Macromolecular Crystallography Laboratory, Protein Structure Section at the NCI-Frederick campus.

Review articles

Asante-Appiah E, Skalka AM. Molecular mechanisms in retrovirus DNA integration.
Antiviral Res 1997 Dec; 36(3): 139-156.

Andrake MD, et al. Retroviral integrase, putting the pieces together.
J Biol Chem. 1996 Aug 16; 271(33): 19633-19636.

Rice P, et al. Retroviral integrases and their cousins.
Curr Opin Struct Biol. 1996 Feb; 6(1): 76-83.

Yang W, et al. Recombining the structures of HIV integrase, RuvC and RNase H.
Structure. 1995 Feb 15; 3(2): 131-134.

Link to an excellent site, http://www-micro.msb.le.ac.uk/335/Retroviruses.html, at Leicester University Department of Microbiology and Immunology with a discussion of retroviruses. (This is not a review article, but it is very good.)

Here's another excellent review article at http://nmrweb.ncifcrf.gov/abl/mvcl/pavlab10.html from the Pavlakis lab. here at NCI-FCRDC. It was published in the book AIDS: Biology, Diagnosis, Treatment and Prevention, 4th Edition VT DeVita Jr, S Hellman, and SA Rosenberg, editors, Lippincott-Raven Publishers, pp. 45-74, 1997.

Research articles

Sayasith K, et al. Characterization of mutant HIV-1 integrase carrying amino acid changes in the catalytic domain.
Mol Cells. 2000 Oct 31;10(5):525-32.

Chen IJ, et al. Identification of HIV-1 integrase inhibitors via three-dimensional database searching using ASV and HIV-1 integrases as targets.
Bioorg Med Chem. 2000 Oct;8(10):2385-98.

Espeseth AS, et al. HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase.
Proc Natl Acad Sci U S A. 2000 Oct 10;97(21):11244-9.

Skinner LM, et al. Nucleophile selection for the endonuclease activities of human, ovine, and avian retroviral integrases.
J Biol Chem. 2000 Oct 6 [epub ahead of print] 276(1) Jan 5, pp.114-124, 2001

Depienne C, et al. Cellular distribution and karyophilic properties of matrix, integrase, and vpr proteins from the human and simian immunodeficiency viruses.
Exp Cell Res. 2000 Nov 1;260(2):387-95.

Wang T, et al. Major and minor groove contacts in retroviral integrase-LTR interactions.
Biochemistry 1999 Mar 23;38(12):3624-32.

Greenwald J, et al. The mobility of an HIV-1 integrase active site loop is correlated with catalytic activity.
Biochemistry 1999 Jul 13;38(28):8892-8 .

Asante-Appiah E, et al. HIV-1 integrase: structural organization, conformational changes, and catalysis.
Adv Virus Res 1999;52:351-369.

Gerton JL, et al. Effects of mutations in residues near the active site of human immunodeficiency virus type 1 integrase on specific enzyme-substrate interactions.
J Virol 1998 Jun;72(6):5046-5055.

Katz RA, et al. A preferred target DNA structure for retroviral integrase in vitro.
J Biol Chem 1998 Sep 11;273(37):24190-24195.

Maignan S, et al. Crystal structures of the catalytic domain of HIV-1 integrase free and complexed with its metal cofactor: high level of similarity of the active site with other viral integrases.
J Mol Biol 1998 Sep 18;282(2):359-368.

McCord M, et al. Purification of recombinant Rous sarcoma virus integrase possessing physical and catalytic properties similar to virion-derived integrase.
Protein Expr Purif 1998 Nov;14(2):167-177.

Goldgur Y, et al. Three new structures of the core domain of HIV-1 integrase: an active site that binds magnesium.
Proc Natl Acad Sci U S A 1998 Aug 4;95(16):9150-9154

McDougall B, et al. Dicaffeoylquinic and dicaffeoyltartaric acids are selective inhibitors of human immunodeficiency virus type 1 integrase.
Antimicrob Agents Chemother 1998 Jan;42(1):140-146.

Katzman M, Sudol M. Mapping viral DNA specificity to the central region of integrase by using functional human immunodeficiency virus type 1/visna virus chimeric proteins.
J Virol 1998 Mar;72(3):1744-1753.

Jenkins TM, et al. Critical contacts between HIV-1 integrase and viral DNA identified by structure-based analysis and photo-crosslinking.
EMBO J 1997 Nov 17;16(22):6849-6859.

Drake RR, et al. Identification of a nucleotide binding site in HIV-1 integrase.
Proc Natl Acad Sci U S A 1998 Apr 14;95(8):4170-4175 .

Carteau S, et al. Human immunodeficiency virus type 1 nucleocapsid protein specifically stimulates Mg2+-dependent DNA integration in vitro.
J Virol 1997 Aug;71(8):6225-6229.

Dyda F, et al. Crystal structure of the catalytic domain of HIV-1 integrase: similarity to other polynucleotidyl transferases.
Science. 1994 Dec 23; 266(5193): 1981-1986.

Asante-Appiah E, et al. A metal-induced conformational change and activation of HIV-1 integrase.
J Biol Chem. 1997 Jun 27; 272(26): 16196-16205.

Hickman AB, et al. Biophysical and enzymatic properties of the catalytic domain of HIV-1 integrase.
J Biol Chem. 1994 Nov 18; 269(46): 29279-29287.

Andrake MD, et al. Multimerization determinants reside in both the catalytic core and C terminus of avian sarcoma virus integrase.
J Biol Chem. 1995 Dec 8; 270(49): 29299-29306.

Mazumder A, et al. Chemical trapping of ternary complexes of human immunodeficiency virus type 1 integrase, divalent metal, and DNA substrates containing an abasic site. Implications for the role of lysine 136 in DNA binding.
J Biol Chem. 1996 Nov 1; 271(44): 27330-27338.

Hickman AB, et al. Molecular organization in site-specific recombination: the catalytic domain of bacteriophage HP1 integrase at 2.7 Å resolution.
Cell. 1997 Apr 18; 89(2): 227-237.

Engelman A, et al. Structure-based mutagenesis of the catalytic domain of human immunodeficiency virus type 1 integrase.
J Virol. 1997 May; 71(5): 3507-3514.

Kulkosky J, et al. Activities and substrate specificity of the evolutionarily conserved central domain of retroviral integrase.
Virology. 1995 Jan 10; 206(1): 448-456.

Mazumder A, et al. Inhibition of the human immunodeficiency virus type 1 integrase by guanosine quartet structures.
Biochemistry. 1996 Oct 29; 35(43): 13762-13771.

Kukolj G, et al. Enhanced and coordinated processing of synapsed viral DNA ends by retroviral integrases in vitro.
Genes Dev. 1995 Oct 15; 9(20): 2556-2567.

Zheng R, et al. Zinc folds the N-terminal domain of HIV-1 integrase, promotes multimerization, and enhances catalytic activity.
Proc Natl Acad Sci U S A. 1996 Nov 26; 93(24): 13659-13664.

Rice P, et al. Structure of the bacteriophage Mu transposase core: a common structural motif for DNA transposition and retroviral integration.
Cell. 1995 Jul 28; 82(2): 209-220.

Vipond IB, et al. Divalent metal ions at the active sites of the EcoRV and EcoRI restriction endonucleases.
Biochemistry. 1995 Jan 17; 34(2): 697-704.

Shibagaki Y, et al. Central core domain of retroviral integrase is responsible for target site selection.
J Biol Chem. 1997 Mar 28; 272(13): 8361-8369.

Hazuda DJ, et al. Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase.
J Virol. 1997 Sep; 71(9): 7005-7011.

Neamati N, et al. Potent inhibitors of human immunodeficiency virus type 1 integrase: identification of a novel four-point pharmacophore and tetracyclines as novel inhibitors.
Mol Pharmacol. 1997 Dec; 52(6): 1041-1055.

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If you have questions or comments about the Integrase Project web site,
contact: Jerry N. Alexandratos at alexandr@ncifcrf.gov.