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TGX-221

TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .

TGX-221 is a LY294002  (structure shown below) analogue, able to inhibit selectively the PI3Kβ isoform in vitro.   The observed inhibition of platelet-ECC interaction and platelet activation by tirofiban contributes to explain the mechanism of "platelet anaesthesia". TGX-221 represents a promising alternative to GP IIb/IIIa blockade and should be further investigated for use during ECC in vivo. see http://www.ncbi.nlm.nih.gov/pubmed/18327411.

Current developer:   

 1. Carlson, Coby B.; Robers, Matthew B.; Vogel, Kurt W.; Machleidt, Thomas. Development of LanthaScreen cellular assays for key components within the PI3K/AKT/mTOR pathway. Journal of Biomolecular Screening (2009), 14(2), 121-132. CODEN: JBISF3 ISSN:1087-0571. CAN 152:372598 AN 2010:291701

2. Edgar, Kyle A.; Wallin, Jeffrey J.; Berry, Megan; Lee, Leslie B.; Prior, Wei Wei; Sampath, Deepak; Friedman, Lori S.; Belvin, Marcia. Isoform-Specific Phosphoinositide 3-Kinase Inhibitors Exert Distinct Effects in Solid Tumors. Cancer Research (2010), 70(3), 1164-1172. CODEN: CNREA8 ISSN:0008-5472. CAN 152:469647 AN 2010:129884

3. Kim, Soochong; Mangin, Pierre; Dangelmaier, Carol; Lillian, Rivka; Jackson, Shaun P.; Daniel, James L.; Kunapuli, Satya P. Role of phosphoinositide 3-kinase  in glycoprotein VI-mediated Akt activation in platelets. Journal of Biological Chemistry (2009), 284(49), 33763-33772. CODEN: JBCHA3 ISSN:0021-9258. CAN 152:70920 AN 2009:1485944

4. Kong, Dexin; Yamori, Takao. Advances in development of phosphatidylinositol 3-kinase inhibitors. Current Medicinal Chemistry (2009), 16(22), 2839-2854. CODEN: CMCHE7 ISSN:0929-8673. CAN 151:235330 AN 2009:988459

5. Billottet, Clotilde; Banerjee, Lalita; Vanhaesebroeck, Bart; Khwaja, Asim. Inhibition of Class I Phosphoinositide 3-Kinase Activity Impairs Proliferation and Triggers Apoptosis in Acute Promyelocytic Leukemia without Affecting Atra-Induced Differentiation. Cancer Research (2009), 69(3), 1027-1036. CODEN: CNREA8 ISSN:0008-5472. CAN 150:389388 AN 2009:117671

6. Straub, Andreas; Wendel, Hans Peter; Dietz, Klaus; Schiebold, Daniela; Peter, Karlheinz; Schoenwaelder, Simone M.; Ziemer, Gerhard. Selective inhibition of the platelet phosphoinositide 3-kinase p110 as promising new strategy for platelet protection during extracorporeal circulation. Thrombosis and Haemostasis (2008), 99(3), 609-615. CODEN: THHADQ ISSN:0340-6245. CAN 149:347128 AN 2008:780796

7. Kim, Tae-Wan; Dipaolo, Gilbert; Kang, Min Suk; Berman, Diego; McIntire, Laura Beth Johnson. Phosphoinositide modulation for the treatment of neurodegenerative diseases. PCT Int. Appl. (2008), 78 pp. CODEN: PIXXD2 WO 2008064244 A2 20080529 CAN 149:1496 AN 2008:640221

8. Chaussade, Claire; Rewcastle, Gordon W.; Kendall, Jackie D.; Denny, William A.; Cho, Kitty; Gronning, Line M.; Chong, Mei Ling; Anagnostou, Sasha H.; Jackson, Shaun P.; Daniele, Nathalie; Shepherd, Peter R. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochemical Journal (2007), 404(3), 449-458.

9. Wolff, Michael; Haasen, Dorothea; Merk, Susanne; Kroner, Margareta; Maier, Udo; Bordel, Sandra; Wiedenmann, Joerg; Nienhaus, Gerd Ulrich; Valler, Martin; Heilker, Ralf. Automated high content screening for phosphoinositide 3 kinase inhibition using an AKT1 redistribution assay. Combinatorial Chemistry & High Throughput Screening (2006), 9(5), 339-350. 

10. Sturgeon Sharelle A; Jones Catherine; Angus James A; Wright Christine E Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat. European journal of pharmacology (2008), 587(1-3), 209-15. 

11. Anonymous Safer clotbuster on the horizon. Health news (Waltham, Mass.) (2005), 11(9), 2.