Gideon Bollag

Summary

Publications

  1. ncbi request reprint Raf pathway inhibitors in oncology
    Gideon Bollag
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Curr Opin Investig Drugs 4:1436-41. 2003
  2. doi request reprint Vemurafenib: the first drug approved for BRAF-mutant cancer
    Gideon Bollag
    Plexxikon, 91 Bolivar Drive, Berkeley, California 94710, USA
    Nat Rev Drug Discov 11:873-86. 2012
  3. doi request reprint Setting up a kinase discovery and development project
    Gideon Bollag
    Plexxikon Inc, Berkeley, CA 94710, USA
    Curr Top Microbiol Immunol 355:3-18. 2012
  4. pmc Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
    Gideon Bollag
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, California 94710, USA
    Nature 467:596-9. 2010
  5. pmc Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma
    William D Tap
    Division of Hematology Oncology, Department of Medicine, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA
    Neoplasia 12:637-49. 2010
  6. pmc Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor
    Chao Zhang
    Plexxikon Inc, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 110:5689-94. 2013
  7. pmc Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
    James Tsai
    Plexxikon, Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 105:3041-6. 2008
  8. doi request reprint Scaffold-based design of kinase inhibitors for cancer therapy
    Chao Zhang
    Plexxikon Inc, 91 Bolivar Dr, Berkeley, CA 94710, United States
    Curr Opin Genet Dev 20:79-86. 2010
  9. ncbi request reprint Phosphodiesterase-4 as a potential drug target
    Kam Y J Zhang
    Plexxikon, Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Expert Opin Ther Targets 9:1283-305. 2005
  10. pmc Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent
    Dean R Artis
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 106:262-7. 2009

Collaborators

Detail Information

Publications14

  1. ncbi request reprint Raf pathway inhibitors in oncology
    Gideon Bollag
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Curr Opin Investig Drugs 4:1436-41. 2003
    ..Indeed, the Raf inhibitor BAY-43-9006 recently entered phase III clinical trials. Here, we review the current development status of potential Raf pathway therapeutics...
  2. doi request reprint Vemurafenib: the first drug approved for BRAF-mutant cancer
    Gideon Bollag
    Plexxikon, 91 Bolivar Drive, Berkeley, California 94710, USA
    Nat Rev Drug Discov 11:873-86. 2012
    ..This Review describes the underlying biology of BRAF, the technology used to identify vemurafenib and its clinical development milestones, along with future prospects based on lessons learned during its development...
  3. doi request reprint Setting up a kinase discovery and development project
    Gideon Bollag
    Plexxikon Inc, Berkeley, CA 94710, USA
    Curr Top Microbiol Immunol 355:3-18. 2012
    ..This chapter will focus on some of the critical considerations in setting up a kinase discovery and development project, citing examples particularly targeting the Raf kinases...
  4. pmc Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma
    Gideon Bollag
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, California 94710, USA
    Nature 467:596-9. 2010
    ..These data demonstrate that BRAF-mutant melanomas are highly dependent on B-RAF kinase activity...
  5. pmc Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma
    William D Tap
    Division of Hematology Oncology, Department of Medicine, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA
    Neoplasia 12:637-49. 2010
    ..We sought to investigate the efficacy of PLX4032 (BRAF inhibitor) to identify patterns/predictors of response/resistance and to study the effects of BRAF in melanoma...
  6. pmc Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor
    Chao Zhang
    Plexxikon Inc, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 110:5689-94. 2013
    ..More importantly, the dual FMS and KIT inhibition profile has translated into a combination of benefits in preclinical disease models of inflammation and cancer...
  7. pmc Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity
    James Tsai
    Plexxikon, Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 105:3041-6. 2008
    ....
  8. doi request reprint Scaffold-based design of kinase inhibitors for cancer therapy
    Chao Zhang
    Plexxikon Inc, 91 Bolivar Dr, Berkeley, CA 94710, United States
    Curr Opin Genet Dev 20:79-86. 2010
    ..Here, we review such a paradigm termed scaffold-based design and show how implementation of these methods results in novel, potent, and specific drug candidates...
  9. ncbi request reprint Phosphodiesterase-4 as a potential drug target
    Kam Y J Zhang
    Plexxikon, Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Expert Opin Ther Targets 9:1283-305. 2005
    ..Finally, recent advances in the structural biology of PDE4 and their complexes with various inhibitors, as well as its potential impact on the rational design of potent and selective PDE4 inhibitors, are presented...
  10. pmc Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent
    Dean R Artis
    Plexxikon Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Proc Natl Acad Sci U S A 106:262-7. 2009
    ..Indeglitazar has now progressed to Phase II clinical evaluations for Type 2 diabetes mellitus (T2DM)...
  11. ncbi request reprint A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
    Graeme L Card
    Plexxikon Inc, 91 Bolivar Dr, Berkeley, California 94710, USA
    Nat Biotechnol 23:201-7. 2005
    ....
  12. ncbi request reprint Structural basis for the activity of drugs that inhibit phosphodiesterases
    Graeme L Card
    Plexxikon, Inc, 91 Bolivar Drive, Berkeley, CA 94710, USA
    Structure 12:2233-47. 2004
    ..These structural insights will enable the design of isoform-selective inhibitors with improved binding affinity and should facilitate the discovery of more potent and selective PDE inhibitors for the treatment of a variety of diseases...
  13. ncbi request reprint Hyperactive Ras in developmental disorders and cancer
    Suzanne Schubbert
    Department of Pediatrics, University of California, 513 Parnassus Avenue, Room HSE 302, San Francisco, California 94143, USA
    Nat Rev Cancer 7:295-308. 2007
    ..Here we will discuss the implications of germline mutations in the Ras-Raf-MEK-ERK pathway for understanding normal developmental processes and cancer pathogenesis...
  14. ncbi request reprint BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis
    Scott M Wilhelm
    Bayer Pharmaceuticals Corporation, West Haven, Connecticut 06516, USA
    Cancer Res 64:7099-109. 2004
    ..These data demonstrate that BAY 43-9006 is a novel dual action RAF kinase and VEGFR inhibitor that targets tumor cell proliferation and tumor angiogenesis...