About: Synthesis, Binding and Antiviral Properties of Potent Core-Extended Naphthalene Diimides Targeting the HIV-1 Long Terminal Repeat Promoter G-Quadruplexes

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About: Synthesis, Binding and Antiviral Properties of Potent Core-Extended Naphthalene Diimides Targeting the HIV-1 Long Terminal Repeat Promoter G-Quadruplexes Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Synthesis, Binding and Antiviral Properties of Potent Core-Extended Naphthalene Diimides Targeting the HIV-1 Long Terminal Repeat Promoter G-Quadruplexes
Creator	Botti, Silvia Butovskaya, Elena Doria, Filippo Frasson, Ilaria Freccero, Mauro Grande, Vincenzo Lago, Sara Nadai, Matteo Perrone, Rosalba Scalabrin, Matteo Richter, Sara
Source	Medline; PMC
abstract	[Image: see text] We have previously reported that stabilization of the G-quadruplex structures in the HIV-1 long terminal repeat (LTR) promoter suppresses viral transcription. Here we sought to develop new G-quadruplex ligands to be exploited as antiviral compounds by enhancing binding toward the viral G-quadruplex structures. We synthesized naphthalene diimide derivatives with a lateral expansion of the aromatic core. The new compounds were able to bind/stabilize the G-quadruplex to a high extent, and some of them displayed clear-cut selectivity toward the viral G-quadruplexes with respect to the human telomeric G-quadruplexes. This feature translated into low nanomolar anti-HIV-1 activity toward two viral strains and encouraging selectivity indexes. The selectivity depended on specific recognition of LTR loop residues; the mechanism of action was ascribed to inhibition of LTR promoter activity in cells. This is the first example of G-quadruplex ligands that show increased selectivity toward the viral G-quadruplexes and display remarkable antiviral activity.
has issue date	2015-11-24(xsd:dateTime)
bibo:doi	10.1021/acs.jmedchem.5b01283
bibo:pmid	26599611
has license	no-cc
sha1sum (hex)	a7413d2d2f103768cb45b13fc91c8f96568eaccb
schema:url	https://doi.org/10.1021/acs.jmedchem.5b01283
resource representing a document's title	Synthesis, Binding and Antiviral Properties of Potent Core-Extended Naphthalene Diimides Targeting the HIV-1 Long Terminal Repeat Promoter G-Quadruplexes
has PubMed Central identifier	PMC4690987
has PubMed identifier	26599611
schema:publication	J Med Chem
resource representing a document's body	covid:a7413d2d2f103768cb45b13fc91c8f96568eaccb#body_text
is schema:about of	named entity 'HUMAN' named entity 'HIGH' named entity 'HIV-1' named entity 'STRUCTURES' named entity 'RECOGNITION' named entity 'HERE' named entity 'ANTIVIRAL' named entity 'LOW' named entity 'CORE' named entity 'LONG TERMINAL REPEAT' named entity 'NAPHTHALENE DIIMIDE' covid:arg/a7413d2d2f103768cb45b13fc91c8f96568eaccb named entity 'BIND' named entity 'BINDING' named entity 'G-QUADRUPLEXES' named entity 'PROPERTIES' named entity 'INDEXES' named entity 'PROMOTER ACTIVITY' named entity 'SYNTHESIZED' named entity 'LATERAL EXPANSION' named entity 'BINDING' named entity 'HIV-1' named entity 'EXTENDED' named entity 'CORE' named entity 'TARGETING' named entity 'HAVE' named entity 'SELECTIVITY' named entity 'LIGANDS' named entity 'MECHANISM OF ACTION' named entity 'SYNTHESIS' named entity 'ANTIVIRAL' named entity 'PROMOTER' named entity 'VIRAL TRANSCRIPTION' named entity 'NEW' named entity 'ANTI-HIV-1 ACTIVITY' named entity 'DISPLAY' named entity 'ENHANCING' named entity 'G-QUADRUPLEXES' named entity 'EXTENT' named entity 'VIRAL' named entity 'DISPLAYED' named entity 'LOOP' named entity 'PREVIOUSLY' named entity 'RESPECT' named entity 'LONG TERMINAL REPEAT' named entity 'NAPHTHALENE' named entity 'PROMOTER' named entity 'DIIMIDES' named entity 'SUPPRESSES' named entity 'STABILIZATION' named entity 'CUT' named entity 'INCREASED' named entity 'ANTIVIRAL ACTIVITY' named entity 'REPORTED' named entity 'FEATURE' named entity 'INHIBITION' named entity 'TRANSLATED' named entity 'SPECIFIC' named entity 'NANOMOLAR' named entity 'LTR' named entity 'CELLS' named entity 'AROMATIC' named entity 'G-QUADRUPLEX' named entity 'STRAINS' named entity 'EXAMPLE' named entity 'CLEAR' named entity 'G-quadruplexes' named entity 'G-quadruplex' named entity 'long terminal repeat' named entity 'LTR' named entity 'G-quadruplex'

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