1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine

Isoquinolines

Piperazines

Protein Kinase C

Tetradecanoylphorbol Acetate

Diglycerides

Protein Kinase Inhibitors

Enzyme Inhibitors

Calcium

Receptors, Retinoic Acid

Phorbol 12,13-Dibutyrate

Staurosporine

Sulfonamides

Alkaloids

Phlorhizin

Sphingosine

Calcimycin

List of MeSH codes (D03)

List of MeSH codes (D02)

Protein3

• We found that 5-Aza-Dc and TSA can effectively decrease the mRNA and protein expressions of RhoC, ROCK1, and ROCK2. (medscimonit.com)
• Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. (embl-heidelberg.de)
• Of these, the H series protein kinase inhibitors (1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H7), N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide (H8) N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H89)) are frequently used to block signaling pathways in studies of cellular regulation. (embl-heidelberg.de)

Inhibitor1

• RPMI8226 and U266 cell lines were treated by 5-aza-2-deoxycytidine (5-Aza-Dc), trichostatin A (TSA), RhoA inhibitor CCG-1423, Rac1 inhibitor NSC23766, and ROCK inhibitor fasudil. (medscimonit.com)

Form1

• The crystal structure of the tyrosine kinase domain of fibroblast growth factor receptor 1 (FGFR1K) has been determined in its unliganded form to 2.0 angstroms resolution and in complex with with an ATP analog to 2.3 angstrosms A resolution. (embl-heidelberg.de)

Inhibitors1

• Other protein kinase inhibitors may be useful in down regulating transcription of HIV-1 provirus and thereby virus replication in HIV-infected patients. (biomedcentral.com)

Inhibition2

• Phosphodiesterase-5 inhibition preserves exercise-onset vasodilator kinetics when NOS activity is reduced. (ouhsc.edu)
• The inhibition by PTX of protein kinase C (PKC) or cAMP-dependent protein kinase (PKA)-mediated activation by phorbol ester (PMA) and tumor necrosis factor alpha (TNF- α ) of HIV-1-LTR-regulated reporter gene expression was studied in human CD4 + T lymphocytes (Jurkat) and human embryo kidney cells (293-27-2). (biomedcentral.com)

Extracts1

• PTX inhibited PKC- or PKA-catalyzed activation of NF- κ B in cytoplasmic extracts from unstimulated Jurkat or 293-27-2 cells, but not interaction of preactivated NF- κ B with its motifs. (biomedcentral.com)

Tumor necro1

• Treatment of vascular media and VSMCs with lipopolysaccharide (LPS) or cytokines [tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β)] resulted in a dose-dependent increase of NO release. (researchwithrutgers.com)

Amino1

• On the other hand, induction of certain genes such as amino levulinate synthase 1 by PB is not regulated by CAR. (nih.gov)

Genes1

• In addition to coordinating these enzymes, CAR plays other roles in hepatic gene expression: CAR represses various genes including carnitine palmitoyltransferase 1a and phosphoenolpyruvate carboxykinase 1 in response to PB, and the receptor regulates the constitutive expression of genes such as squalene epoxidase. (nih.gov)

Activation2

• The mechanism of inhibitory action of PTX on virus replication and NF- κ B-induced trans -activation of HIV-1 gene expression has been elucidated as due to blocking PKC-dependent PMA- or TNF- α -induced activation of NF- κ B in Jurkat and 293-27-2 cells. (biomedcentral.com)
• The involvement of Raf-1 kinase in the activation of NF- κ B was also reported ( 23 ). (biomedcentral.com)

Type2

• This investigation deals with the molecular mechanism of anti-human immunodeficiency virus type 1 (HIV-1) action of pentoxifylline (PTX) [1-(5′-oxohexyl)-3,7-dimethylxanthine] a drug widely used for the treatment of conditions involving defective regional microcirculation. (biomedcentral.com)
• Human immunodeficiency virus type 1 (HIV-1) is implicated in the deadly disease acquired immune deficiency syndrome (AIDS). (biomedcentral.com)

Cells2

• We have reported that treatment of cells with pentoxifylline (PTX) [1-(5-oxohexyl)-3,7-dimethylxanthine] inhibits HIV-1 replication ( 2 ). (biomedcentral.com)
• The drug down-regulates HIV-1 LTR-driven gene expression in stimulated cells through its action upon the two nuclear factor kappa B (NF- κ B) motifs in the LTR ( 3 ). (biomedcentral.com)

Research1

• 1 Pharmacogenetics Section, Laboratory of Reproductive and Developmental Toxicology, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, NC 27709, USA. (nih.gov)