A novel small-molecule inhibitor of NF-κB signaling

Biochemical and Biophysical Research Communications

Volumn 368, Issue 4, 2008, Pages 1007-1013

  Nakajima, Hiroto ^a   Fujiwara, Hideyasu ^a   Furuichi, Yasuhiro ^a   Tanaka, Keiji ^b   Shimbara, Naoki ^a  

^a GeneCare Research Institute   (Japan)

^b TOKYO METROPOLITAN INSTITUTE OF MEDICAL SCIENCE   (Japan)

Author keywords

Inhibitor; I B ; NF B; Proteasome; Ubiquitylation

Indexed keywords

4 [3 BENZYL 4 [5 (2 FLUOROPHENYL)FURAN 2 YLMETHYLENE] 5 OXO 4,5 DIHYDROPYRAZOL 1 YL]BENZOIC ACID; BENZYLOXYCARBONYLLEUCYLLEUCYLLEUCINAL; BETA CATENIN; GS 143; I KAPPA B; I KAPPA B ALPHA; I KAPPA B KINASE; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; INHIBITOR PROTEIN; PROTEIN MDM2; PROTEIN P53; TUMOR NECROSIS FACTOR ALPHA; UBIQUITIN CONJUGATING ENZYME E2; UBIQUITIN PROTEIN LIGASE; UBIQUITIN PROTEIN LIGASE E1; UBIQUITIN PROTEIN LIGASE E3; UNCLASSIFIED DRUG;

ARTICLE; CARCINOGENESIS; CONTROLLED STUDY; GENE INDUCTION; HUMAN; HUMAN CELL; IN VITRO STUDY; INFLAMMATION; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; UBIQUITINATION;

EID: 40049104359     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2008.01.166     Document Type: Article

References (13)

1. N.D. Perkins Integrating cell-signalling pathways with NF-kappaB and IKK function Nat. Rev. Mol. Cell Biol. 8 2007 49 62
2. Z.J. Chen Ubiquitin signalling in the NF-kappaB pathway Nat. Cell. Biol. 7 2005 758 765
3. A. Hershko A. Ciechanover The ubiquitin system Annu. Rev. Biochem. 67 1998 425 479
4. D. Voges P. Zwickl W. Baumeister The 26S proteasome: a molecular machine designed for controlled proteolysis Annu. Rev. Biochem. 68 1999 1015 1068
5. S.Y. Fuchs V.S. Spiegelman K.G. Kumar The many faces of beta-TrCP E3 ubiquitin ligases: reflections in the magic mirror of cancer Oncogene 23 2004 2028 2036
6. T. Kawakami T. Chiba T. Suzuki K. Iwai K. Yamanaka N. Minato H. Suzuki N. Shimbara Y. Hidaka F. Osaka M. Omata K. Tanaka NEDD8 recruits E2-ubiquitin to SCF E3 ligase EMBO J. 20 2001 4003 4012
7. L.T. Vassilev B.T. Vu B. Graves D. Carvajal F. Podlaski Z. Filipovic N. Kong U. Kammlott C. Lukacs C. Klein N. Fotouhi E.A. Liu In vivo activation of the p53 pathway by small-molecule antagonists of MDM2 Science 303 2004 844 848
8. Y. Sun Overview of approaches for screening for ubiquitin ligase inhibitors Methods Enzymol. 399 2005 654 663
9. P.G. Richardson C. Mitsiades T. Hideshima K.C. Anderson Bortezomib: proteasome inhibition as an effective anticancer therapy Annu. Rev. Med. 57 2006 33 47
10. Z. Lai T. Yang Y.B. Kim T.M. Sielecki M.A. Diamond P. Strack M. Rolfe M. Caligiuri P.A. Benfield K.R. Auger R.A. Copeland Differentiation of Hdm2-mediated p53 ubiquitination and Hdm2 autoubiquitination activity by small molecular weight inhibitors Proc. Natl. Acad. Sci. USA 99 2002 14734 14739
11. R. Stoll C. Renner S. Hansen S. Palme C. Klein A. Belling W. Zeslawski M. Kamionka T. Rehm P. Muhlhahn R. Schumacher F. Hesse B. Kaluza W. Voelter R.A. Engh T.A. Holak Chalcone derivatives antagonize interactions between the human oncoprotein MDM2 and p53 Biochemistry 40 2001 336 344
12. Y. Yang R.L. Ludwig J.P. Jensen S.A. Pierre M.V. Medaglia I.V. Davydov Y.J. Safiran P. Oberoi J.H. Kenten A.C. Phillips A.M. Weissman K.H. Vousden Small molecule inhibitors of HDM2 ubiquitin ligase activity stabilize and activate p53 in cells Cancer Cell 7 2005 547 559
13. D.C. Swinney Y.Z. Xu L.E. Scarafia I. Lee A.Y. Mak Q.F. Gan C.S. Ramesha M.A. Mulkins J. Dunn O.Y. So T. Biegel M. Dinh P. Volkel J. Barnett S.A. Dalrymple S. Lee M. Huber A small molecule ubiquitination inhibitor blocks NF-kappa B-dependent cytokine expression in cells and rats J. Biol. Chem. 277 2002 23573 23581