Daniel Appella, Ph.D.

Section Chief: Synthetic Bioactive Molecules Section, Laboratory of Bioorganic Chemistry

Scientific Focus Areas: Chemical Biology

appellad@niddk.nih.gov 301-451-1052 Add to Contacts

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Publications

A selection of recent and significant publications can be viewed below.

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Preclinical evaluation of a mercaptobenzamide and its prodrug for NCp7-targeted inhibition of human immunodeficiency virus.

Hartman TL, Yang L, Helfrick AN, Hassink M, Shank NI, George Rosenker K, Scerba MT, Saha M, Hughes E, Wang AQ, Xu X, Gupta P, Buckheit RW Jr, Appella DH.

Antiviral Res (2016 Oct) 134:216-225. Abstract/Full Text

Reaction Kinetics Direct a Rational Synthesis of an HIV-1 Inactivator of Nucleocapsid Protein 7 and Provide Mechanistic Insight into Cellular Metabolism and Antiviral Activity.

Nikolayevskiy H, Scerba MT, Deschamps JR, Appella DH.

Chemistry (2018 Jul 5) 24:9485-9489. Abstract/Full Text

Programmable nanoscaffolds that control ligand display to a G-protein-coupled receptor in membranes to allow dissection of multivalent effects.

Dix AV, Moss SM, Phan K, Hoppe T, Paoletta S, Kozma E, Gao ZG, Durell SR, Jacobson KA, Appella DH.

J Am Chem Soc (2014 Sep 3) 136:12296-303. Abstract/Full Text

Probing Mercaptobenzamides as HIV Inactivators via Nucleocapsid Protein 7.

Saha M, Scerba MT, Shank NI, Hartman TL, Buchholz CA, Buckheit RW Jr, Durell SR, Appella DH.

ChemMedChem (2017 May 22) 12:714-721. Abstract/Full Text

Quantification of plasma HIV RNA using chemically engineered peptide nucleic acids.

Zhao C, Hoppe T, Setty MK, Murray D, Chun TW, Hewlett I, Appella DH.

Nat Commun (2014 Oct 6) 5:5079. Abstract/Full Text

Additional Publications

Chemical Features Important for Activity in a Class of Inhibitors Targeting the Wip1 Flap Subdomain.

Tagad HD, Debnath S, Clausse V, Saha M, Mazur SJ, Appella E, Appella DH.

ChemMedChem (2018 May 8) 13:894-901. Abstract/Full Text

Multivalent LKγ-PNA oligomers bind to a human telomere DNA G-rich sequence to form quadruplexes.

Gupta P, Rastede EE, Appella DH.

Bioorg Med Chem Lett (2015 Nov 1) 25:4757-4760. Abstract/Full Text

An Intravaginal Ring for the Simultaneous Delivery of an HIV-1 Maturation Inhibitor and Reverse-Transcriptase Inhibitor for Prophylaxis of HIV Transmission.

Ugaonkar SR, Clark JT, English LB, Johnson TJ, Buckheit KW, Bahde RJ, Appella DH, Buckheit RW Jr, Kiser PF.

J Pharm Sci (2015 Oct) 104:3426-39. Abstract/Full Text

G-quadruplex formation between G-rich PNA and homologous sequences in oligonucleotides and supercoiled plasmid DNA.

Gaynutdinov TI, Englund EA, Appella DH, Onyshchenko MI, Neumann RD, Panyutin IG.

Nucleic Acid Ther (2015 Apr) 25:78-84. Abstract/Full Text

PNA-Based Multivalent Scaffolds Activate the Dopamine D2 Receptor.

Dix AV, Conroy JL, George Rosenker KM, Sibley DR, Appella DH.

ACS Med Chem Lett (2015 Apr 9) 6:425-9. Abstract/Full Text

PPG peptide nucleic acids that promote DNA guanine quadruplexes.

Englund EA, Gupta P, Micklitsch CM, Onyshchenko MI, Remeeva E, Neumann RD, Panyutin IG, Appella DH.

Chembiochem (2014 Sep 5) 15:1887-90. Abstract/Full Text

Recognition of HIV-TAR RNA using neomycin-benzimidazole conjugates.

Ranjan N, Kumar S, Watkins D, Wang D, Appella DH, Arya DP.

Bioorg Med Chem Lett (2013 Oct 15) 23:5689-93. Abstract/Full Text

Novel inhibitors of a Grb2 SH3C domain interaction identified by a virtual screen.

Simister PC, Luccarelli J, Thompson S, Appella DH, Feller SM, Hamilton AD.

Bioorg Med Chem (2013 Jul 15) 21:4027-33. Abstract/Full Text

Cyclopentane-peptide nucleic acids for qualitative, quantitative, and repetitive detection of nucleic acids.

Micklitsch CM, Oquare BY, Zhao C, Appella DH.

Anal Chem (2013 Jan 2) 85:251-7. Abstract/Full Text

Click dimers to target HIV TAR RNA conformation.

Kumar S, Kellish P, Robinson WE Jr, Wang D, Appella DH, Arya DP.

Biochemistry (2012 Mar 20) 51:2331-47. Abstract/Full Text

Programmable multivalent display of receptor ligands using peptide nucleic acid nanoscaffolds.

Englund EA, Wang D, Fujigaki H, Sakai H, Micklitsch CM, Ghirlando R, Martin-Manso G, Pendrak ML, Roberts DD, Durell SR, Appella DH.

Nat Commun (2012 Jan 10) 3:614. Abstract/Full Text

Combinatorial Synthesis, Screening, and Binding Studies of Highly Functionalized Polyamino-amido Oligomers for Binding to Folded RNA.

Pokorski JK, Appella DH.

J Nucleic Acids (2012) 2012:971581. Abstract/Full Text

Quadruplex formation is necessary for stable PNA invasion into duplex DNA of BCL2 promoter region.

Onyshchenko MI, Gaynutdinov TI, Englund EA, Appella DH, Neumann RD, Panyutin IG.

Nucleic Acids Res (2011 Sep 1) 39:7114-23. Abstract/Full Text

A one-pot preparation of N-2-mercaptobenzoyl-amino amides.

Bahde RJ, Appella DH, Trenkle WC.

Tetrahedron Lett (2011 Aug 10) 52:4103-4105. Abstract/Full Text

Optimization of a cyclic peptide inhibitor of Ser/Thr phosphatase PPM1D (Wip1).

Hayashi R, Tanoue K, Durell SR, Chatterjee DK, Jenkins LM, Appella DH, Appella E.

Biochemistry (2011 May 31) 50:4537-49. Abstract/Full Text

Methoxyethylamino-numonafide is an efficacious and minimally toxic amonafide derivative in murine models of human cancer.

Liu Y, Norton JT, Witschi MA, Xu Q, Lou G, Wang C, Appella DH, Chen Z, Huang S.

Neoplasia (2011 May) 13:453-60. Abstract/Full Text

Inhibition of multidrug resistance by SV40 pseudovirion delivery of an antigene peptide nucleic acid (PNA) in cultured cells.

Macadangdang B, Zhang N, Lund PE, Marple AH, Okabe M, Gottesman MM, Appella DH, Kimchi-Sarfaty C.

PLoS One (2011 Mar 22) 6:e17981. Abstract/Full Text

Small-molecule inactivation of HIV-1 NCp7 by repetitive intracellular acyl transfer.

Miller Jenkins LM, Ott DE, Hayashi R, Coren LV, Wang D, Xu Q, Schito ML, Inman JK, Appella DH, Appella E.

Nat Chem Biol (2010 Dec) 6:887-9. Abstract/Full Text

Multivalent binding oligomers inhibit HIV Tat-TAR interaction critical for viral replication.

Wang D, Iera J, Baker H, Hogan P, Ptak R, Yang L, Hartman T, Buckheit RW Jr, Desjardins A, Yang A, Legault P, Yedavalli V, Jeang KT, Appella DH.

Bioorg Med Chem Lett (2009 Dec 15) 19:6893-7. Abstract/Full Text

Stabilization of G-quadruplex in the BCL2 promoter region in double-stranded DNA by invading short PNAs.

Onyshchenko MI, Gaynutdinov TI, Englund EA, Appella DH, Neumann RD, Panyutin IG.

Nucleic Acids Res (2009 Dec) 37:7570-80. Abstract/Full Text

Synthesis and anticancer activities of 6-amino amonafide derivatives.

Norton JT, Witschi MA, Luong L, Kawamura A, Ghosh S, Stack MS, Sim E, Avram MJ, Appella DH, Huang S.

Anticancer Drugs (2008 Jan) 19:23-36. Abstract/Full Text

Colorimetric detection of anthrax DNA with a Peptide nucleic acid sandwich-hybridization assay.

Zhang N, Appella DH.

J Am Chem Soc (2007 Jul 11) 129:8424-5. Abstract/Full Text

Gamma-substituted peptide nucleic acids constructed from L-lysine are a versatile scaffold for multifunctional display.

Englund EA, Appella DH.

Angew Chem Int Ed Engl (2007) 46:1414-8. Abstract/Full Text