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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. [1] Protein kinases are enzymes that phosphorylate (add a phosphate , or PO 4 , group) to a protein and can modulate its function.
Protein phosphorylation is a reversible post-translational modification of proteins in which an amino acid residue is phosphorylated by a protein kinase by the addition of a covalently bound phosphate group. Phosphorylation alters the structural conformation of a protein, causing it to become activated, deactivated, or otherwise modifying its ...
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 ...
A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit. TKIs are typically used as ...
WEE1 kinase and PLK1 are also targeted by Chk1 to induce cell cycle arrest. Phosphorylation of WEE1 kinase inhibits cdk1 which results in cell cycle arrest at the G2 phase. [8] Chk1 has a role in the spindle checkpoint during mitosis thus interacts with spindle assembly proteins Aurora A kinase and Aurora B kinase. [9]
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 ...
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 ...
In cell biology, protein kinase C, commonly abbreviated to PKC (EC 2.7.11.13), is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins, or a member of this family.