Structure-based Drug Design and Synthesis of PARP Inhibitors - Couverture souple

Murahari, Manikanta

9786200437785: Structure-based Drug Design and Synthesis of PARP Inhibitors

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ISBN 10 : 6200437785 ISBN 13 : 9786200437785

Editeur : LAP Lambert Academic Publishing, 2019

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La poly(ADP-ribose) polym�rase (PARP) est une enzyme nucl�aire li�e � la chromatine qui est activ�e par les ruptures d'ADN, utilise le NAD comme substrat et catalyse la ribosylation poly-ADP d'une vari�t� de prot�ines. L'enzyme PARP est consid�r�e comme une cible appropri�e pour l'activit� anticanc�reuse car elle est impliqu�e dans une vari�t� de fonctions physiologiques telles que la prolif�ration cellulaire, la diff�renciation, l'apoptose et la r�plication de l'ADN. Sur la base de la litt�rature, des mod�les pharmacophoriques et de l'approche de remplacement bio-isost�rique, la quinazolinone et les d�riv�s de phtalazinone ont �t� s�lectionn�s pour concevoir des mol�cules pour calculer l'affinit� de liaison et visualiser les conformations et les interactions de liaison au niveau de la poche active de la prot�ine PARP-1 cible. Pour l'�valuation pr�liminaire, des compos�s potentiels in silico ont �t� s�lectionn�s pour synth�tiser, purifi�s par chromatographie sur colonne, caract�ris�s par des �tudes HRMN et spectrales de masse et r�alis�es pour la cytotoxicit� in vitro. L'amarrage mol�culaire et les donn�es exp�rimentales pr�liminaires ont aid� � �tudier la relation structure-activit� pour la conception d'inhibiteurs de PARP-1 s�rs et potentiels pour le traitement du cancer.

Les informations fournies dans la section � Synopsis � peuvent faire r�f�rence � une autre �dition de ce titre.

�diteurLAP Lambert Academic Publishing
Date d'�dition2019
ISBN 10 6200437785
ISBN 13 9786200437785
ReliureBroch�
Langueanglais
Nombre de pages108
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Structure-based Drug Design and Synthesis of PARP Inhibitors

Manikanta Murahari

Edit� par LAP LAMBERT Academic Publishing, 2019

ISBN 10 : 6200437785 ISBN 13 : 9786200437785

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Etat : New. Dieser Artikel ist ein Print on Demand Artikel und wird nach Ihrer Bestellung fuer Sie gedruckt. Autor/Autorin: Murahari ManikantaDr. Manikanta Murahari is an academic researcher presently working as Assistant Professor at Department of Pharmaceutical Chemistry, Faculty of Pharmacy, M.S. Ramaiah University of Applied Sciences, Bangalore. He wo. N� de r�f. du vendeur 335816147

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Structure-based Drug Design and Synthesis of PARP Inhibitors

Manikanta Murahari

Edit� par LAP LAMBERT Academic Publishing Okt 2019, 2019

ISBN 10 : 6200437785 ISBN 13 : 9786200437785

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Taschenbuch. Etat : Neu. This item is printed on demand - it takes 3-4 days longer - Neuware -Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy. 108 pp. Englisch. N� de r�f. du vendeur 9786200437785

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Structure-based Drug Design and Synthesis of PARP Inhibitors : Poly(ADP-ribose)polymerase-1 Inhibitors

Manikanta Murahari

Edit� par LAP LAMBERT Academic Publishing, 2019

ISBN 10 : 6200437785 ISBN 13 : 9786200437785

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Taschenbuch. Etat : Neu. nach der Bestellung gedruckt Neuware - Printed after ordering - Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy. N� de r�f. du vendeur 9786200437785

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Structure-based Drug Design and Synthesis of PARP Inhibitors

Manikanta Murahari

Edit� par LAP LAMBERT Academic Publishing Okt 2019, 2019

ISBN 10 : 6200437785 ISBN 13 : 9786200437785

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Taschenbuch. Etat : Neu. Neuware -Poly(ADP-ribose)polymerase (PARP) is a chromatin bound nuclear enzyme which gets activated by DNA breaks, uses NAD as substrate and catalyses the poly-ADP ribosylation of a variety of proteins. The enzyme PARP is considered as a suitable target for anti-cancer activity as it is involved in a variety of physiological functions like cellular proliferation, differentiation, apoptosis and DNA replication. Based on the literature, pharmacophoric templates and bio-isosteric replacement approach, quinazolinone and phthalazinone derivatives were selected to design molecules to calculate binding affinity and visualize binding conformations and interactions at the active pocket of target PARP-1 protein. For preliminary evaluation, in silico potential compounds were selected to synthesize, purified by column chromatography, characterized by HNMR and Mass Spectral studies and carried out for in vitro cytotoxicity. Molecular docking and preliminary experimental data helped to investigate Structure Activity Relationship for design of safe and potential PARP-1 inhibitors for cancer therapy.Books on Demand GmbH, �berseering 33, 22297 Hamburg 108 pp. Englisch. N� de r�f. du vendeur 9786200437785

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