Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis (589 views)
Biol Chem Biological Chemistry (ISSN: 1431-6730, 1437-4315), 1998 Sep; 379(8-9): 987-1006.
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Paper type: Journal Article,
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Keywords: Antithrombotics, Hirunorms, Thrombin Synthetic Inhibitors, X-Ray Crystal Structure, Anticoagulant Agent, Hirudin, Serine Proteinase, Serine Proteinase Inhibitor, Thrombin Inhibitor, Chemical Structure, Comparative Study, Hemostasis, Human, Priority Journal, Review, Structure Activity Relation, Thrombosis, Amino Acid Chloromethyl Ketones, Animals, Antithrombins, Binding Sites, Molecular Mimicry, Protein Binding, Protein Conformation,
Affiliations:
Ctro. Interuniversitario di R. P. B., Ctro. Stud. Biocristallografia-CNR, University of Napoli Federico II, via Mezzocannone 4, 80134 Napoli, Italy
Dipartimento di Biochimica Mediche, University of Napoli Federico II, via Pansini 5, 80129 Napoli, Italy
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Biol Chem Biological Chemistry (ISSN: 1431-6730, 1437-4315), 1998 Sep; 379(8-9): 987-1006.
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Keywords: Antithrombotics, Hirunorms, Thrombin Synthetic Inhibitors, X-Ray Crystal Structure, Anticoagulant Agent, Hirudin, Serine Proteinase, Serine Proteinase Inhibitor, Thrombin Inhibitor, Chemical Structure, Comparative Study, Hemostasis, Human, Priority Journal, Review, Structure Activity Relation, Thrombosis, Amino Acid Chloromethyl Ketones, Animals, Antithrombins, Binding Sites, Molecular Mimicry, Protein Binding, Protein Conformation,
Affiliations:
Ctro. Interuniversitario di R. P. B., Ctro. Stud. Biocristallografia-CNR, University of Napoli Federico II, via Mezzocannone 4, 80134 Napoli, Italy
Dipartimento di Biochimica Mediche, University of Napoli Federico II, via Pansini 5, 80129 Napoli, Italy
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Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis
The central role of the serine protease thrombin in hemostasis and thrombosis brought many scientists to develop highly potent and selective thrombin inhibitors. Thrombin-inhibitor complexes have extensively been studied in order to understand structure-function relationships, and to design new inhibitors that can be used with broader efficacy over existing antithrombotic agents. In this paper, we summarize in a comparative manner the state of the art on reversible thrombin inhibitors and we discuss some structural aspects of thrombin-inhibitor interaction, which account for the different affinity and potency of these molecules. We also report here our approach to develop a new class of synthetic, multisite-directed thrombin inhibitors, named hirunorms, designed to mimic the distinctive binding mode of hirudin, We emphasize here that, despite the high specificity of thrombin action, the interaction of inhibitors in its active site may occur with quite different mechanisms.
The central role of the serine protease thrombin in hemostasis and thrombosis brought many scientists to develop highly potent and selective thrombin inhibitors. Thrombin-inhibitor complexes have extensively been studied in order to understand structure-function relationships, and to design new inhibitors that can be used with broader efficacy over existing antithrombotic agents. In this paper, we summarize in a comparative manner the state of the art on reversible thrombin inhibitors and we discuss some structural aspects of thrombin-inhibitor interaction, which account for the different affinity and potency of these molecules. We also report here our approach to develop a new class of synthetic, multisite-directed thrombin inhibitors, named hirunorms, designed to mimic the distinctive binding mode of hirudin, We emphasize here that, despite the high specificity of thrombin action, the interaction of inhibitors in its active site may occur with quite different mechanisms.
Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis
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Multiple binding mode of reversible synthetic thrombin inhibitors. A comparative structural analysis
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De Simone G, Bua S, Supuran CT, Alterio V
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De Simone G, Lombardi A, Galdiero S, Nastri F, Della Morte R, Staiano N, Pedone C, Bolognesi M, Pavone V
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Pavone V, Lombardi A, Saviano M, Di Blasio B, Nastri F, Fattorusso R, Zaccaro L, Maglio O, Yamada T, Omote Y
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* Benzyl alcohol inhibits carbonic anhydrases by anchoring to the zinc coordinated water molecule (11 views)
Biochem Biophys Res Commun (ISSN: 0006-291xlinking), 2021 Apr 9; 548: 217-221.
Impact Factor: 3.575
View Export to BibTeX Export to EndNote
Riccardi C, Napolitano E, Platella C, Musumeci D, Montesarchio D
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Impact Factor: 11.127
View Export to BibTeX Export to EndNote
Cella L, D'Avino V, Liuzzi R, Conson M, Doria F, Faiella A, Loffredo F, Salvatore M, Pacelli R
* Multivariate normal tissue complication probability modeling of gastrointestinal toxicity after external beam radiotherapy for localized prostate cancer (389 views)
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View Export to BibTeX Export to EndNote
Doti N, Raimondo D, Sabatella M, Ruvo M
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Impact Factor: 2.275
View Export to BibTeX Export to EndNote
Piazza O, De Robertis E, Caranci F, Quarantelli M, Tufano R
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View Export to BibTeX Export to EndNote
Marasco D, Perretta G, Sabatella M, Ruvo M
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View Export to BibTeX Export to EndNote
Di Fiore A, Pedone C, Antel J, Waldeck H, Witte A, Wurl M, Scozzafava A, Supuran CT, De Simone G
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Bioorg Med Chem Lett (ISSN: 1464-3405, 0960-894x, 1464-3405electronic), 2008 Apr 15; 18(8): 2669-2674.
Impact Factor: 2.531
View Export to BibTeX Export to EndNote
Hesse B, Lindhardt TB, Acampa W, Anagnostopoulos C, Ballinger J, Bax JJ, Edenbrandt L, Flotats A, Germano G, Stopar TG, Franken P, Kelion A, Kjaer A, Le Guludec D, Ljungberg M, Maenhout AF, Marcassa C, Marving J, Mckiddie F, Schaefer WM, Stegger L, Underw
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Eur J Nucl Med (ISSN: 1619-7070, 1619-7089, 0340-6997), 2008 Apr; 35(4): 851-885.
Impact Factor: 4.532
View Export to BibTeX Export to EndNote
Menchise V, De Simone G, Alterio V, Di Fiore A, Pedone C, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: Stacking with Phe131 determines active site binding region of inhibitors as exemplified by the X-ray crystal structure of a membrane-impermeant antitumor sulfonamide complexed with isozyme II (482 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2005 Sep 8; 48(18): 5721-5727.
Impact Factor: 4.926
View Export to BibTeX Export to EndNote
Di Fiore A, De Simone G, Menchise V, Pedone C, Casini A, Scozzafava A, Supuran CT
* Carbonic anhydrase inhibitors: X-ray crystal structure of a benzenesulfonamide strong CA II and CA IX inhibitor bearing a pentafluorophenylaminothioureido tail in complex with isozyme II (489 views)
Bioorg Med Chem Lett Bioorganic And Medicinal Chemistry Letters (ISSN: 0960-894x), 2005 Apr 1; 15(7): 1937-1942.
Impact Factor: 2.478
View Export to BibTeX Export to EndNote
De Simone G, Menchise V, Omaggio S, Pedone C, Scozzafava A, Supuran CT
* Design of weakly basic thrombin inhibitors incorporating novel P1 binding functions: Molecular and X-ray crystallographic studies (352 views)
Biochemistry (ISSN: 0006-2960, 1520-4995, 1520-4995electronic), 2003 Sep 5; 42(30): 9013-9021.
Impact Factor: 3.922
View Export to BibTeX Export to EndNote
De Falco S, Ruvoletto MG, Verdoliva A, Ruvo M, Raucci A, Marino M, Senatore S, Cassani G, Alberti A, Pontisso P, Fassina G
* Cloning and Expression of a Novel Hepatitis B Virus-binding Protein from HepG2 Cells (622 views)
Jbc Papers (ISSN: 0021-9258, 1083-351x, 0021-9258linking), 2001 Sep 28; 276(39): 36613-36623.
Impact Factor: 7.258
View Export to BibTeX Export to EndNote
Lombardi A, De Simone G, Galdiero S, Staiano N, Nastri F, Pavone V
From natural to synthetic multisite thrombin inhibitors (349 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1999; 51(1): 19-39.
Impact Factor: 2.331
View Export to BibTeX Export to EndNote
De Simone G, Lombardi A, Galdiero S, Nastri F, Della Morte R, Staiano N, Pedone C, Bolognesi M, Pavone V
Hirunorms Are True Hirudin Mimetics. The Crystal Structure Of Human Alpha-Thrombin-Hirunorm V Complex (519 views)
Protein Sci (ISSN: 0961-8368, 1469-896xelectronic), 1998 Feb; 7(2): 243-253.
Impact Factor: 4.44
View Export to BibTeX Export to EndNote
Pavone V, Lombardi A, Saviano M, Di Blasio B, Nastri F, Fattorusso R, Zaccaro L, Maglio O, Yamada T, Omote Y
Mixed conformation in C(α, α)-disubstituted tripeptides: X-ray crystal structures of Z-Aib-Dph-Gly-OMe and Bz-Dph-Dph-Gly-OMe (400 views)
Biopolymers (ISSN: 0006-3525, 0006-6352, 0006-3525print), 1994 Dec; 34(12): 1595-1604.
Impact Factor: 2.425
View Export to BibTeX Export to EndNote
18 Records (18 excluding Abstracts).
Total impact factor: 68.085 (68.085 excluding Abstracts).
Total 5 year impact factor: 63.533 (63.533 excluding Abstracts).
Total impact factor: 68.085 (68.085 excluding Abstracts).
Total 5 year impact factor: 63.533 (63.533 excluding Abstracts).
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