Daniel F. Ortwine

Overview

Best Publications

• Histone Deacetylase (HDAC) Inhibitor Kinetic Rate Constants Correlate with Cellular Histone Acetylation but Not Transcription and Cell Viability

  Benjamin E.L. Lauffer;Robert Mintzer;Rina Fong;Susmith Mukund

  440
  Citations

• Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.

  Shivani Ahuja;Susmith Mukund;Lunbin Deng;Kuldip Khakh

  338
  Citations

• Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran-2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus.

  B D Roth;C J Blankley;A W Chucholowski;E Ferguson

  269
  Citations

• Discovery and Characterization of a Novel Inhibitor of Matrix Metalloprotease-13 That Reduces Cartilage Damage in Vivo without Joint Fibroplasia Side Effects

  Adam R. Johnson;Alexander G. Pavlovsky;Daniel F. Ortwine;Faith Prior

  259
  Citations

• Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.

  James J. Crawford;Adam R. Johnson;Dinah L. Misner;Lisa D. Belmont

  252
  Citations

• Substituted 2-Benzothiazolamines as Sodium Flux Inhibitors: Quantitative Structure-Activity Relationships and Anticonvulsant Activity

  Sheryl J. Hays;Michael J. Rice;Daniel F. Ortwine;Graham Johnson

  152
  Citations

• X-ray structure of a hydroxamate inhibitor complex of stromelysin catalytic domain and its comparison with members of the zinc metalloproteinase superfamily.

  V. Dhanaraj;Q. Z. Ye;L. L. Johnson;D. J. Hupe

  148
  Citations

• Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations

  Adam R. Johnson;Pawan Bir Kohli;Arna Katewa;Emily Gogol

  145
  Citations

• 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.

  Brian D Palmer;Andrew M Thompson;R John Booth;Ellen M Dobrusin

  143
  Citations

• Structure−Activity Relationships and Pharmacokinetic Analysis for a Series of Potent, Systemically Available Biphenylsulfonamide Matrix Metalloproteinase Inhibitors

  Patrick M. O'brien;Daniel F. Ortwine;Alexander G. Pavlovsky;Joseph A. Picard

  142
  Citations

• N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor.

  Alexander J. Bridges;Robert F. Bruns;Daniel F. Ortwine;Steven R. Priebe

  141
  Citations

• GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

  Jun Liang;Jason R Zbieg;Robert A Blake;Jae H Chang

  130
  Citations

• Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.

  Daniel L. Flynn;Thomas R. Belliotti;Amal M. Boctor;David T. Connor

  128
  Citations

• Novel Series of Achiral, Low Molecular Weight, and Potent HIV-1 Protease Inhibitors

  J. V. N. Vara Prasad;Kimberly S. Para;Elizabeth A. Lunney;Daniel F. Ortwine

  128
  Citations

• Benzothiopyranoindazoles, a new class of chromophore modified anthracenedione anticancer agents. Synthesis and activity against murine leukemias.

  Showalter Hd;Angelo Mm;Berman Em;Kanter Gd

  106
  Citations

• Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists

  Harriet W. Hamilton;Daniel F. Ortwine;Donald F. Worth;James A. Bristol

  104
  Citations

• X-RAY STRUCTURE OF GELATINASE A CATALYTIC DOMAIN COMPLEXED WITH A HYDROXAMATE INHIBITOR

  Venugopal Dhanaraj;Mark G. Williams;Qi Zhuang Ye;Franck Molina

  99
  Citations

• A rationalization of the acidic pH dependence for stromelysin-1 (Matrix metalloproteinase-3) catalysis and inhibition.

  Linda L. Johnson;Alexander G. Pavlovsky;Adam R. Johnson;Jeffrey A. Janowicz

  99
  Citations

• Quinazolinones and Pyrido[3,4-d]pyrimidin-4-ones as Orally Active and Specific Matrix Metalloproteinase-13 Inhibitors for the Treatment of Osteoarthritis

  Jie Jack Li;Joe Nahra;Adam R. Johnson;Amy Bunker

  97
  Citations

• X-ray structure of human stromelysin catalytic domain complexed with nonpeptide inhibitors: implications for inhibitor selectivity.

  Alexander G. Pavlovsky;Mark G. Williams;Qi Zhuang Ye;Daniel F. Ortwine

  95
  Citations

• Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus.

  Bruce D. Roth;D. F. Ortwine;M. L. Hoefle;C. D. Stratton

  94
  Citations