The same site on the integrase-binding domain of lens epithelium-derived growth factor is a therapeutic target for MLL leukemia and HIV

Blood

Volumn 124, Issue 25, 2014, Pages 3730-3737

  Murai, Marcelo J ^a   Pollock, Jonathan ^a   He, Shihan ^a   Miao, Hongzhi ^a   Purohit, Trupta ^a   Yokom, Adam ^a   Hess, Jay L ^a   Muntean, Andrew G ^a   Grembecka, Jolanta ^a   Cierpicki, Tomasz ^a  

^a UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

INTEGRASE; LENS EPITHELIUM DERIVED GROWTH FACTOR; METHIONINE; MIXED LINEAGE LEUKEMIA PROTEIN; HISTONE LYSINE METHYLTRANSFERASE; LENS EPITHELIUM-DERIVED GROWTH FACTOR; MEN1 PROTEIN, HUMAN; MLL PROTEIN, HUMAN; ONCOPROTEIN; PEPTIDE FRAGMENT; PROTEIN BINDING; SIGNAL PEPTIDE;

ANIMAL CELL; ARTICLE; BINDING SITE; BONE MARROW; CELL DIFFERENTIATION; CHROMATIN; CHROMATIN IMMUNOPRECIPITATION; CONTROLLED STUDY; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; ISOTHERMAL TITRATION CALORIMETRY; LEUKEMIA; MIXED LINEAGE LEUKEMIA; MOUSE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; POINT MUTATION; PROTEIN EXPRESSION; PROTEIN PURIFICATION; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; ANIMAL; C57BL MOUSE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; GENETICS; HEK293 CELL LINE; HIV INFECTIONS; HUMAN; IMMUNOPRECIPITATION; LEUKEMIA, BIPHENOTYPIC, ACUTE; METABOLISM; MOLECULARLY TARGETED THERAPY; MUTATION; PROTEIN TERTIARY STRUCTURE;

ANIMALS; BINDING SITES; HEK293 CELLS; HISTONE-LYSINE N-METHYLTRANSFERASE; HIV INFECTIONS; HIV INTEGRASE; HUMANS; IMMUNOPRECIPITATION; INTERCELLULAR SIGNALING PEPTIDES AND PROTEINS; LEUKEMIA, BIPHENOTYPIC, ACUTE; MAGNETIC RESONANCE SPECTROSCOPY; MICE, INBRED C57BL; MODELS, MOLECULAR; MOLECULAR TARGETED THERAPY; MUTATION; MYELOID-LYMPHOID LEUKEMIA PROTEIN; PEPTIDE FRAGMENTS; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTO-ONCOGENE PROTEINS;

EID: 84919628704     PISSN: 00064971     EISSN: 15280020     Source Type: Journal    
DOI: 10.1182/blood-2014-01-550079     Document Type: Article

References (32)

1. Dietz F, Franken S, Yoshida K, Nakamura H, Kappler J, Gieselmann V. The family of hepatoma-derived growth factor proteins: characterization of a new member HRP-4 and classification of its subfamilies. Biochem J. 2002;366(pt 2):491-500.
2. Ge H, Si Y, Roeder RG. Isolation of cDNAs encoding novel transcription coactivators p52 and p75 reveals an alternate regulatory mechanism of transcriptional activation. EMBO J. 1998;17(22):6723-6729.
3. Singh DP, Fatma N, Kimura A, Chylack LT Jr, Shinohara T. LEDGF binds to heat shock and stress-related element to activate the expression of stress-related genes. Biochem Biophys Res Commun. 2001;283(4):943-955.
4. Singh DP, Kimura A, Chylack LT Jr, Shinohara T. Lens epithelium-derived growth factor (LEDGF/p75) and p52 are derived from a single gene by alternative splicing. Gene. 2000;242(1-2):265-273.
5. Hussey DJ, Moore S, Nicola M, Dobrovic A. Fusion of the NUP98 gene with the LEDGF/p52 gene defines a recurrent acute myeloid leukemia translocation. BMC Genet. 2001;2:20.
6. Morerio C, Acquila M, Rosanda C, et al. t(9;11)(p22;p15) with NUP98-LEDGF fusion gene in pediatric acute myeloid leukemia. Leuk Res. 2005;29(4):467-470.
7. Huang TS, Myklebust LM, Kjarland E, et al. LEDGF/p75 has increased expression in blasts from chemotherapy-resistant human acute myelogenic leukemia patients and protects leukemia cells from apoptosis in vitro. Mol Cancer. 2007;6:31.
8. Yokoyama A, Cleary ML. Menin critically links MLL proteins with LEDGF on cancer-associated target genes. Cancer Cell. 2008;14(1):36-46.
9. Llano M, Saenz DT, Meehan A, et al. An essential role for LEDGF/p75 in HIV integration. Science. 2006;314(5798):461-464.
10. Maertens G, Cherepanov P, Pluymers W, et al. LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells. J Biol Chem. 2003;278(35):33528-33539.
11. Cherepanov P, Devroe E, Silver PA, Engelman A. Identification of an evolutionarily conserved domain in human lens epithelium-derived growth factor/transcriptional co-activator p75 (LEDGF/p75) that binds HIV-1 integrase. J Biol Chem. 2004;279(47):48883-48892.
12. De Rijck J, Vandekerckhove L, Gijsbers R, et al. Overexpression of the lens epithelium-derived growth factor/p75 integrase binding domain inhibits human immunodeficiency virus replication. J Virol. 2006;80(23):11498-11509.
13. Christ F, Debyser Z. The LEDGF/p75 integrase interaction, a novel target for anti-HIV therapy. Virology. 2013;435(1):102-109.
14. Christ F, Voet A, Marchand A, et al. Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication. Nat Chem Biol. 2010;6(6):442-448.
15. Christ F, Shaw S, Demeulemeester J, et al. Small-molecule inhibitors of the LEDGF/p75 binding site of integrase block HIV replication and modulate integrase multimerization. Antimicrob Agents Chemother. 2012;56(8):4365-4374.
16. Huang J, Gurung B, Wan B, et al. The same pocket in menin binds both MLL and JUND but has opposite effects on transcription. Nature. 2012;482(7386):542-546.
17. Muntean AG, Tan J, Sitwala K, et al. The PAF complex synergizes with MLL fusion proteins at HOX loci to promote leukemogenesis. Cancer Cell. 2010;17(6):609-621.
18. Grembecka J, Belcher AM, Hartley T, Cierpicki T. Molecular basis of the mixed lineage leukemiamenin interaction: implications for targeting mixed lineage leukemias. J Biol Chem. 2010;285(52):40690-40698.
19. Tugarinov V, Kay LE. Quantitative NMR studies of high molecular weight proteins: application to domain orientation and ligand binding in the 723 residue enzyme malate synthase G. J Mol Biol. 2003;327(5):1121-1133.
20. Güntert P. Automated NMR structure calculation with CYANA. Methods Mol Biol. 2004;278:353-378.
21. Shen Y, Delaglio F, Cornilescu G, Bax A. TALOS+: a hybrid method for predicting protein backbone torsion angles from NMR chemical shifts. J Biomol NMR. 2009;44(4):213-223.
22. Wang J, Muntean AG, Hess JL. ECSASB2 mediates MLL degradation during hematopoietic differentiation. Blood. 2012;119(5):1151-1161.
23. Liu Y, Chen W, Gaudet J, et al. Structural basis for recognition of SMRT/N-CoR by the MYND domain and its contribution to AML1/ETO's activity. Cancer Cell. 2007;11(6):483-497.
24. Leach BI, Kuntimaddi A, Schmidt CR, Cierpicki T, Johnson SA, Bushweller JH. Leukemia fusion target AF9 is an intrinsically disordered transcriptional regulator that recruits multiple partners via coupled folding and binding. Structure. 2013;21(1):176-183.
25. Yokoyama A, Somervaille TC, Smith KS, Rozenblatt-Rosen O, Meyerson M, Cleary ML. The menin tumor suppressor protein is an essential oncogenic cofactor for MLL-associated leukemogenesis. Cell. 2005;123(2):207-218.
26. Cherepanov P, Ambrosio AL, Rahman S, Ellenberger T, Engelman A. Structural basis for the recognition between HIV-1 integrase and transcriptional coactivator p75. Proc Natl Acad Sci USA. 2005;102(48):17308-17313.
27. Vandegraaff N, Devroe E, Turlure F, Silver PA, Engelman A. Biochemical and genetic analyses of integrase-interacting proteins lens epithelium-derived growth factor (LEDGF)/p75 and hepatoma-derived growth factor related protein 2 (HRP2) in preintegration complex function and HIV-1 replication. Virology. 2006;346(2):415-426.
28. Méreau H, De Rijck J, Cermáková K, et al. Impairing MLL-fusion gene-mediated transformation by dissecting critical interactions with the lens epithelium-derived growth factor (LEDGF/p75). Leukemia. 2013;27(6):1245-1253.
29. Grembecka J, He S, Shi A, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nat Chem Biol. 2012;8(3):277-284.
30. Shi A, Murai MJ, He S, et al. Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia. Blood. 2012;120(23):4461-4469.
31. Marx SJ. Molecular genetics of multiple endocrine neoplasia types 1 and 2. Nat Rev Cancer. 2005;5(5):367-375.
32. Hombrouck A, De Rijck J, Hendrix J, et al. Virus evolution reveals an exclusive role for LEDGF/p75 in chromosomal tethering of HIV. PLoS Pathog. 2007;3(3):e47.