Silvia Paoletta
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Explore the profile of Silvia Paoletta including associated specialties, affiliations and a list of published articles.
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41
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1032
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Recent Articles
1.
Welti J, Sharp A, Brooks N, Yuan W, McNair C, Chand S, et al.
Cancer Discov
. 2021 Jan;
11(5):1118-1137.
PMID: 33431496
Resistance to androgen receptor (AR) blockade in castration-resistant prostate cancer (CRPC) is associated with sustained AR signaling, including through alternative splicing of AR (AR-SV). Inhibitors of transcriptional coactivators that regulate...
2.
Federico S, Margiotta E, Paoletta S, Kachler S, Klotz K, Jacobson K, et al.
Medchemcomm
. 2019 Aug;
10(7):1094-1108.
PMID: 31391881
A series of adenosine receptor antagonists bearing a reactive linker was developed. Functionalization of these derivatives is useful to easily obtain multi-target ligands, receptor probes, drug delivery systems, and diagnostic...
3.
Ciancetta A, OConnor R, Paoletta S, Jacobson K
J Chem Inf Model
. 2017 Nov;
57(12):3104-3123.
PMID: 29182323
We performed a molecular modeling analysis of 100 nucleotide-like bisphosphates and 46 non-nucleotide arylurea derivatives previously reported as P2YR binders using the recently solved hP2YR structures. We initially docked the...
4.
Du L, Gao Z, Paoletta S, Wan T, Gizewski E, Barbour S, et al.
Purinergic Signal
. 2017 Nov;
14(1):59-71.
PMID: 29170977
Activity of the A adenosine receptor (AR) allosteric modulators LUF6000 (2-cyclohexyl-N-(3,4-dichlorophenyl)-1H-imidazo [4,5-c]quinolin-4-amine) and LUF6096 (N-{2-[(3,4-dichlorophenyl)amino]quinolin-4-yl}cyclohexanecarbox-amide) was compared at four AAR species homologs used in preclinical drug development. In guanosine 5'-[γ-[S]thio]triphosphate...
5.
Lecchi A, Femia E, Paoletta S, Dupuis A, Ohlmann P, Gachet C, et al.
Hamostaseologie
. 2016 Aug;
36(4):279-283.
PMID: 27487748
The platelet adenosine 5'-diphosphate (ADP) receptor P2Y (P2YR) plays a critical role in platelet aggregation. The present report illustrates an update of dysfunctional platelet P2YR mutations diagnosed with congenital lifelong...
6.
Bacilieri M, Paoletta S, Basili S, Fanton M, Moro S
Mol Inform
. 2016 Jul;
30(11-12):927-38.
PMID: 27468148
In the present paper, we are interested to explore if the application of docking-driven conformational analysis could increase the goodness of 3D-QSAR statistical models, as alternative approach to a conventional...
7.
Baltos J, Paoletta S, Nguyen A, Gregory K, Tosh D, Christopoulos A, et al.
Mol Pharmacol
. 2016 May;
90(1):12-22.
PMID: 27136943
Biased agonism at G protein-coupled receptors (GPCRs) has significant implications for current drug discovery, but molecular determinants that govern ligand bias remain largely unknown. The adenosine A3 GPCR (A3AR) is...
8.
Tosh D, Paoletta S, Chen Z, Crane S, Lloyd J, Gao Z, et al.
Medchemcomm
. 2015 Aug;
6:555-563.
PMID: 26236460
2-Arylethynyl derivatives of (N)-methanocarba adenosine 5'-uronamides are selective AAR (adenosine receptor) agonists. Here we substitute a 1,2,3-triazol-1-yl linker in place of the rigid, linear ethynyl group to eliminate its potential...
9.
Paoletta S, Sabbadin D, von Kugelgen I, Hinz S, Katritch V, Hoffmann K, et al.
J Comput Aided Mol Des
. 2015 Jul;
29(8):737-56.
PMID: 26194851
The G protein-coupled P2Y12 receptor (P2Y12R) is an important antithrombotic target and of great interest for pharmaceutical discovery. Its recently solved, highly divergent crystallographic structures in complex either with nucleotides...
10.
Tosh D, Crane S, Chen Z, Paoletta S, Gao Z, Gizewski E, et al.
ACS Med Chem Lett
. 2015 Jul;
6(7):804-8.
PMID: 26191370
Substitution of rigidified A3 adenosine receptor (AR) agonists with a 2-((5-chlorothiophen-2-yl)ethynyl) or a 2-(4-(5-chlorothiophen-2-yl)-1H-1,2,3-triazol-1-yl) group provides prolonged protection in a model of chronic neuropathic pain. These agonists contain a bicyclo[3.1.0]hexane...