Milton T. Stubbs II Pages 543 - 552 ( 10 )
Factor Xa is responsible for both extrinsic and intrinsic generation of active thrombin. The recent structure determination of human factor Xa provides a basis for structure based drug design. Until very recently, however, it .has not been possible to analyse factor Xa - ligand interactions directly. A semi-conservative modelling approach, in which the interaction of factor Xa inhibitors with related serine proteinases is investigated, has yielded valuable information on the structural determinants for factor Xa inhibition. The interactions of factor Xa with DX9065a, tissue factor pathway inhibitor (TFPI), variants of basic pancre tic trypsin inhibitor (BPTI) and tick anticoagulant peptide (TAP) are discussed.