.2005  PMID:11068883
    • Lisnock, J., Griffin, P., Calaycay, J., Frantz, B., Parsons, J., O'Keefe, S. J., LoGrasso, P. Activation of JNK3 alpha 1 requires both MKK4 and MKK7: Kinetic characterization of in vitro phosphorylated JNK3 alpha 1 Biochemistry  2000 39:3141-3148  DOI:10.1021/bi992410+  PMID:10715136
    • Wisniewski, D., LoGrasso, P., Calaycay, J., Marcy, A. Assay for i kappa b kinases using an in vivo biotinylated i kappa b protein substrate Analytical Biochemistry  1999 274:220-228  DOI:10.1006/abio.1999.4287  PMID:10527519
    • Xue, S., Green, M. A., LoGrasso, P. V., Boettcher, B. R., Madison, E. L., Curtiss, L. K., Miles, L. A. Comparison of the effects of apo(a) kringle IV-10 and plasminogen kringles on the interactions of lipoprotein(a) with regulatory molecules Thrombosis and Haemostasis  1999 81:428-435  PMID:10102473
    • Lisnock, J. M., Tebben, A., Frantz, B., O'Neill, E. A., Croft, G., O'Keefe, S. J., Li, B., Hacker, C., de Laszlo, S., Smith, A., Libby, B., Liverton, N., et al. Molecular basis for p38 protein kinase inhibitor specificity Biochemistry  1998 37:16573-16581  DOI:10.1021/bi981591x  PMID:9843424
    • LoGrasso, P. V., Frantz, B., Rolando, A. M., Okeefe, S. J., Hermes, J. D., Oneill, E. A. Kinetic mechanism for p38 map kinase Biochemistry  1997 36:10422-10427  DOI:10.1021/bi9706778  PMID:9265622
    • LoGrasso, P. V., Hawkins, J., Frank, L. J., Wisniewski, D., Marcy, A. Mechanism of activation for zap-70 catalytic activity Proceedings of the National Academy of Sciences of the United States of America  1996 93:12165-12170  DOI:10.1073/pnas.93.22.12165  PMID:8901551
    • Mikol, V., LoGrasso, P. V., Boettcher, B. R. Crystal structures of apolipoprotein(a) kringle iv37 free and complexed with 6-aminohexanoic acid and with p-aminomethylbenzoic acid: Existence of novel and expected binding modes Journal of Molecular Biology  1996 256:751-761  DOI:10.1006/jmbi.1996.0122  PMID:8642595
    • Tu, C. K., Chen, X., Ren, X. L., Lograsso, P. V., Jewell, D. A., Laipis, P. J., Silverman, D. N. Interactions of active-site residues and catalytic activity of human carbonic anhydrase III Journal of Biological Chemistry  1994 269:23002-23006  PMID:8083199
    • Lograsso, P. V., Cornellkennon, S., Boettcher, B. R. Comparison of the inhibition of yeast, rat, and human squalene synthetase Bioorganic Chemistry  1994 22:294-299  DOI:10.1006/bioo.1994.1023
    • Lograsso, P. V., Cornellhennon, S., Boettcher, B. R. Cloning, expression, and characterization of human apolipoprotein(a) kringle iv37 Journal of Biological Chemistry  1994 269:21820-21827  PMID:8063825
    • Lograsso, P. V., Soltis, D. A., Boettcher, B. R. Overexpression, purification, and kinetic characterization of a carboxyl-terminal-truncated yeast squalene synthetase Archives of Biochemistry and Biophysics  1993 307:193-199  DOI:10.1006/abbi.1993.1578  PMID:8239656
    • Chen, X., Tu, C. K., Lograsso, P. V., Laipis, P. J., Silverman, D. N. Interaction and influence of phenylalanine-198 and threonine-199 on catalysis by human carbonic anhydrase III Biochemistry  1993 32:7861-7865  DOI:10.1021/bi00082a004  PMID:8347590
    • Lograsso, P. V., Tu, C. K., Chen, X., Taoka, S. C., Laipis, P. J., Silverman, D. N. Influence of amino acid replacement at position 198 on catalytic properties of zinc-bound water in human carbonic anhydrase III Biochemistry  1993 32:5786-5791  DOI:10.1021/bi00073a010  PMID:8504098
    • Lograsso, P. V., Tu, C. K., Jewell, D. A., Wynns, G. C., Laipis, P. J., Silverman, D. N. Catalytic enhancement of human carbonic anhydrase III by replacement of phenylalanine-198 with leucine Biochemistry  1991 30:8463-8470  DOI:10.1021/bi00098a025  PMID:1909176
    • Jewell, D. A., Tu, C. K., Paranawithana, S. R., Tanhauser, S. M., Lograsso, P. V., Laipis, P. J., Silverman, D. N. Enhancement of the catalytic properties of human carbonic anhydrase-iii by site-directed mutagenesis Biochemistry  1991 30:1484-1490  DOI:10.1021/bi00220a006  PMID:1899618
    • Tu, C. K., Paranawithana, S. R., Jewell, D. A., Tanhauser, S. M., Lograsso, P. V., Wynns, G. C., Laipis, P. J., Silverman, D. N. Buffer enhancement of proton-transfer in catalysis by human carbonic anhydrase-iii Biochemistry  1990 29:6400-6405  DOI:10.1021/bi00479a009  PMID:2169869
    • Lograsso, P. V., Nicholson, L. K., Cross, T. A. N-h bond length determinations and implications for the gramicidin channel conformation and dynamics from n-15-h-1 dipolar interactions Journal of the American Chemical Society  1989 111:1910-1912  DOI:10.1021/ja00187a072
    • Nicholson, L. K., Lograsso, P. V., Cross, T. A. Experimental-observation of orientational dispersion in the peptide backbone of the gramicidin cation channel Journal of the American Chemical Society  1989 111:400-401  DOI:10.1021/ja00183a077
    • Lograsso, P. V., Moll, F., Cross, T. A. Solvent history dependence of gramicidin-a conformations in hydrated lipid bilayers Biophysical Journal  1988 54:259-267  DOI:10.1016/S0006-3495(88)82955-2  PMID:2462923  PMCID:PMC1330292
    • Nicholson, L. K., Moll, F., Mixon, T. E., Lograsso, P. V., Lay, J. C., Cross, T. A. Solid-state n-15 NMR of oriented lipid bilayer bound gramicidin a' Biochemistry  1987 26:6621-6626  DOI:10.1021/bi00395a009  PMID:2447939

featured in

  • A Sense of Balance: The Scripps Research LoGrasso Lab Develops the First New Class of Potential Therapies for Neurodegenerative Disease to Pass the Blood-Brain Barrier  News Release
  • Medicine Man: Philip LoGrasso Targets Drug Discovery  Newsletter
  • Scripps Florida Forms Molecular Therapeutics Department  Newsletter
  • Scripps Florida Scientist Wins $1 Million Grant to Develop New Tests That Could Lead to New Therapeutics for Alzheimer’s, Parkinson’s Disease  News Release
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Research

research overview

  • The major focus of our research effort is the study of structure function relationships of enzymes (kinases, protease, dehydrogenases) and how this relates to drug discovery of enzyme inhibitors. Of particular current interest is the MAP kinase family member c-jun-N-terminal kinase 3 (JNK3). JNK3 has been shown to play a significant role in neuronal survival and is a viable target for developing drugs to treat neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and stroke. Another kinase that we have interest in is Rho-kinase (ROCK). ROCK is involved in smooth-muscle contraction and has been shown to have therapeutic potential in conditions ranging from angina to spinal cord injury. We utilize molecular biology, protein chemistry, enzymology, cell biology, and structure-based drug design to achieve these goals. A third focus of the lab is in the area of chemical biology. Here we are interested in discovering molecular targets for molecules that have been shown to have activity in anxiety, cancer, and infectious disease.
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Background

education and training

  • Ph.D. in Pharmacology, University of Florida 1992
  • M.S. in Biochemistry, The Florida State University 1988
  • B.A. in Chemistry, New York University 1985
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Contact

full name

  • Philip V. LoGrasso

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