Blog of Signaling Pathways

LY2484595 is one of two CETP inhibitors currently being evaluated

2830 views | May 02 2013

LY2484595 results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. [Read the Full Post]

Tubastatin A was substantially more selective than the known HDAC6 inhibitor

4067 views | Apr 28 2013

Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. [Read the Full Post]

SP600125 is supplied as a lyophilized powder

3348 views | Apr 26 2013

SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. [Read the Full Post]

Nilotinib was approved as Tasigna in the America

3189 views | Apr 24 2013

Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-SMA and collagen in activated HSCs. Nilotinib induces apoptosis of HSCs, which is correlated with reduced bcl-2 expression, increases p53 expression, cleavage of PARP, as well as increases expression of PPARγ and TRAIL-R. Nilotinib also induces cell cycle arrest, accompanied by increased expression of p27 and downregulation of cyclin D1. [Read the Full Post]

MG132 is a specific potent reversible and cell permeable proteasome inhibitor

3731 views | Apr 22 2013

MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. MG-132 induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM. [Read the Full Post]

MDV3100 was found clinically active for metastatic

2845 views | Apr 18 2013

MDV3100 is an androgen receptor antagonist drug developed by the pharmaceutical company Medivation for the treatment of metastatic castration-resistant prostate cancer. [Read the Full Post]

IOX2 is a potent inhibitor of HIF1with IC50 of 21 nM

4480 views | Apr 16 2013

IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM. [Read the Full Post]

PD98059 is a potent and selective inhibitor of MAP kinase

2365 views | Apr 10 2013

PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. PD98059 does not inhibit the MAPK homologues JNK and P38. PD98059 is highly selective against MEK, as it does not inhibit a number of other kinase activities including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol 3-kinase. [Read the Full Post]

Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases

3067 views | Apr 08 2013

These include all receptors for platelet-derived growth factor (PDGF-Rs) and vascular endothelial growth factor receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation. [Read the Full Post]

Quizartinib is currently under development for the treatment of acute myeloid leukaemia

4233 views | Apr 03 2013

Quizartinib (AC220) is a small molecule receptor tyrosine kinase inhibitor that is currently under development for the treatment of acute myeloid leukaemia. Its molecular target is FLT3, also known as CD135 which is a proto-oncogene. [Read the Full Post]

Sunitinib was the first cancer drug simultaneously approved for two different indications

2877 views | Apr 01 2013

Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. [Read the Full Post]

PD98059 is a non ATP competitive MEK inhibitor with IC50

2415 views | Mar 27 2013

PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. PD98059 does not inhibit the MAPK homologues JNK and P38. [Read the Full Post]

PS341 was tested in a small Phase I clinical trial on patients with multiple myeloma cancer

2759 views | Mar 25 2013

PS-341 is the first therapeutic proteasome inhibitor to be tested in humans. It is approved in the U.S. for treating relapsed multiple myeloma[1] and mantle cell lymphoma. In multiple myeloma, complete clinical responses have been obtained in patients with otherwise refractory or rapidly advancing disease. [Read the Full Post]

Telaprevir is an associate of a class of antiviral drugs

4563 views | Mar 21 2013

Telaprevir is an associate of a class of antiviral drugs called protease inhibitors. Especially, telaprevir prevents the hepatitis C viral enzyme NS3.4A serine protease. Telaprevir is just indicated for use against hepatitis d genotype 1 viral infections and hasnt been which can have an impact on or being protected when employed for other genotypes of the herpes virus. The standard therapy of ribavirin and pegylated interferon is less successful on genotype 1 and a welcome addition is offered by telaprevir to the treatment of this genotype. [Read the Full Post]

Vorinostat is a member of a larger class of compounds that inhibit histone deacetylases

3990 views | Mar 06 2013

A total of 155 children were screened for enrollment in the study, with 110 children being excluded on the basis of the enrollment criteria. The predominant reasons for exclusion were based on either the age or the weight criterion. Forty-five Vorinostat children meeting enrollment criteria for the PK substudy were enrolled: 23 in the AL arm and 22 in the AQ-AS arm. [Read the Full Post]

Enzalutamide is an androgen receptor inhibitor

2422 views | Feb 27 2013

Little is known of pathways involved in upstream control of Notch1 gene expression and activity in keratinocytes, and mammalian cells in general. To address this issue we undertook a chemical genetics approach. Rather than screening a large collection of unknown chemicals, enzalutamide we chose a library of 489 compounds [Read the Full Post]

Tolbutamide is a type of medicine called a sulphonylurea

3076 views | Feb 17 2013

Surgery was performed using aseptic procedures. Anaesthesia was induced using ketamine, which was followed by 2 C5% isofluorane Tolbutamide mixed with oxygen administered by inhalation for the length of the surgical procedure. The skin and fascia were removed from the dorsal surface of the skull. [Read the Full Post]

Tolbutamide is a first generation potassium channel blocker

3037 views | Feb 01 2013

Systemic lupus erythematosus (SLE) is an autoimmune disease characterized by excessive and chronic activation of inflammatory pathways via immune Tolbutamide complex deposition, complement activation, and Fc receptor (FcR) ligation, often leading to significant clinical pathologies including glomerulonephritis [Read the Full Post]

Ridaforolimus is a smallmolecule inhibitor of mTOR

2230 views | Jan 30 2013

Upon activation of PI3-K, the serine?Cthreonine kinase phosphoinositide-dependent kinase 1 is translocated to the membrane by binding of its PH domain to the second messenger PIP3. PDK1 can activate a variety of kinases from the AGC family including PKB, p70 ribosomal S6 kinase and several Ridaforolimus isoforms of protein kinase C . [Read the Full Post]

Olaparib for the treatment of the BRCA1 or BRCA2 gene mutations in cancer

3376 views | Jan 23 2013

A broad range of pathological disorders is linked to oxidative stress, including carcinogenesis and several age-dependent disorders . Oxidative stress is defined as an imbalance Olaparib in which the production of reactive oxygen species overcomes the antioxidative cell defence system [Read the Full Post]