Marcelo G Kazanietz

Summary

Affiliation: University of Pennsylvania
Country: USA

Publications

  1. ncbi Pharmacology of the receptors for the phorbol ester tumor promoters: multiple receptors with different biochemical properties
    M G Kazanietz
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, 19104 6160, USA
    Biochem Pharmacol 60:1417-24. 2000
  2. ncbi Targeting protein kinase C and "non-kinase" phorbol ester receptors: emerging concepts and therapeutic implications
    Marcelo G Kazanietz
    Department of Pharmacology, University of Pennsylvania School of Medicine, 816 Biomedical Research Building II III, 421 Curie Blvd, Philadelphia, PA 19104 6160, USA
    Biochim Biophys Acta 1754:296-304. 2005
  3. ncbi Protein kinase C and prostate carcinogenesis: targeting the cell cycle and apoptotic mechanisms
    M Veronica Gavrielides
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Curr Drug Targets 5:431-43. 2004
  4. ncbi Novel "nonkinase" phorbol ester receptors: the C1 domain connection
    Marcelo G Kazanietz
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Mol Pharmacol 61:759-67. 2002
  5. pmc A novel cross-talk in diacylglycerol signaling: the Rac-GAP beta2-chimaerin is negatively regulated by protein kinase Cdelta-mediated phosphorylation
    Erin M Griner
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 285:16931-41. 2010
  6. pmc Phospholipase Cgamma/diacylglycerol-dependent activation of beta2-chimaerin restricts EGF-induced Rac signaling
    HongBin Wang
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160, USA
    EMBO J 25:2062-74. 2006
  7. ncbi Protein kinase C promotes apoptosis in LNCaP prostate cancer cells through activation of p38 MAPK and inhibition of the Akt survival pathway
    Yuichi Tanaka
    Center for Experimental Therapeutics and Department of Pharmacology, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 278:33753-62. 2003
  8. ncbi S-Phase-specific activation of PKC alpha induces senescence in non-small cell lung cancer cells
    Jose L Oliva
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 283:5466-76. 2008
  9. ncbi Rac-GAP-dependent inhibition of breast cancer cell proliferation by {beta}2-chimerin
    Chengfeng Yang
    Department of Pharmacology, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 280:24363-70. 2005
  10. pmc Coordinated activation of the Rac-GAP β2-chimaerin by an atypical proline-rich domain and diacylglycerol
    Alvaro Gutiérrez-Uzquiza
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6160, USA
    Nat Commun 4:1849. 2013

Collaborators

Detail Information

Publications60

  1. ncbi Pharmacology of the receptors for the phorbol ester tumor promoters: multiple receptors with different biochemical properties
    M G Kazanietz
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, 19104 6160, USA
    Biochem Pharmacol 60:1417-24. 2000
    ..The differential pharmacological properties of the phorbol ester receptors can be exploited to generate specific agonists and antagonists that will be helpful tools to dissect their cellular function...
  2. ncbi Targeting protein kinase C and "non-kinase" phorbol ester receptors: emerging concepts and therapeutic implications
    Marcelo G Kazanietz
    Department of Pharmacology, University of Pennsylvania School of Medicine, 816 Biomedical Research Building II III, 421 Curie Blvd, Philadelphia, PA 19104 6160, USA
    Biochim Biophys Acta 1754:296-304. 2005
    ..The discovery of the chimaerins and other "non-kinase" phorbol ester receptors has major implications in the design of agents for cancer therapy...
  3. ncbi Protein kinase C and prostate carcinogenesis: targeting the cell cycle and apoptotic mechanisms
    M Veronica Gavrielides
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Curr Drug Targets 5:431-43. 2004
    ....
  4. ncbi Novel "nonkinase" phorbol ester receptors: the C1 domain connection
    Marcelo G Kazanietz
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Mol Pharmacol 61:759-67. 2002
    ..Alternative pharmacological and molecular approaches are therefore needed to dissect the involvement of each receptor class as a mediator of phorbol ester/DAG responses...
  5. pmc A novel cross-talk in diacylglycerol signaling: the Rac-GAP beta2-chimaerin is negatively regulated by protein kinase Cdelta-mediated phosphorylation
    Erin M Griner
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 285:16931-41. 2010
    ....
  6. pmc Phospholipase Cgamma/diacylglycerol-dependent activation of beta2-chimaerin restricts EGF-induced Rac signaling
    HongBin Wang
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160, USA
    EMBO J 25:2062-74. 2006
    ..Our results represent the first direct evidence of divergence in DAG signaling downstream of a tyrosine-kinase receptor via a PKC-independent mechanism...
  7. ncbi Protein kinase C promotes apoptosis in LNCaP prostate cancer cells through activation of p38 MAPK and inhibition of the Akt survival pathway
    Yuichi Tanaka
    Center for Experimental Therapeutics and Department of Pharmacology, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 278:33753-62. 2003
    ....
  8. ncbi S-Phase-specific activation of PKC alpha induces senescence in non-small cell lung cancer cells
    Jose L Oliva
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 283:5466-76. 2008
    ....
  9. ncbi Rac-GAP-dependent inhibition of breast cancer cell proliferation by {beta}2-chimerin
    Chengfeng Yang
    Department of Pharmacology, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 280:24363-70. 2005
    ....
  10. pmc Coordinated activation of the Rac-GAP β2-chimaerin by an atypical proline-rich domain and diacylglycerol
    Alvaro Gutiérrez-Uzquiza
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6160, USA
    Nat Commun 4:1849. 2013
    ..Our studies underscore a coordinated mechanism for β2-chimaerin activation that involves lipid interactions via the C1 domain and protein-protein interactions via the N-terminal proline-rich region...
  11. ncbi Heregulin beta1 promotes breast cancer cell proliferation through Rac/ERK-dependent induction of cyclin D1 and p21Cip1
    Chengfeng Yang
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics, University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA
    Biochem J 410:167-75. 2008
    ..Taken together, these findings establish a central role for Rac1 in the control of HRG-induced breast cancer cell-cycle progression and proliferation through up-regulating the expression of cyclin D1 and p21(Cip1)...
  12. pmc Identification of an autoinhibitory mechanism that restricts C1 domain-mediated activation of the Rac-GAP alpha2-chimaerin
    Francheska Colon-Gonzalez
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics ITMAT, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 283:35247-57. 2008
    ..Like other DAG/phorbol ester receptors, including protein kinase C isozymes, alpha2-chimaerin is subject to autoinhibition by intramolecular contacts, suggesting a highly regulated mechanism for the activation of this Rac-GAP...
  13. pmc Non-small cell lung carcinoma cell motility, rac activation and metastatic dissemination are mediated by protein kinase C epsilon
    M Cecilia Caino
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, United States of America
    PLoS ONE 7:e31714. 2012
    ..The role of PKCε in lung cancer metastasis has not yet been established...
  14. pmc Essential role for Rac in heregulin beta1 mitogenic signaling: a mechanism that involves epidermal growth factor receptor and is independent of ErbB4
    Chengfeng Yang
    Department of Pharmacology, University of Pennsylvania School of Medicine, 816 Biomedical Research Building II III, 421 Curie Blvd, Philadelphia, PA 19104 6160, USA
    Mol Cell Biol 26:831-42. 2006
    ....
  15. pmc p23/Tmp21 differentially targets the Rac-GAP beta2-chimaerin and protein kinase C via their C1 domains
    HongBin Wang
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160
    Mol Biol Cell 21:1398-408. 2010
    ..Our study also highlights the relevance of C1 domains in protein-protein interactions in addition to their well-established lipid-binding properties...
  16. pmc ROCK mediates phorbol ester-induced apoptosis in prostate cancer cells via p21Cip1 up-regulation and JNK
    Liqing Xiao
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 284:29365-75. 2009
    ..Taken together, our studies implicate ROCK-mediated up-regulation of p21(Cip1) and the cytoskeleton in PKCdelta-dependent apoptosis in prostate cancer cells...
  17. pmc p23/Tmp21 associates with protein kinase Cdelta (PKCdelta) and modulates its apoptotic function
    HongBin Wang
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 286:15821-31. 2011
    ....
  18. pmc Regulation of prostate cancer cell survival by protein kinase Cepsilon involves bad phosphorylation and modulation of the TNFalpha/JNK pathway
    John Meshki
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 285:26033-40. 2010
    ..Our results established that PKCepsilon modulates survival in prostate cancer cells via multiple pathways...
  19. pmc PKC-mediated secretion of death factors in LNCaP prostate cancer cells is regulated by androgens
    Liqing Xiao
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Mol Carcinog 48:187-95. 2009
    ....
  20. pmc Biochemical characterization of hyperactive beta2-chimaerin mutants revealed an enhanced exposure of C1 and Rac-GAP domains
    Maria Soledad Sosa
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    Biochemistry 48:8171-8. 2009
    ..These studies suggest that beta2-chimaerin must undergo a conformational rearrangement in order to expose its lipid binding sites and become activated...
  21. pmc Bryostatin 1 inhibits phorbol ester-induced apoptosis in prostate cancer cells by differentially modulating protein kinase C (PKC) delta translocation and preventing PKCdelta-mediated release of tumor necrosis factor-alpha
    Vivian A von Burstin
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Mol Pharmacol 78:325-32. 2010
    ..The identification of an antiapoptotic effect of bryostatin 1 may have significant relevance in the context of its therapeutic efficacy...
  22. ncbi C1 domains exposed: from diacylglycerol binding to protein-protein interactions
    Francheska Colon-Gonzalez
    Department of Pharmacology, University of Pennsylvania School of Medicine, 816 Biomedical Research Building II III, 421 Curie Blvd, Philadelphia, PA 19104 6160, USA
    Biochim Biophys Acta 1761:827-37. 2006
    ..Thus, it is clear that the protein context plays a major role in determining whether binding of DAG to the C1 domain would lead to enzyme activation or merely serves as an anchoring mechanism...
  23. doi Phorbol ester-induced apoptosis and senescence in cancer cell models
    Liqing Xiao
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics ITMAT, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania, USA
    Methods Enzymol 446:123-39. 2008
    ..This chapter describes the methods we use to assess these phorbol ester responses in cancer cell models, focusing on apoptosis and senescence...
  24. ncbi Benzo[a]pyrene-7,8-dihydrodiol promotes checkpoint activation and G2/M arrest in human bronchoalveolar carcinoma H358 cells
    M Cecilia Caino
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160, USA
    Mol Pharmacol 71:744-50. 2007
    ..Our data suggest that a p53-independent pathway operates in lung epithelial cells in response to BPD that involves P450 induction and subsequent activation of the ATR/ATM/Chk1 damage check-point pathway and cell cycle arrest in G2/M...
  25. ncbi Androgens regulate protein kinase Cdelta transcription and modulate its apoptotic function in prostate cancer cells
    M Veronica Gavrielides
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    Cancer Res 66:11792-801. 2006
    ..Our studies identified a novel hormonal mechanism for the control of PKCdelta expression via transcriptional regulation that fine-tunes the magnitude of PKCdelta apoptotic responses...
  26. ncbi Protein kinase C delta stimulates apoptosis by initiating G1 phase cell cycle progression and S phase arrest
    Ademi E Santiago-Walker
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, 19104 6061, USA
    J Biol Chem 280:32107-14. 2005
    ..Importantly, they reveal the existence of a novel, cell cycle-dependent mechanism through which PKCdelta stimulates cell death...
  27. ncbi Phorbol ester-induced G1 phase arrest selectively mediated by protein kinase Cdelta-dependent induction of p21
    Motonori Nakagawa
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 280:33926-34. 2005
    ..Our results identify a novel link between PKCdelta and G1 arrest via p21 up-regulation and highlight the complexities in the downstream effectors of PKC isozymes in the context of cell cycle progression and proliferation...
  28. pmc Cucurbitacin I inhibits Rac1 activation in breast cancer cells by a reactive oxygen species-mediated mechanism and independently of Janus tyrosine kinase 2 and P-Rex1
    Cynthia Lopez-Haber
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6160, USA
    Mol Pharmacol 83:1141-54. 2013
    ..Moreover, they established that the inhibitory effect of cucurbitacin I on Rac1 activity involves the alteration of the balance between Rho and Rac...
  29. ncbi Protein kinase C and other diacylglycerol effectors in cancer
    Erin M Griner
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics ITMAT, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    Nat Rev Cancer 7:281-94. 2007
    ....
  30. pmc Characterization of the Rac-GAP (Rac-GTPase-activating protein) activity of beta2-chimaerin, a 'non-protein kinase C' phorbol ester receptor
    Maria Jose Caloca
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, 421 Curie Boulevard, Philadelphia, PA 19104 6160, USA
    Biochem J 375:313-21. 2003
    ..These results strongly emphasize the high complexity of DAG signalling due to the activation of PKC-independent pathways, and cast doubts regarding the selectivity of phorbol esters and DAG analogues as selective PKC activators...
  31. ncbi PKC isozymes and diacylglycerol-regulated proteins as effectors of growth factor receptors
    Jose Luis Oliva
    School of Medicine, University of Pennsylvania, Department of Pharmacology, Philadelphia, PA 19104 6160, USA
    Growth Factors 23:245-52. 2005
    ..Moreover, the identification of novel "non-kinase" DAG-binding proteins has added a new level of complexity to the field of DAG signaling...
  32. pmc Rac signaling in breast cancer: a tale of GEFs and GAPs
    Eva Wertheimer
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104 6160, USA
    Cell Signal 24:353-62. 2012
    ..Most notably, P-Rex1 is highly overexpressed in human luminal breast tumors, particularly those expressing ErbB2 and estrogen receptor (ER). The P-Rex1/Rac signaling pathway may represent an attractive target for breast cancer therapy...
  33. pmc Differential regulation of gene expression by protein kinase C isozymes as determined by genome-wide expression analysis
    M Cecilia Caino
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    J Biol Chem 286:11254-64. 2011
    ..Our studies offer a unique opportunity for establishing novel transcriptional effectors for PKC isozymes and may have significant functional and therapeutic implications...
  34. ncbi Regulation of the neuronal glutamate transporter excitatory amino acid carrier-1 (EAAC1) by different protein kinase C subtypes
    Marco I Gonzalez
    Department of Pediatrics and Pharmacology, Children s Hospital of Philadelphia, University of Pennsylvania, Philadelphia, Pennsylvania, USA
    Mol Pharmacol 62:901-10. 2002
    ..The potential relationship of the present work with a previously identified role for PKCalpha in certain forms of synaptic plasticity is discussed...
  35. pmc Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells
    Brian C DiPaolo
    Department of Bioengineering, School of Engineering and Applied Science, University of Pennsylvania, Philadelphia, PA 19104, USA
    Am J Physiol Lung Cell Mol Physiol 305:L141-53. 2013
    ..In summary, our data suggest that constitutive activity of Rac1, which is necessary for stretch-induced activation of the Rac1 downstream proteins, mediates stretch-induced increases in permeability and PJAR formation. ..
  36. pmc The zebrafish homologue of mammalian chimerin Rac-GAPs is implicated in epiboly progression during development
    Federico Coluccio Leskow
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160, USA
    Proc Natl Acad Sci U S A 103:5373-8. 2006
    ..Our results reveal a crucial role for chn1 in early development and implicate Rac as a key regulator of morphogenetic movements during zebrafish epiboly...
  37. ncbi Phorbol ester-induced apoptosis in prostate cancer cells via autocrine activation of the extrinsic apoptotic cascade: a key role for protein kinase C delta
    Anatilde M Gonzalez-Guerrico
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 280:38982-91. 2005
    ..Taken together, our results demonstrate that activation of PKCdelta in prostate cancer cells causes apoptosis via the release of death receptor ligands and the activation of the extrinsic apoptotic cascade...
  38. ncbi Phorbol esters as probes for the study of protein kinase C function
    Marcelo G Kazanietz
    Center for Experimental Therapeutics, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, USA
    Methods Mol Biol 233:423-39. 2003
  39. ncbi Chimaerins: GAPs that bridge diacylglycerol signalling and the small G-protein Rac
    Chengfeng Yang
    Department of Pharmacology and Institute for Translational Medicine and Therapeutics, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160, USA
    Biochem J 403:1-12. 2007
    ..In addition, vigorous recent studies have begun to decipher the critical roles of chimaerins in the central nervous system, development and tumour progression...
  40. pmc Activation of nuclear factor κB (NF-κB) in prostate cancer is mediated by protein kinase C epsilon (PKCepsilon)
    Rachana Garg
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Biol Chem 287:37570-82. 2012
    ..Our studies identified a molecular link between PKCε and NF-κB that controls key responses implicated in prostate cancer progression...
  41. doi Rho GEFs and cancer: linking gene expression and metastatic dissemination
    Laura Barrio-Real
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA
    Sci Signal 5:pe43. 2012
    ....
  42. ncbi Lysophosphatidic acid promotes survival and differentiation of rat Schwann cells
    Yiwen Li
    Department of Neurology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
    J Biol Chem 278:9585-91. 2003
    ..Thus, the multiple effects of LPA in Schwann cells (actin reorganization, survival, and myelin gene expression) appear to be mediated through the different G protein-dependent pathways activated by the LPA receptor...
  43. ncbi Hedgehog proteins activate pro-angiogenic responses in endothelial cells through non-canonical signaling pathways
    Pilar Chinchilla
    Department of Biochemistry and Molecular Biology, Thomas Jefferson University, Philadelphia, PA, USA
    Cell Cycle 9:570-79. 2010
    ..of novel non-canonical responses elicited by Hh proteins in endothelial cells highlights the complexity of the Hh signaling pathway and reveals striking differences in ligand strength for transcriptional and non-transcriptional responses..
  44. ncbi Polycyclic aromatic hydrocarbon o-quinones inhibit the activity of the catalytic fragment of protein kinase C
    Deshan Yu
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6084, USA
    Biochemistry 41:11888-94. 2002
    ..These data suggest that PAH o-quinones, generated by AKRs, may affect cellular signaling through suppression of the activity of PKC isoforms...
  45. ncbi Chimaerins, novel non-protein kinase C phorbol ester receptors, associate with Tmp21-I (p23): evidence for a novel anchoring mechanism involving the chimaerin C1 domain
    HongBin Wang
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 277:4541-50. 2002
    ..In this setting, Tmp21-I serves as an anchoring protein that determines the intracellular localization of these novel phorbol ester receptors...
  46. ncbi Pharmacological probes for protein kinase C: an introduction
    Marcelo G Kazanietz
    Center for Experimental Therapeutics, Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, USA
    Methods Mol Biol 233:389-95. 2003
  47. ncbi Divergence and complexities in DAG signaling: looking beyond PKC
    Chengfeng Yang
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 6160, USA
    Trends Pharmacol Sci 24:602-8. 2003
    ....
  48. ncbi Post-transcriptional destabilization of p21cip1 by protein kinase C in fibroblasts
    Janice L Walker
    Department of Pharmacology, University of Pennsylvania School of Medicine, 3620 Hamilton Walk, Philadelphia, PA 19104 6084, USA
    J Biol Chem 281:38127-32. 2006
    ..Thus, post-transcriptional destabilization of p21(cip1) appears to be a major mitogenic effect of PKCdelta in fibroblasts...
  49. ncbi Diacylglycerol (DAG)-lactones, a new class of protein kinase C (PKC) agonists, induce apoptosis in LNCaP prostate cancer cells by selective activation of PKCalpha
    Maria Laura Garcia-Bermejo
    Center for Experimental Therapeutics and Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6160, USA
    J Biol Chem 277:645-55. 2002
    ..An attractive hypothesis is that selective activation of PKC isozymes by pharmacological agents in cells can be achieved by differential intracellular targeting of each PKC...
  50. ncbi NFkappaB-independent signaling to the cyclin D1 gene by Rac
    Eric A Klein
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania, USA
    Cell Cycle 6:1115-21. 2007
    ..We conclude that, in MEFs, Rac-mediated induction of cyclin D1 mRNA requires activation of a parallel NFkappaB pathway whereas ERK induces cyclin D1 transcription independent of NFkappaB...
  51. pmc Identification of the Rac-GEF P-Rex1 as an essential mediator of ErbB signaling in breast cancer
    Maria Soledad Sosa
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA
    Mol Cell 40:877-92. 2010
    ..In addition to the prognostic and therapeutic implications, our findings reveal an ErbB effector pathway that is crucial for breast cancer progression...
  52. pmc Characterization of a P-Rex1 gene signature in breast cancer cells
    Laura Barrio-Real
    Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, USA
    Oncotarget . 2016
    ..Notably, there is a significant association in the expression of P-Rex1 and MMP10 in human luminal breast cancer, and their co-expression is indicative of poor prognosis...
  53. ncbi The P-Rex1/Rac signaling pathway as a point of convergence for HER/ErbB receptor and GPCR responses
    Marcelo G Kazanietz
    a Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA
    Small Gtpases . 2016
    ..We propose a model in which P-Rex1 acts as a crucial node for the integration of upstream inputs from HER/ErbB receptors and CXCR4 in luminal breast cancer cells...
  54. pmc Phospholipase cbeta is critical for T cell chemotaxis
    Tami L Bach
    Department of Medicine, Abramson Family Cancer Research Institute, Philadelphia, PA, USA
    J Immunol 179:2223-7. 2007
    ..This study demonstrates that, in contrast to neutrophils, phospholipid second messengers generated by PLCbeta play a critical role in T lymphocyte chemotaxis...
  55. ncbi Interaction of the novel anthracycline antitumor agent N-benzyladriamycin-14-valerate with the C1-regulatory domain of protein kinase C: structural requirements, isoform specificity, and correlation with drug cytotoxicity
    J Brent Roaten
    Department of Pharmacology, University of Tennessee College of Medicine, Memphis, Tennessee 38163, USA
    Mol Cancer Ther 1:483-92. 2002
    ....
  56. ncbi alpha6beta4 integrin activates Rac-dependent p21-activated kinase 1 to drive NF-kappaB-dependent resistance to apoptosis in 3D mammary acini
    Julie C Friedland
    Department of Pharmacology, University of Pennsylvania, Philadelphia, PA 19104, USA
    J Cell Sci 120:3700-12. 2007
    ....
  57. doi Hallmarks for senescence in carcinogenesis: novel signaling players
    M Cecilia Caino
    Department of Pharmacology, School of Medicine, University of Pennsylvania, Philadelphia, PA 19104 6160, USA
    Apoptosis 14:392-408. 2009
    ..These novel findings suggest a complex array of cross-talks between senescence pathways and may have significant implications in cancer therapy...
  58. pmc Heregulin/ErbB3 Signaling Enhances CXCR4-Driven Rac1 Activation and Breast Cancer Cell Motility via Hypoxia-Inducible Factor 1α
    Cynthia Lopez-Haber
    Department of Systems Pharmacology and Translational Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA
    Mol Cell Biol 36:2011-26. 2016
    ..Our results uncovered a novel function for ErbB3 in enhancing breast cancer cell motility and sensitization of the P-Rex1/Rac1 pathway through HIF-1α-mediated transcriptional induction of CXCR4. ..
  59. pmc A host GPCR signaling network required for the cytolysis of infected cells facilitates release of apicomplexan parasites
    Melanie G Millholland
    Department of Pharmacology, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA
    Cell Host Microbe 13:15-28. 2013
    ..Importantly, an orally bioavailable PKC inhibitor prolonged survival in an experimental cerebral malaria model...
  60. doi Protein kinase C regulation: C1 meets C-tail
    Marcelo G Kazanietz
    Department of Pharmacology, University of Pennsylvania School of Medicine, Philadelphia, PA, USA
    Structure 19:144-6. 2011
    ..2011) describe the structure of PKCβII, an AGC kinase, revealing an unanticipated intramolecular autoinhibitory interaction between its C-terminal tail and the diacylglycerol and phorbol ester binding site of its C1b domain...