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ACS Medicinal Chemistry Letters
entering proteomic frontier. Curr. Top. Med. Chem. 2002,
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AUTHORS INFORMATION
Corresponding Author
*(M.S.) Phone: +39 079-228-753. Fax: +39 079-229-559. E-
7) Robinette, D.; Neamati, N.; Tomer, K. B.; Borchers, C. H.
Photoaffinity labeling combined with mass spectrometric
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approaches for identifying target proteins and elucidating
the structure of a ligand-binding region using carbene-
generating photoreactive probes. Anal. Sci. 2006, 22, 209-
218
ORCID:
Nicolino Pala: 0000-0002-9681-5233
Francesca Esposito: 0000-0001-9725-7977
Enzo Tramontano: 0000-0002-4849-0980
Pankaj Kumar Singh: 0000-0002-4774-6358
Vanna Sanna: 0000-0001-9068-349
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in biochemistry. Biochem. 1994, 33, 5661-5673
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Therapy Curr. Opin. HIV AIDS 2012, 7, 383–389
12) Pommier, Y.; Johnson, A. A.; Marchand, C. Integrase
inhibitors to treat HIV/AIDS. Nat. Rev. Drug
Discovery 2005, 4, 236– 248
Mauro Carcelli: 0000-0001-5888-4556
Mario Sechi: 0000-0003-2983-6090
Author Contributions
13) Li,
A. Structural
integration. Virology 2011, 411, 194– 205
X.; Krishnan,
L.; Cherepanov,
P.; Engelman,
DNA
biology
of
retroviral
This work was done through contributions of all authors. All
authors have given approval to the final version of the
manuscript.
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HIV-1 integrase with strand transfer inhibitors. Drug
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Stillmock, K.; Grobler, J. A.; Espeseth, A.; Gabryelski, L.;
Schleif, W.; Blau, C.; Miller, M. D. Inhibitors of strand
transfer that prevent integration and inhibit HIV-1
replication in cells. Science 2000, 287, 646−650
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HIV-1 integrase. Future Science OA 2018, 4 (9) , FSO338.
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design. In: HIV-1 Integrase: Mechanism of Action and
Inhibitor Design. Wiley Series in Drug Discovery and
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20) Rogolino, D., Carcelli, M., Sechi, M., and Neamati, N.
Viral enzymes containing magnesium: metal binding as a
successful strategy in drug design. Coord. Chem.
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DNA Integration. Chem. Rev. 2016, 116, 12730−12757
22) Grobler, J. A.; Stillmock, K.; Binghua, H.; Witmer, M.;
Felock, P.; Espeseth, A. S.; Wolfe, A.; Egbertson, M.;
Bourgeois, M,; Melamed, J.; Wai, J. S.; Young, S.; Vacca,
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Design and Synthesis of Photoactivatable Aryl Diketo
Acid-Containing HIV-1 Integrase Inhibitors as Potential
Affinity Probes. Bioorg. Med. Chem. Lett. 2004, 14, 1205-
2007
Notes
The authors have the great pleasure to celebrate the 10th years
of the ACS Med. Chem. Letters on the Special Issue
“Medicinal Chemistry: From Targets to Therapies”. The
authors declare no competing financial interest.
ACKNOWLEDGMENT
The authors are grateful to Schrödinger Team for the
opportunity to evaluate a trial of the latest version of software
Maestro.
ABBREVIATIONS
HIV-1, Human Immunodeficiency Virus-1; IN, Integrase;
PAL, Photoaffinity Labeling; HAART, Highly Active
Antiretroviral Therapy; CCD, catalytic core domain; RAL,
Raltegravir; WB, Western-Blotting; SBDD, structure-based
drug design; DKAs, β-diketo acids; cDNA; dexoxyribonuleic
acid; ST, strand transfer; SDS-PAGE, Sodium Dodecyl
Sulphate - PolyAcrylamide Gel Electrophoresis; LEDGF,
Lens epithelium-derived growth factor; RMSD, Root-mean-
square deviation.
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