PTP1B antisense oligonucleotide lowers PTP1B protein, normalizes blood glucose, and improves insulin sensitivity in diabetic mice

Bradley A. Zinker, Cristina M. Rondinone, James M. Trevillyan, +19

Proceedings of the National Academy of Sciences

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Emily J. Faivre, Keith F. McDaniel, Daniel H. Albert, +31

Nature

Bd2 BromodomainMedicineNatural SciencesMolecular BiologyCancer Biology +7

Discovery of <i>N</i>-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

Keith F. McDaniel, Le Wang, Todd Soltwedel, +29

Journal of Medicinal Chemistry

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Mai H. Bui, Daniel H. Albert, Leiming Li, +21

Cancer Research

Discovery of <i>N</i>-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1<i>H</i>-pyrrolo[2,3-<i>c</i>]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

George S. Sheppard, Le Wang, Steven D. Fidanze, +20

Journal of Medicinal Chemistry

Synthesis and Characterization of Non-Steroidal Ligands for the Glucocorticoid Receptor:  Selective Quinoline Derivatives with Prednisolone-Equivalent Functional Activity

Michael J. Coghlan, Philip R. Kym, Steven W. Elmore, +10

Journal of Medicinal Chemistry

Medicinal ChemistryAllergyPrednisolone-equivalent Functional ActivityG Protein-coupled ReceptorMedicine +10

Hepatic Glucocorticoid Receptor Antagonism Is Sufficient to Reduce Elevated Hepatic Glucose Output and Improve Glucose Control in Animal Models of Type 2 Diabetes

Peer B. Jacobson, Thomas W von Geldern, Lars Öhman, +22

Journal of Pharmacology and Experimental Therapeutics

Liver-Selective Glucocorticoid Antagonists:  A Novel Treatment for Type 2 Diabetes

Thomas W von Geldern, Noah P. Tu, Philip R. Kym, +23

Journal of Medicinal Chemistry

ImmunologyGlucocorticoidMetabolic SyndromeBile Acid ConjugationBile Acid +14

Hepatic knockdown of mitochondrial GPAT1 in ob/ob mice improves metabolic profile

Haiyan Xu, Denise Wilcox, Phong Nguyen, +13

Biochemical and Biophysical Research Communications

Metabolic SyndromeEnergy MetabolismMetabolic ProfileBiochemistryMitochondrial Function +11

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors

Le Wang, John K. Pratt, Todd Soltwedel, +30

Journal of Medicinal Chemistry