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Mk-2206 inhibitor 4 years 28 weeks ago

MK2206 is a Akt inhibitor, is also an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor MK2206 binds to and inhibits the activity of Akt in a non-ATP competitive manner

Loratadine Inhibitor 4 years 14 weeks ago

Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Reference Reading
1.Effects of Prednisolone on the Pharmacokinetics of Loratadine after Oral and Intravenous Administration of Loratadine in Rats
2.Physicochemical characterization and dissolution enhancement of loratadine by solid dispersion technique

Cycling Benefits - Health Benefits of Cycling 2 years 11 weeks ago

Everyone knows that cycling is good for health. But do you know what exactly cycling affects?

Riding a bicycle has a positive effect on almost all systems of the human body. The cycle has the greatest effect on the muscles of the legs and back, but also involves other muscles, including the shoulders and the abs. Cycling will help you find a taut figure and relief muscles.
Read more about the health benefits of cycling here.

Vorinostat Inhibitor 4 years 6 weeks ago

Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM.
Reference Reading
1. Clinical pharmacology profile of vorinostat, a histone deacetylase inhibitor
Marian Iwamoto • Evan J. Friedman •Punam Sandhu • Nancy G. B. Agrawal. Cancer Chemother Pharmacol (2013) 72:493–508
Vorinostat is an HDAC inhibitor currently marketed in the United States and other countries for the treatment of cutaneous manifestations in patients with cutaneous T cell lymphoma (CTCL) who have progressive disease, persistent, or recurrent disease following two systemic therapies. Vorinostat inhibits the enzymatic activity of Class I (HDAC1, HDAC2, HDAC3) and Class II (HDAC6) HDACs at nanomolar concentrations (IC50<86 nM). A clinical study of vorinostat in patients with stage Ib and higher CTCL, who had failed to two systemic therapies (one containing bexarotene), demonstrated a 30 % overall objective response. An additional study in refractory CTCL patients demonstrated a similar response rate of 31 %.

Cyt387 Inhibitor 4 years 32 weeks ago

Cyt387, also called Momelotinib, under the IUPAC name N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide, is an ATP competitive inhibitor of JAK1 (IC50 = 11 nM) and JAK2 (IC50 = 18 nM) with potential antineoplastic activity, which may result result in the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

Simvastatin Inhibitor 4 years 6 weeks ago

Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM .
TargetsHMG-CoA Reductase (HMGCR)
Reference Reading
1. Input of selected human pharmaceutical metabolites into the Norwegian aquatic environment
Although we did not detect any ATV metabolites in surface water, interestingly we did detect the presence of the main and active metabolite of the statin prodrug simvastatin (SV); simvastatin hydroxy carboxylic acid (SVA) in four of the surface water and sediments collected from Oslofjord.The surface water samples collected contained SVA at concentrations > LODand up to 66 ng L-1, whilst two sediment samples contained low ng g-1 (dw) concentrations of SVA also. No effluent concentrations of SVA were determined; however, we have previously reported the occurrence of SV at low ng L-1 in VEAS WwTW effluent suggesting from these preliminary data that effluent concentrations of SVA would indeed be higher.

Protein Methylation 3 years 5 weeks ago

Protein methylation is a post-translational modification process, in which proteins are modified by an addition of methyl groups by S-adenosylmethionine dependent methyltransferases, with S-adenosyl methionine (SAM) as the primary donor of methyl group. Methylation of proteins can occur on multiple amino acids on proteins, including arginine, lysine, histidine, etc. Methylation is mediated by methyltransferases, Methylation of lysine involves the addition of one to three methyl groups on the amino acid's ε-amine group, to form mono-, di- or tri-methyllysine. This modification often occurs in a conserved sequence motif on proteins. For example, two typical motifs are RGG box and RXR sequence. Depending on the site of residual methyl group attached to, there are two types of methylation: N-methylation and O-methylation. N-methylation is irreversible, whereas, O-methylation is potentially reversible.