Marion Lanier

Summary

Affiliation: Human BioMolecular Research Institute
Country: USA

Publications

  1. ncbi Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response
    Marion Lanier
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121 2804, United States
    J Med Chem 55:697-708. 2012
  2. ncbi Design and synthesis of selective inhibitors of placental alkaline phosphatase
    Marion Lanier
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121 2804, USA
    Bioorg Med Chem 18:573-9. 2010
  3. ncbi Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor
    Joe A Tran
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 16:3693-6. 2006
  4. ncbi Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines
    Joe A Tran
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 15:833-7. 2005
  5. ncbi A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice
    Joseph Pontillo
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 15:2541-6. 2005
  6. ncbi Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling
    Dennis Schade
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121 2804, USA
    J Med Chem 55:9946-57. 2012
  7. ncbi Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists
    Zhiqiang Guo
    Department of Medicinal Chemistry, Neurocrine Biosciences Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    J Med Chem 48:5104-7. 2005
  8. ncbi Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties
    John E Tellew
    Department of Medicinal Chemistry, Neurocrine Biosciences, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 20:7259-64. 2010
  9. ncbi Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells
    Erik Willems
    Muscle Development and Regeneration Program, Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Cell Stem Cell 11:242-52. 2012
  10. ncbi Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor
    Joseph Pontillo
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 14:5605-9. 2004

Collaborators

Detail Information

Publications11

  1. ncbi Wnt inhibition correlates with human embryonic stem cell cardiomyogenesis: a structure-activity relationship study based on inhibitors for the Wnt response
    Marion Lanier
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121 2804, United States
    J Med Chem 55:697-708. 2012
    ..Taken together, these data show that Wnt signaling inhibition is essential for cardiogenic activity and that the pathway can be targeted for the design of druglike cardiogenic molecules...
  2. ncbi Design and synthesis of selective inhibitors of placental alkaline phosphatase
    Marion Lanier
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121 2804, USA
    Bioorg Med Chem 18:573-9. 2010
    ..These selective PLAP inhibitors will provide small molecule probes for the study of the pathophysiological role of PLAP...
  3. ncbi Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor
    Joe A Tran
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 16:3693-6. 2006
    ..A series of 2-pyridinylpiperazines derived from beta-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki=6.5 nM) possessed high potency...
  4. ncbi Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines
    Joe A Tran
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 15:833-7. 2005
    ..3 and 4.5 nM, respectively. Interestingly, 12e was a full agonist with an EC(50) value of 31 nM, and 12l was a weak partial agonist (IA=17%) and functioned as an antagonist (IC(50)=300 nM)...
  5. ncbi A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice
    Joseph Pontillo
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 15:2541-6. 2005
    ..2 nM) with a selectivity of 240-fold over MC3R. It proved to be an insurmountable antagonist in a cAMP assay. Compound 14c potently stimulated food intake in satiated mice when given by intracerebroventricular administration...
  6. ncbi Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling
    Dennis Schade
    Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121 2804, USA
    J Med Chem 55:9946-57. 2012
    ..This stereopreference was not observed for the low level inhibition against Activin A signaling and was reversed for effects on calcium handling in HL-1 cells...
  7. ncbi Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists
    Zhiqiang Guo
    Department of Medicinal Chemistry, Neurocrine Biosciences Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    J Med Chem 48:5104-7. 2005
    ..In our effort to identify CRF(1) antagonists with improved pharmacokinetics properties, 16g exhibited a favorably lower volume of distribution...
  8. ncbi Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties
    John E Tellew
    Department of Medicinal Chemistry, Neurocrine Biosciences, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 20:7259-64. 2010
    ..Compound (S)-8d was identified as a high affinity ligand with a pK(i) value of 8.2 and a functional CRF(1) antagonist with pIC(50) value of 7.0 in the in vitro CRF ACTH production assay...
  9. ncbi Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells
    Erik Willems
    Muscle Development and Regeneration Program, Sanford Burnham Medical Research Institute, La Jolla, CA 92037, USA
    Cell Stem Cell 11:242-52. 2012
    ..ITD-1 is a highly selective TGF-β inhibitor and reveals an unexpected role for TGF-β signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors...
  10. ncbi Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor
    Joseph Pontillo
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 12790 El Camino Real, San Diego, CA 92130, USA
    Bioorg Med Chem Lett 14:5605-9. 2004
    ....
  11. ncbi Structure-activity relationships of piperazinebenzylamines as potent and selective agonists of the human melanocortin-4 receptor
    Joseph Pontillo
    Department of Medicinal Chemistry, Neurocrine Biosciences, Inc, 10555 Science Center Drive, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 14:4417-23. 2004
    ..Analogs bearing an additional hetero-atom in the side-chain possessed good agonist potency. Thus, 11h had a Ki of 11 nM, and 13g exhibited an EC50 of 3.8 nM and a Ki of 6.4 nM...