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Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells. Though temsirolimus shows activity on its own, it is also known to be converted to sirolimus (rapamycin) in vivo; [4] therefore, its activity may be more attributed to its metabolite rather than the prodrug itself (despite claims to the ...
mTOR inhibitors are a class of drugs used to treat several human diseases, including cancer, autoimmune diseases, and neurodegeneration. They function by inhibiting the mammalian target of rapamycin (mTOR) (also known as the mechanistic target of rapamycin), which is a serine/threonine-specific protein kinase that belongs to the family of phosphatidylinositol-3 kinase (PI3K) related kinases ...
For example, postmortem studies of human AD brain reveal dysregulation in PTEN, Akt, S6K, and mTOR. [ 99 ] [ 100 ] [ 101 ] mTOR signaling appears to be closely related to the presence of soluble amyloid beta (Aβ) and tau proteins, which aggregate and form two hallmarks of the disease, Aβ plaques and neurofibrillary tangles, respectively. [ 102 ]
This prevents the structure from being recruited to the preautophagosomal structure at the plasma membrane, inhibiting autophagy. [ 59 ] mTORC1's ability to inhibit autophagy while at the same time stimulate protein synthesis and cell growth can result in accumulations of damaged proteins and organelles, contributing to damage at the cellular ...
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.
Sirolimus, also known as rapamycin and sold under the brand name Rapamune among others, is a macrolide compound that is used to coat coronary stents, prevent organ transplant rejection, treat a rare lung disease called lymphangioleiomyomatosis, and treat perivascular epithelioid cell tumour (PEComa).
Crystal structure of the second generation Bcr-Abl tyrosine-kinase inhibitor nilotinib (red) in complex with an Abl kinase domain (blue). Nilotinib is used to treat chronic myelogenous leukemia (CML), a hematological malignancy. A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases.
A ternary complex is a protein complex containing three different molecules that are bound together. In structural biology, ternary complex can also be used to describe a crystal containing a protein with two small molecules bound, such as a cofactor and a substrate; or a complex formed between two proteins and a single substrate. [1]