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1. MEK inhibitors overcome resistance to BET inhibition across a number of solid and hematologic cancers.

2. Small-Molecule Targets in Immuno-Oncology.

3. Role of Histone-Modifying Enzymes and Their Complexes in Regulation of Chromatin Biology.

4. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.

5. A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.

6. Control of NF-kB activity in human melanoma by bromodomain and extra-terminal protein inhibitor I-BET151.

7. SMYD3 links lysine methylation of MAP3K2 to Ras-driven cancer.

8. Long residence time inhibition of EZH2 in activated polycomb repressive complex 2.

9. Cancer epigenetics drug discovery and development: the challenge of hitting the mark.

10. Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer.

11. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.

12. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.

13. Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.

14. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.

15. Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation.

16. ALDH1A1 is a novel EZH2 target gene in epithelial ovarian cancer identified by genome-wide approaches.

17. Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).

18. Biochemical characterization of human HIF hydroxylases using HIF protein substrates that contain all three hydroxylation sites.

19. Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor.

20. C-terminal region of USP7/HAUSP is critical for deubiquitination activity and contains a second mdm2/p53 binding site.

21. Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

22. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.

23. Myelosuppression and kinase selectivity of multikinase angiogenesis inhibitors.

24. Evidence for allosteric interactions of antagonist binding to the smoothened receptor.

25. Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1.

26. The catalytic role of INCENP in Aurora B activation and the kinetic mechanism of Aurora B/INCENP.

27. Characterization of PI3K class IA isoforms with regulatory subunit p55alpha using a scintillation proximity assay.

28. Biochemical characterization of human prolyl hydroxylase domain protein 2 variants associated with erythrocytosis.

29. Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.

30. Conformation-dependent ligand regulation of ATP hydrolysis by human KSP: activation of basal hydrolysis and inhibition of microtubule-stimulated hydrolysis by a single, small molecule modulator.

31. Residence time of receptor-ligand complexes and its effect on biological function.

32. Effects of oncogenic p110alpha subunit mutations on the lipid kinase activity of phosphoinositide 3-kinase.

33. Characterization of an exosite binding inhibitor of matrix metalloproteinase 13.

34. Binding of TPX2 to Aurora A alters substrate and inhibitor interactions.

35. Targeting enzyme inhibitors in drug discovery.

36. A second p53 binding site in the central domain of Mdm2 is essential for p53 ubiquitination.

37. An assay for Fe(II)/2-oxoglutarate-dependent dioxygenases by enzyme-coupled detection of succinate formation.

38. A biochemical rationale for the anticancer effects of Hsp90 inhibitors: slow, tight binding inhibition by geldanamycin and its analogues.

39. Expression, purification, and enzymatic characterization of the dual specificity mitogen-activated protein kinase phosphatase, MKP-4.

40. Enzymatic characterization of the pancreatic islet-specific glucose-6-phosphatase-related protein (IGRP).

41. Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors.

42. Helicobacter pylori 3-deoxy-D-manno-octulosonate-8-phosphate (KDO-8-P) synthase is a zinc-metalloenzyme.

43. 5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.

44. Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.

45. Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.

46. 4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme.

47. Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.

48. Genomic-sequence comparison of two unrelated isolates of the human gastric pathogen Helicobacter pylori.

49. Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: the profound effect of polarity on antiviral activity.

50. 4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.

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