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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;mTOR;inhibitor;PI3K;ulcerative colitis;inflammation
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)1,2. The discovery, synthesis and a SAR of new cyano-pyridyl based small molecule inhibitor which suppresses DSS-induced colitis by inhibiting T cell function3 is discussed. The most potent small molecule inhibitor of mTOR did not inhibit PI3K/Akt phosphorylation and thus turned out to be mTOR selective.
Page(s): 1761-1765
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.48B(12) December 2009]

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