Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders

Guillaume De Nanteuil; Philippe Gloanec; Suzette Beguin; Peter L. A. Giesen; H. Coenraad Hemker; Philippe  Mennecier; Alain  Rupin; Tony J.  Verbeuren

doi:10.1021/jm0606950

Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders

Guillaume De Nanteuil^*
, Philippe Gloanec
, Suzette Beguin
, Peter L. A. Giesen
, H. Coenraad Hemker
, Philippe Mennecier
, Alain Rupin
, Tony J. Verbeuren

^*Corresponding author for this work

Research output: Contribution to journal › Comment/Letter to the editor › Academic › peer-review

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Abstract

The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor VIIIa, involved in the regulation of bleeding in hemophilia A. Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant protease thrombin. Moreover, compound 1 significantly restored the generation of thrombin in hemophiliac plasma.

Original language	English
Pages (from-to)	5047-5050
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	49
Issue number	17
DOIs	https://doi.org/10.1021/jm0606950
Publication status	Published - 25 Jul 2006

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title = "Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders",

abstract = "The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor VIIIa, involved in the regulation of bleeding in hemophilia A. Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant protease thrombin. Moreover, compound 1 significantly restored the generation of thrombin in hemophiliac plasma.",

author = "\{De Nanteuil\}, Guillaume and Philippe Gloanec and Suzette Beguin and Giesen, \{Peter L. A.\} and Hemker, \{H. Coenraad\} and Philippe Mennecier and Alain Rupin and Verbeuren, \{Tony J.\}",

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language = "English",

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T1 - Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders

AU - De Nanteuil, Guillaume

AU - Gloanec, Philippe

AU - Beguin, Suzette

AU - Giesen, Peter L. A.

AU - Hemker, H. Coenraad

AU - Mennecier, Philippe

AU - Rupin, Alain

AU - Verbeuren, Tony J.

PY - 2006/7/25

Y1 - 2006/7/25

N2 - The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor VIIIa, involved in the regulation of bleeding in hemophilia A. Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant protease thrombin. Moreover, compound 1 significantly restored the generation of thrombin in hemophiliac plasma.

AB - The synthesis and evaluation of inhibitors of activated protein C (aPC) are reported. This serine protease is partly responsible for the degradation of factor VIIIa, involved in the regulation of bleeding in hemophilia A. Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant protease thrombin. Moreover, compound 1 significantly restored the generation of thrombin in hemophiliac plasma.

U2 - 10.1021/jm0606950

DO - 10.1021/jm0606950

M3 - Comment/Letter to the editor

C2 - 16913694

SN - 0022-2623

VL - 49

SP - 5047

EP - 5050

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 17

ER -

Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders

Abstract

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