133 results on '"St. Jean, David J."'
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2. Figure 5 from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
3. Data from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
4. Figure 6 from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
5. Figure 4 from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
6. Figure 1 from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
7. Figure 2 from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
8. Figure 3 from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
9. Supplementary Tables and Figures from STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts
10. Abstract P4-07-04: STX-478, a mutant-selective PI3Kα H1047X inhibitor clinical candidate with a best-in-class profile: Pharmacology and therapeutic activity as monotherapy and in combination in breast cancer xenograft models
11. Discovery of Small-Molecule Glucokinase Regulatory Protein Modulators That Restore Glucokinase Activity
12. Abstract LB194: Discovery and characterization of a mutant selective PI3KαH1047Xinhibitor with a best-in-class profile
13. Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors
14. A general route toward the synthesis of the cladiellin skeleton utilizing a SmI2-mediated cyclization
15. 11β-Hydroxysteroid Dehydrogenase Type 1 as a Therapeutic Target for Type 2 Diabetes
16. Structural Characterization and Pharmacodynamic Effects of an Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor
17. A general method for the facile synthesis of optically active 2-substituted piperazines via functionalized 2,5-diketopiperazines
18. Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism
19. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σ*S–X) Interaction for Conformational Constraint
20. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors
21. Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis
22. Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2
23. The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core
24. ChemInform Abstract: A General Method for the Facile Synthesis of Optically Active 2-Substituted Piperazines via Functionalized 2,5-Diketopiperazines.
25. ChemInform Abstract: Nonracemic Synthesis of GK—GKRP Disruptor AMG‐3969.
26. Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 4. Exploration of a Novel Binding Pocket
27. Nonracemic Synthesis of GK–GKRP Disruptor AMG-3969
28. Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the N-Arylsulfonamido-N′-arylpiperazine Series
29. Correction to Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept
30. Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept
31. Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 2. Leveraging Structure-Based Drug Design to Identify Analogues with Improved Pharmacokinetic Profiles
32. Correction to Mitigating Heterocycle Metabolism in Drug Discovery
33. Mitigating Heterocycle Metabolism in Drug Discovery
34. Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes
35. From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)
36. Discovery of a Calcimimetic with Differential Effects on Parathyroid Hormone and Calcitonin Secretion
37. Discovery of a Potent, Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor for Clinical Study: Identification of (S)-2-((1S,2S,4R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221)
38. Discovery and Optimization of Substituted 1-(1-Phenyl-1H-pyrazol-3-yl)methanamines as Potent and Efficacious Type II Calcimimetics
39. The discovery of 2-anilinothiazolones as 11β-HSD1 inhibitors
40. Piperidine amides as 11β-hydroxysteroid dehydrogenase type 1 inhibitors
41. Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model
42. ChemInform Abstract: A Tandem Cross‐Coupling/SNAr Approach to Functionalized Carbazoles.
43. Structural Characterization and Pharmacodynamic Effects of an Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor
44. A Tandem Cross-Coupling/SNAr Approach to Functionalized Carbazoles
45. 2-(S)-Phenethylaminothiazolones as Potent, Orally Efficacious Inhibitors of 11β-Hydroxysteriod Dehydrogenase Type 1
46. Thiourea
47. Development of a tandem cyclization mediated by samarium(II) iodide: sequential intramolecular conjugate addition/nucleophilic acyl substitution
48. Toward a General Route to the Eunicellin Diterpenes: The Asymmetric Total Synthesis of Deacetoxyalcyonin Acetate.
49. Samarium(II) Iodide-Mediated Intramolecular Conjugate Additions of α,β-Unsaturated Lactones
50. Small Molecule Disruptors of the Glucokinase–GlucokinaseRegulatory Protein Interaction: 4. Exploration of a Novel BindingPocket.
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