Exploring the ability of cyclic peptides to target SAM domains: a computational and experimental study (42 visite)
Chembiochem (ISSN: 1439-4227linking, 1439-7633), 2019 Sep 20; N/D: N/D-N/D.
Tipo di articolo: Journal Article,
Impact factor: 2.641, Impact factor a 5 anni: 3.684
Url: Non disponibile.
Parole chiave: Epha2, Nmr, Sam Domains, Cyclic Peptides, Virtual Screening,
Affiliazioni:
*** IBB - CNR ***
ITALY., Consiglio Nazionale delle Ricerche, Istitute of Biostructures and Bioimaging, Via Mezzocannone 16, 80134, Naples, ITALY.,
Riferimenti:
Non disponibile.
Chembiochem (ISSN: 1439-4227linking, 1439-7633), 2019 Sep 20; N/D: N/D-N/D.
Tipo di articolo: Journal Article,
Impact factor: 2.641, Impact factor a 5 anni: 3.684
Url: Non disponibile.
Parole chiave: Epha2, Nmr, Sam Domains, Cyclic Peptides, Virtual Screening,
Affiliazioni:
*** IBB - CNR ***
ITALY., Consiglio Nazionale delle Ricerche, Istitute of Biostructures and Bioimaging, Via Mezzocannone 16, 80134, Naples, ITALY.,
Riferimenti:
Non disponibile.
SAM domains are protein interaction modules with a helical fold. SAM-SAM interactions often adopt the Mid-Loop (ML)/End-Helix (EH) model in which the C-terminal helix and adjacent loops of one SAM unit (EH site) bind the central regions of another SAM domain (ML site). Herein, an original strategy to attack SAM-SAM associations is reported. It relies on the design of cyclic peptides targeting a region of the SAM domain positioned at the bottom side of the EH interface, that is thought to be important for the rise of a SAM-SAM complex. We preliminarily tested this strategy by using as model system heterotypic SAM-SAM interactions involving EphA2 receptor and implementing a multidisciplinary plan made up of computational docking studies, experimental interaction assays (by NMR and SPR techniques) and conformational analysis (by NMR and CD). This work further highlights how only a specific balance between flexibility and rigidity may be needed to generate modulators of SAM-SAM interactions.
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16 Records (16 escludendo Abstract e Conferenze).
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Impact factor a 5 anni totale: 42.2 (42.2 escludendo Abstract e Conferenze).
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Ultima modifica di Stefania De Luca in data Wednesday 23 October 2019, 9:40:25
42 visite. Ultima visita in data Saturday 14 December 2019, 10:15:26
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