Our Science – Marchand Website

Christophe Marchand, Ph.D.

Selected Publications

1) Marchand C, Lea WA, Jadhav A, Dexheimer TS, Austin CP, Inglese J, Pommier Y, Simeonov A.
Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay.
Mol. Cancer Ther. 8: 240-8, 2009. [Journal]

2) Marinello J, Marchand C, Mott BT, Bain A, Thomas CJ, Pommier Y.
Comparison of raltegravir and elvitegravir on HIV-1 integrase catalytic reactions and on a series of drug-resistant integrase mutants.
Biochemistry. 47: 9345-54, 2008. [Journal]

3) Di Santo R, Costi R, Roux A, Miele G, Crucitti GC, Iacovo A, Rosi F, Lavecchia A, Marinelli L, Di Giovanni C, Novellino E, Palmisano L, Andreotti M, Amici R, Galluzzo CM, Nencioni L, Palamara AT, Pommier Y, Marchand C.
Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities.
J. Med. Chem. 51: 4744-50, 2008. [Journal]

4) Dexheimer TS, Antony S, Marchand C, Pommier Y.
Tyrosyl-DNA Phosphodiesterase as a Target for Anticancer Therap.
Anti-cancer agents in medicinal chemistry. 8: 381-9, 2008. [Journal]

5) Zhao XZ, Semenova EA, Vu BC, Maddali K, Marchand C, Hughes SH, Pommier Y, Burke TR.
2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors.
J. Med. Chem. 51: 251-9, 2008. [Journal]

6) Semenova EA, Marchand C, Pommier Y.
HIV-1 Integrase Inhibitors: Update and Perspectives.
Adv. Pharmacol. 56: 199-228, 2008. [Journal]

7) Marchand C, Beutler JA, Wamiru A, Budihas S, Möllmann U, Heinisch L, Mellors JW, Le Grice SF, Pommier Y.
Madurahydroxylactone Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and RNase H.
Antimicrob. Agents Chemother. 52: 361-4, 2008. [Journal]

8) Liao C, Karki RG, Marchand C, Pommier Y, Nicklaus MC.
Virtual screening application of a model of full-length HIV-1 integrase complexed with viral DNA.
Bioorg Med Chem Lett. 2007. [Journal]

9) Antony S, Marchand C, Stephen AG, Thibaut L, Agama KK, Fisher RJ, Pommier Y.
Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1.
Nucleic Acids Res. 35: 4474-84, 2007. [Journal]

10) Johnson AA, Marchand C, Patil SS, Costi R, Di Santo R, Burke TR, Pommier Y.
Probing HIV-1 integrase inhibitor binding sites with position-specific integrase-DNA cross-linking assays.
Mol. Pharmacol. 71: 893-901, 2007. [Journal]

11) Bona R, Andreotti M, Buffa V, Leone P, Galluzzo CM, Amici R, Palmisano L, Mancini MG, Michelini Z, Di Santo R, Costi R, Roux A, Pommier Y, Marchand C, Vella S, Cara A.
Development of a human immunodeficiency virus vector-based, single-cycle assay for evaluation of anti-integrase compounds.
Antimicrob. Agents Chemother. 50: 3407-17, 2006. [Journal]

12) Marchand C, Krajewski K, Lee HF, Antony S, Johnson AA, Amin R, Roller P, Kvaratskhelia M, Pommier Y.
Covalent binding of the natural antimicrobial peptide indolicidin to DNA abasic sites.
Nucleic Acids Res. 34: 5157-65, 2006. [Journal]

13) Pommier Y, Barcelo JM, Rao VA, Sordet O, Jobson AG, Thibaut L, Miao ZH, Seiler JA, Zhang H, Marchand C, Agama K, Nitiss JL, Redon C.
Repair of topoisomerase I-mediated DNA damage.
Prog. Nucleic Acid Res. Mol. Biol. 81: 179-229, 2006. [Journal]

14) Di Santo R, Costi R, Roux A, Artico M, Lavecchia A, Marinelli L, Novellino E, Palmisano L, Andreotti M, Amici R, Galluzzo CM, Nencioni L, Palamara AT, Pommier Y, Marchand C.
Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action.
J. Med. Chem. 49: 1939-45, 2006. [Journal]

15) Marchand C, Antony S, Kohn KW, Cushman M, Ioanoviciu A, Staker BL, Burgin AB, Stewart L, Pommier Y.
A novel norindenoisoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex.
Mol. Cancer Ther. 5: 287-95, 2006. [Journal]

16) Semenova EA, Johnson AA, Marchand C, Davis DA, Yarchoan R, Pommier Y.
Preferential inhibition of the magnesium-dependent strand transfer reaction of HIV-1 integrase by alpha-hydroxytropolones.
Mol. Pharmacol. 69: 1454-60, 2006. [Journal]

17) Johnson AA, Santos W, Pais GC, Marchand C, Amin R, Burke TR, Verdine G, Pommier Y.
Integration requires a specific interaction of the donor DNA terminal 5'-cytosine with glutamine 148 of the HIV-1 integrase flexible loop.
J. Biol. Chem. 281: 461-7, 2006. [Journal]

18) Pommier Y, Marchand C.
Interfacial inhibitors of protein-nucleic acid interactions.
Current medicinal chemistry. Anti-cancer agents. 5: 421-9, 2005. [Journal]

19) Di Santo R, Costi R, Artico M, Ragno R, Greco G, Novellino E, Marchand C, Pommier Y.
Design, synthesis and biological evaluation of heteroaryl diketohexenoic and diketobutanoic acids as HIV-1 integrase inhibitors endowed with antiretroviral activity.
Farmaco. 60: 409-17, 2005. [Journal]

20) Pommier Y, Johnson AA, Marchand C.
Integrase inhibitors to treat HIV/AIDS.
Nature reviews. Drug discovery. 4: 236-48, 2005. [Journal]

21) Krajewski K, Marchand C, Long YQ, Pommier Y, Roller PP.
Synthesis and HIV-1 integrase inhibitory activity of dimeric and tetrameric analogs of indolicidin.
Bioorg. Med. Chem. Lett. 14: 5595-8, 2004. [Journal]

22) Johnson AA, Marchand C, Pommier Y.
HIV-1 integrase inhibitors: a decade of research and two drugs in clinical trial.
Current topics in medicinal chemistry. 4: 1059-77, 2004. [Journal]

23) Svarovskaia ES, Barr R, Zhang X, Pais GC, Marchand C, Pommier Y, Burke TR, Pathak VK.
Azido-containing diketo acid derivatives inhibit human immunodeficiency virus type 1 integrase in vivo and influence the frequency of deletions at two-long-terminal-repeat-circle junctions.
J. Virol. 78: 3210-22, 2004. [Journal]

24) Zhang X, Marchand C, Pommier Y, Burke TR.
Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes.
Bioorg. Med. Chem. Lett. 14: 1205-7, 2004. [Journal]

25) Krajewski K, Long YQ, Marchand C, Pommier Y, Roller PP.
Design and synthesis of dimeric HIV-1 integrase inhibitory peptides.
Bioorg. Med. Chem. Lett. 13: 3203-5, 2003. [Journal]

26) Zhang X, Pais GC, Svarovskaia ES, Marchand C, Johnson AA, Karki RG, Nicklaus MC, Pathak VK, Pommier Y, Burke TR.
Azido-containing aryl beta-diketo acid HIV-1 integrase inhibitors.
Bioorg. Med. Chem. Lett. 13: 1215-9, 2003. [Journal]

27) Pais GC, Zhang X, Marchand C, Neamati N, Cowansage K, Svarovskaia ES, Pathak VK, Tang Y, Nicklaus M, Pommier Y, Burke TR.
Structure activity of 3-aryl-1,3-diketo-containing compounds as HIV-1 integrase inhibitors.
J. Med. Chem. 45: 3184-94, 2002. [Journal]

28) Marchand C, Zhang X, Pais GC, Cowansage K, Neamati N, Burke TR, Pommier Y.
Structural determinants for HIV-1 integrase inhibition by beta-diketo acids.
J. Biol. Chem. 277: 12596-603, 2002. [Journal]

29) Marchand C, Pourquier P, Laco GS, Jing N, Pommier Y.
Interaction of human nuclear topoisomerase I with guanosine quartet-forming and guanosine-rich single-stranded DNA and RNA oligonucleotides.
J. Biol. Chem. 277: 8906-11, 2002. [Journal]

30) Jing N, Marchand C, Guan Y, Liu J, Pallansch L, Lackman-Smith C, De Clercq E, Pommier Y.
Structure-activity of inhibition of HIV-1 integrase and virus replication by G-quartet oligonucleotides.
DNA Cell Biol. 20: 499-508, 2001. [Journal]

31) Marchand C, Neamati N, Pommier Y.
In vitro human immunodeficiency virus type 1 integrase assays.
Meth. Enzymol. 340: 624-33, 2001. [Journal]

32) Pilon AA, Marchand C, Kavlick MF, Bajaj K, Owen J, Mitsuya H, Pommier Y.
Mutations in the HIV type 1 integrase of patients receiving long-term dideoxynucleoside therapy do not confer resistance to zidovudine.
AIDS Res. Hum. Retroviruses. 16: 1417-22, 2000. [Journal]

33) Neamati N, Marchand C, Pommier Y.
HIV-1 integrase inhibitors: past, present, and future.
Adv. Pharmacol. 49: 147-65, 2000. [Journal]

34) Pommier Y, Marchand C, Neamati N.
Retroviral integrase inhibitors year 2000: update and perspectives.
Antiviral Res. 47: 139-48, 2000. [Journal]

35) Pluymers W, Neamati N, Pannecouque C, Fikkert V, Marchand C, Burke TR, Pommier Y, Schols D, De Clercq E, Debyser Z, Witvrouw M.
Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters.
Mol. Pharmacol. 58: 641-8, 2000. [Journal]

36) Marchand C, Nguyen CH, Ward B, Sun JS, Bisagni E, Garestier T, Hélène C.
A new family of sequence-specific DNA-cleaving agents directed by triple-helical structures: benzopyridoindole-EDTA conjugates.
Chemistry (Weinheim an der Bergstrasse, Germany). 6: 1559-63, 2000. [Journal]

37) Jing N, Marchand C, Liu J, Mitra R, Hogan ME, Pommier Y.
Mechanism of inhibition of HIV-1 integrase by G-tetrad-forming oligonucleotides in Vitro.
J. Biol. Chem. 275: 21460-7, 2000. [Journal]

38) Zain R, Marchand C, Sun J, Nguyen CH, Bisagni E, Garestier T, Hélène C.
Design of a triple-helix-specific cleaving reagent.
Chem. Biol. 6: 771-7, 1999. [Journal]

39) Marchand C, Sun JS, Bailly C, Waring MJ, Garestier T, Hélène C.
Optimization of alternate-strand triple helix formation at the 5'CpG3' and 5'GpC3' junction steps.
Biochemistry. 37: 13322-9, 1998. [Journal]

40) Marchand C, Bailly C, Nguyen CH, Bisagni E, Garestier T, Hélène C, Waring MJ.
Stabilization of triple helical DNA by a benzopyridoquinoxaline intercalator.
Biochemistry. 35: 5022-32, 1996. [Journal]

41) Bailly C, Marchand C, Hung Nguyen C, Bisagni E, Garestier T, Hélène C, Waring MJ.
Localized chemical reactivity in double-stranded DNA associated with the intercalative binding of benzo[e]pyridoindole and benzo[g]pyridoindole triple-helix-stabilizing ligands.
Eur. J. Biochem. 232: 66-76, 1995. [Journal]

42) Zhou BW, Marchand C, Asseline U, Thuong NT, Sun JS, Garestier T, Hélène C.
Recognition of alternating oligopurine/oligopyrimidine tracts of DNA by oligonucleotides with base-to-base linkages.
Bioconjug. Chem. 6: 516-23, 1995. [Journal]

43) Marchand C, Bailly C, McLean MJ, Moroney SE, Waring MJ.
The 2-amino group of guanine is absolutely required for specific binding of the anti-cancer antibiotic echinomycin to DNA.
Nucleic Acids Res. 20: 5601-6, 1992. [Journal]

44) Pommier Y, Marchand C, Simeonov A, Dexheimer T, Lea W, Inglese J, Austin C, Jadhav A, inventor; DHHS, assignee.
Protein tyrosine phosphatase inhibitors of human tyrosyl-DNA phosphodiesterase (Tdp1) and methods of treating disorders.
US Patent: 61/042,706. 2008. E-Number: E-121-2008. [Patent]

45) Pommier Y, Marchand C, Semenova E, inventor; DHHS, assignee.
Discovery of stilbenedisulfonic acid derivatives as inhibitors of HIV-1 integrase that can be used for the treatment of retroviral infection including AIDS.
US Patent: 60/849,718. 2006. E-Number: E-264-2006. [Patent]

46) Pommier Y, Marchand C, Thibaut L, inventor; DHHS, assignee.
Diamidines Inhibitors of Human Tyrosyl-DNA Phosphodiesterase (Tdp1) for the Treatment of Cancers.
US Patent: 60/786,604. 2006. E-Number: E-165-2006. [Patent]

47) Pommier Y, Marchand C, Thibaut L, inventor; DHHS, assignee.
Tetracyclines Inhibitors of Human Tyrosyl-DNA Phosphodiesterase (Tdp1) for the Treatment of Cancers.
US Patent: 60/786,746. 2006. E-Number: E-097-2006. [Patent]

48) Pommier Y, Marchand C, Semenova E, Johnson A, inventor; DHHS, assignee.
Discovery of tropolone Inhibitors of HIV-1 Integrase that can be Used for the Treatment of Retroviral Infections, Including AIDS.
US Patent: 60/741,769. 2005. E-Number: E-308-2005. [Patent]

49) Roller P, Marchand C, Krajewski K, Pathak V, Zhang Y, Pommier Y, inventor; DHHS, assignee.
Peptide inhibitors of HIV-1 integrase useful for the treatment of retroviral and HIV infections.
US Patent: 60/534,378. 2004. E-Number: E-039-2004. [Patent]

50) Pommier Y, Marchand C, Di Santo R, Artico M, Costi R, inventor; DHHS, assignee.
Quinolin-4-Ones as Inhibitors of Retroviral Integrase for the Treatment of HIV, AIDS and AIDS- Related Complex (ARC).
US Patent: 10/591,679. 2005. E-Number: E-187-2003. [Patent]

51) Burke T, Zhang X, Pais G, Svarovskaia E, Pathak V, Marchand C, Pommier Y, inventor; DHHS, assignee.
Compounds to Treat HIV Infection and AIDS.
US Patent: 10/497,898. 2002. E-Number: E-317-2001. [Patent]

This page was last updated on 1/14/2009.