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Discovery methodology for the development of direct factor VIIa inhibitors.

Identifieur interne : 003245 ( PubMed/Checkpoint ); précédent : 003244; suivant : 003246

Discovery methodology for the development of direct factor VIIa inhibitors.

Auteurs : Brian L. Henry [États-Unis] ; Umesh R. Desai

Source :

Expert opinion on drug discovery [ 1746-045X ] ; 2014.

RBID : pubmed:24882057

Descripteurs français

KwdFr :
- Animaux, Anticoagulants (), Anticoagulants (effets indésirables), Anticoagulants (pharmacologie), Biodisponibilité, Conception de médicament, Facteur VIIa (antagonistes et inhibiteurs), Humains, Hémorragie (), Thiazépines (), Thiazépines (pharmacologie).
MESH :
- antagonistes et inhibiteurs : Facteur VIIa.
- effets indésirables : Anticoagulants.
- pharmacologie : Anticoagulants, Thiazépines.
- Animaux, Anticoagulants, Biodisponibilité, Conception de médicament, Humains, Hémorragie, Thiazépines.

English descriptors

KwdEn :
- Animals, Anticoagulants (adverse effects), Anticoagulants (chemistry), Anticoagulants (pharmacology), Biological Availability, Drug Design, Factor VIIa (antagonists & inhibitors), Hemorrhage (chemically induced), Humans, Thiazepines (chemistry), Thiazepines (pharmacology).
MESH :
- chemical , adverse effects : Anticoagulants.
- chemical , antagonists & inhibitors : Factor VIIa.
- chemical , chemistry : Anticoagulants, Thiazepines.
- chemical , pharmacology : Anticoagulants, Thiazepines.
- chemically induced : Hemorrhage.
- Animals, Biological Availability, Drug Design, Humans.

Abstract

Heparin and warfarin have historically been the only antithrombotics available. Recently, however, newer anticoagulants have been developed. Factor VIIa (fVIIa) inhibitors represent one of the new and potentially exciting classes of anticoagulants currently under development. Indeed, several methodologies have been used to develop fVIIa inhibitors.

DOI: 10.1517/17460441.2014.923398
PubMed: 24882057

Affiliations:

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Le document en format XML

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<author><name sortKey="Henry, Brian L" sort="Henry, Brian L" uniqKey="Henry B" first="Brian L" last="Henry">Brian L. Henry</name>
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<country wicri:rule="url">États-Unis</country>
<wicri:regionArea>University of Pittsburgh Medical Center, Heart and Vascular Institute Pittsburgh, Department of Cardiology , Scaife Hall, Suite B-571.3, 200 Lothrop Street, Pittsburgh, PA 15213 </wicri:regionArea>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term>
<term>Anticoagulants (adverse effects)</term>
<term>Anticoagulants (chemistry)</term>
<term>Anticoagulants (pharmacology)</term>
<term>Biological Availability</term>
<term>Drug Design</term>
<term>Factor VIIa (antagonists & inhibitors)</term>
<term>Hemorrhage (chemically induced)</term>
<term>Humans</term>
<term>Thiazepines (chemistry)</term>
<term>Thiazepines (pharmacology)</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term>
<term>Anticoagulants ()</term>
<term>Anticoagulants (effets indésirables)</term>
<term>Anticoagulants (pharmacologie)</term>
<term>Biodisponibilité</term>
<term>Conception de médicament</term>
<term>Facteur VIIa (antagonistes et inhibiteurs)</term>
<term>Humains</term>
<term>Hémorragie ()</term>
<term>Thiazépines ()</term>
<term>Thiazépines (pharmacologie)</term>
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<keywords scheme="MESH" type="chemical" qualifier="adverse effects" xml:lang="en"><term>Anticoagulants</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Factor VIIa</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Anticoagulants</term>
<term>Thiazepines</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Anticoagulants</term>
<term>Thiazepines</term>
</keywords>
<keywords scheme="MESH" qualifier="antagonistes et inhibiteurs" xml:lang="fr"><term>Facteur VIIa</term>
</keywords>
<keywords scheme="MESH" qualifier="chemically induced" xml:lang="en"><term>Hemorrhage</term>
</keywords>
<keywords scheme="MESH" qualifier="effets indésirables" xml:lang="fr"><term>Anticoagulants</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Anticoagulants</term>
<term>Thiazépines</term>
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<front><div type="abstract" xml:lang="en">Heparin and warfarin have historically been the only antithrombotics available. Recently, however, newer anticoagulants have been developed. Factor VIIa (fVIIa) inhibitors represent one of the new and potentially exciting classes of anticoagulants currently under development. Indeed, several methodologies have been used to develop fVIIa inhibitors.</div>
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<Month>07</Month>
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<Title>Expert opinion on drug discovery</Title>
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<ArticleTitle>Discovery methodology for the development of direct factor VIIa inhibitors.</ArticleTitle>
<Pagination><MedlinePgn>859-72</MedlinePgn>
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<ELocationID EIdType="doi" ValidYN="Y">10.1517/17460441.2014.923398</ELocationID>
<Abstract><AbstractText Label="INTRODUCTION" NlmCategory="BACKGROUND">Heparin and warfarin have historically been the only antithrombotics available. Recently, however, newer anticoagulants have been developed. Factor VIIa (fVIIa) inhibitors represent one of the new and potentially exciting classes of anticoagulants currently under development. Indeed, several methodologies have been used to develop fVIIa inhibitors.</AbstractText>
<AbstractText Label="AREAS COVERED" NlmCategory="METHODS">The authors highlight some of the methologies applied for the discovery of fVIIa inhibitors including phage display, isolation of endogenous peptides from hematophagous animals and the use of the 1,5-benzothiazepine molecular scaffolds and screens of large chemical libraries previously used to identify other serine protease inhibitors. Although these screens were intended to identify thrombin and factor Xa inhibitors, the compounds often had concomitant fVIIa activity. The authors also discuss the utilization of medical chemistry techniques for the discovery of these compounds.</AbstractText>
<AbstractText Label="EXPERT OPINION" NlmCategory="CONCLUSIONS">FVIIa inhibitors represent a viable option for the development of new anticoagulants. There are theoretical advantages that fVIIa inhibitors may possess over existing anticoagulants and highly specific inhibitors that possess oral bioavailability and low bleeding risk may succeed.</AbstractText>
</Abstract>
<AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Henry</LastName>
<ForeName>Brian L</ForeName>
<Initials>BL</Initials>
<AffiliationInfo><Affiliation>University of Pittsburgh Medical Center, Heart and Vascular Institute Pittsburgh, Department of Cardiology , Scaife Hall, Suite B-571.3, 200 Lothrop Street, Pittsburgh, PA 15213 , USA +1 412 647 3429 ; +1 412 647 0481 ; henrybl@upmc.edu.</Affiliation>
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</Author>
<Author ValidYN="Y"><LastName>Desai</LastName>
<ForeName>Umesh R</ForeName>
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<Language>eng</Language>
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<NameOfSubstance UI="D000925">Anticoagulants</NameOfSubstance>
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<NameOfSubstance UI="D013841">Thiazepines</NameOfSubstance>
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<Chemical><RegistryNumber>EC 3.4.21.21</RegistryNumber>
<NameOfSubstance UI="D015942">Factor VIIa</NameOfSubstance>
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<MeshHeadingList><MeshHeading><DescriptorName UI="D000818" MajorTopicYN="N">Animals</DescriptorName>
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<MeshHeading><DescriptorName UI="D000925" MajorTopicYN="N">Anticoagulants</DescriptorName>
<QualifierName UI="Q000009" MajorTopicYN="N">adverse effects</QualifierName>
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<MeshHeading><DescriptorName UI="D015195" MajorTopicYN="Y">Drug Design</DescriptorName>
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<MeshHeading><DescriptorName UI="D015942" MajorTopicYN="N">Factor VIIa</DescriptorName>
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<MeshHeading><DescriptorName UI="D006470" MajorTopicYN="N">Hemorrhage</DescriptorName>
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<MeshHeading><DescriptorName UI="D006801" MajorTopicYN="N">Humans</DescriptorName>
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<QualifierName UI="Q000494" MajorTopicYN="N">pharmacology</QualifierName>
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<KeywordList Owner="NOTNLM"><Keyword MajorTopicYN="N">anticoagulants</Keyword>
<Keyword MajorTopicYN="N">coagulation</Keyword>
<Keyword MajorTopicYN="N">factor VIIa</Keyword>
<Keyword MajorTopicYN="N">small molecule inhibitors</Keyword>
<Keyword MajorTopicYN="N">tissue factor</Keyword>
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Discovery methodology for the development of direct factor VIIa inhibitors.

Discovery methodology for the development of direct factor VIIa inhibitors.

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Links to Exploration step

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri

Pour générer des pages wiki