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A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that phosphorylate (add a phosphate, or PO 4, group) to a protein and can modulate its function. The phosphate groups are usually added to serine, threonine, or tyrosine amino acids on the protein.
Phosphoinositide 3-kinase inhibitors (PI3K inhibitors) are a class of medical drugs that are mainly used to treat advanced cancers. They function by inhibiting one or more of the phosphoinositide 3-kinase (PI3K) enzymes, which are part of the PI3K/AKT/mTOR pathway. This signal pathway regulates cellular functions such as growth and survival. It ...
1027 12576 Ensembl ENSG00000111276 ENSMUSG00000003031 UniProt P46527 P46414 RefSeq (mRNA) NM_004064 NM_009875 RefSeq (protein) NP_004055 NP_034005 Location (UCSC) Chr 12: 12.69 – 12.72 Mb Chr 6: 134.9 – 134.9 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Cyclin-dependent kinase inhibitor 1B (p27 Kip1) is an enzyme inhibitor that in humans is encoded by the CDKN1B gene. It ...
Pages in category "Protein kinase inhibitors" The following 62 pages are in this category, out of 62 total. This list may not reflect recent changes. ...
The PI3K-mTOR pathway leads to the phosphorylation of p70S6K, a kinase that facilitates translational activity, [31] [32] further suggesting that PI3Ks are required for the protein-synthesis phase of LTP induction instead. PI3Ks interact with the insulin receptor substrate (IRS) to regulate glucose uptake through a series of phosphorylation events.
As of 2017, an estimated 29% of approved drugs are enzyme inhibitors [96] of which approximately one-fifth are kinase inhibitors. [96] A notable class of kinase drug targets is the receptor tyrosine kinases which are essential enzymes that regulate cell growth; their over-activation may result in cancer. Hence kinase inhibitors such as imatinib ...
CDKN2A, also known as cyclin-dependent kinase inhibitor 2A, is a gene which in humans is located at chromosome 9, band p21.3. [5] It is ubiquitously expressed in many tissues and cell types. [ 6 ] The gene codes for two proteins , including the INK4 family member p16 (or p16INK4a) and p14arf . [ 7 ]
A number of Rho kinase inhibitors are known. [15] [16] [17]Chemical structure of fasudil. AT-13148 [18]; BA-210; β-ElemeneBelumosudil; Chroman 1 [19] [20]; DJ4, which is a selective multi-specific ATP competitive inhibitor of activity of ROCK1 (IC50 of 5 nM), ROCK2 (IC50 of 50 nM), MRCKα (IC50 of 10 nM) and MRCKβ (IC50 of 100 nM) kinases without affecting activity of PAK1 and DMPK at 5 μM ...