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Title: Mammalian target of rapamycin (mTOR) inhibitors with therapeutic potential for colitis
Authors: Deore, Vijaykumar
Bhonde, Mandar R
Vishwakarma, Ram A
Dagia, Nilesh M
Kumar, Sanjay
Roychowdhury, Abhijit
Keywords: Cyanopyridyl
ulcerative colitis
Issue Date: Dec-2009
Publisher: CSIR
Abstract: Mammalian target of rapamycin (mTOR) is a protein kinase that regulates cell proliferation and protein synthesis in response to mitogens and nutrients. A plethora of recent research has linked increased mTOR activity to heightened inflammatory responses. Many of these findings suggest that mTOR inhibitors may be useful for treatment of ulcerative colitis (UC)<sup>1,2</sup>. The discovery, synthesis and a SAR of new cyano-pyridyl based small molecule inhibitor which suppresses DSS-induced colitis by inhibiting T cell function<sup>3 </sup>is discussed. The most potent small molecule inhibitor of mTOR did not inhibit PI3K/Akt phosphorylation and thus turned out to be mTOR selective.
Description: 1761-1765
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.48B(12) December 2009]

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