Lianhong Xu

Summary

Affiliation: Gilead Sciences
Country: USA

Publications

  1. doi request reprint Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)
    Lianhong Xu
    Department of Medicinal Chemistry, Gilead Sciences, 333 Lakeside Drive, Foster City, CA 94303, USA Electronic address
    Bioorg Med Chem Lett 24:995-9. 2014
  2. ncbi request reprint Pharmacokinetic enhancers for HIV drugs
    Lianhong Xu
    Gilead Sciences Inc, Department of Medicinal Chemistry, 333 Lakeside Drive, Foster City, CA 94404, USA
    Curr Opin Investig Drugs 10:775-86. 2009
  3. doi request reprint SAR studies on dihydropyrimidinone antibiotics
    Lianhong Xu
    Gilead Sciences Inc, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 21:1670-4. 2011
  4. doi request reprint Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: core region
    Hongtao Liu
    Department of Medicinal Chemistry, Gilead Sciences, Foster City, CA, USA Electronic address
    Bioorg Med Chem Lett 24:989-94. 2014
  5. doi request reprint N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
    Michael L Mitchell
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 20:1585-8. 2010
  6. doi request reprint N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
    Michael L Mitchell
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 20:1589-92. 2010
  7. doi request reprint Synthesis and biological evaluation of phosphonate analogues of nevirapine
    Jay Parrish
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 23:1493-7. 2013
  8. pmc Mutations in multiple domains of Gag drive the emergence of in vitro resistance to the phosphonate-containing HIV-1 protease inhibitor GS-8374
    Kirsten M Stray
    Gilead Sciences, Inc, Foster City, California, USA
    J Virol 87:454-63. 2013
  9. pmc Characterization of a novel antibacterial agent that inhibits bacterial translation
    Nina Boddeker
    Gilead Sciences, Foster City, California 94404, USA
    RNA 8:1120-8. 2002
  10. pmc In vitro characterization of GS-8374, a novel phosphonate-containing inhibitor of HIV-1 protease with a favorable resistance profile
    Christian Callebaut
    Gilead Sciences, 333 Lakeside Dr, Foster City, CA 94404, USA
    Antimicrob Agents Chemother 55:1366-76. 2011

Collaborators

Detail Information

Publications12

  1. doi request reprint Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350)
    Lianhong Xu
    Department of Medicinal Chemistry, Gilead Sciences, 333 Lakeside Drive, Foster City, CA 94303, USA Electronic address
    Bioorg Med Chem Lett 24:995-9. 2014
    ..Through these efforts, a potent and selective inhibitor of CYP3A, GS-9350 (cobicistat) with improved physiochemical properties was discovered. ..
  2. ncbi request reprint Pharmacokinetic enhancers for HIV drugs
    Lianhong Xu
    Gilead Sciences Inc, Department of Medicinal Chemistry, 333 Lakeside Drive, Foster City, CA 94404, USA
    Curr Opin Investig Drugs 10:775-86. 2009
    ..This review summarizes salient features and limitations associated with the use of ritonavir as a PK enhancer, and briefly describes novel PK enhancers that are in development...
  3. doi request reprint SAR studies on dihydropyrimidinone antibiotics
    Lianhong Xu
    Gilead Sciences Inc, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 21:1670-4. 2011
    ..Several novel dihydropyrimidinone antibiotics demonstrating comparable antibiotic efficacy while possessing favorable selectivity were identified...
  4. doi request reprint Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: core region
    Hongtao Liu
    Department of Medicinal Chemistry, Gilead Sciences, Foster City, CA, USA Electronic address
    Bioorg Med Chem Lett 24:989-94. 2014
    ....
  5. doi request reprint N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
    Michael L Mitchell
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 20:1585-8. 2010
    ..Efforts to improve the suboptimal pharmacokinetic profile of 1 resulted in the discovery of compound 13, which represents the lead compound in this series with improved pharmacokinetics and similar potency as inhibitor 1...
  6. doi request reprint N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase
    Michael L Mitchell
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 20:1589-92. 2010
    ..Our efforts identified compound 10b, which represents the lead compound in this series with pharmacokinetics and antiviral potency that may support once-daily dosing...
  7. doi request reprint Synthesis and biological evaluation of phosphonate analogues of nevirapine
    Jay Parrish
    Gilead Sciences, Inc, 333 Lakeside Drive, Foster City, CA 94404, USA
    Bioorg Med Chem Lett 23:1493-7. 2013
    ..The effect of the phosphonate was evaluated against the wild type and Y181C HIV replication. An in vivo PK study was performed on a select analogue...
  8. pmc Mutations in multiple domains of Gag drive the emergence of in vitro resistance to the phosphonate-containing HIV-1 protease inhibitor GS-8374
    Kirsten M Stray
    Gilead Sciences, Inc, Foster City, California, USA
    J Virol 87:454-63. 2013
    ..These substrate changes were distributed throughout Gag and acted in an additive manner. Thus, they are classified as primary resistance mutations indicating a unique mechanism and pathway of resistance development for GS-8374...
  9. pmc Characterization of a novel antibacterial agent that inhibits bacterial translation
    Nina Boddeker
    Gilead Sciences, Foster City, California 94404, USA
    RNA 8:1120-8. 2002
    ..Selection and analysis of drug-resistant mutants of S. aureus suggests that drug uptake may be mediated by a dipeptide transport mechanism...
  10. pmc In vitro characterization of GS-8374, a novel phosphonate-containing inhibitor of HIV-1 protease with a favorable resistance profile
    Christian Callebaut
    Gilead Sciences, 333 Lakeside Dr, Foster City, CA 94404, USA
    Antimicrob Agents Chemother 55:1366-76. 2011
    ....
  11. ncbi request reprint Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection
    John O Link
    Medicinal Chemistry, Drug Metabolism, Biology, Formulation and Process Development, Clinical Research, and Structural Chemistry, Gilead Sciences, 333 Lakeside Drive, Foster City, California 94404, United States
    J Med Chem 57:2033-46. 2014
    ..39 has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms. ..
  12. pmc Correlating structure and function of drug-metabolizing enzymes: progress and ongoing challenges
    Eric F Johnson
    Department of Molecular and Experimental Medicine, The Scripps Research Institute, La Jolla, California E F J Department of Pharmacology and Experimental Therapeutics and the Stanley S Scott Cancer Center, Louisiana State University Health Sciences Center, New Orleans, Louisiana J P C, J R R, W L B Department of Medicinal Chemistry, Gilead Sciences, Inc, Foster City, California M C D, L X Department of Pharmaceutical Chemistry J S L and Department of Medicinal Chemistry D F E, E E S, University of Kansas, Lawrence, Kansas
    Drug Metab Dispos 42:9-22. 2014
    ..Although understanding P450 structure/function relationships is an ongoing challenge, translational advances will benefit from continued integration of existing and new biophysical approaches. ..