April 17, 2002Biochemistry

Contribution of Basic Residues of the 70−80-Loop to Heparin Binding and Anticoagulant Function of Activated Protein C

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Population

Mutants of protein C in which basic residues of the 70-80-loop (Arg, Arg, and Lys) were replaced with Ala

Comparison

Mutation of basic residues in the 70-80-loop to… vs Wild-type activated protein C (APC)

Design

Preclinical

Authors

Discussion

APC 70-80 loop residues critical for heparin response; leaves open human translation and therapeutic targeting.

Population

Mutants of protein C in which basic residues of the 70-80-loop (Arg(74), Arg(75), and Lys(78)) were replaced with Ala

Intervention

Mutation of basic residues in the 70-80-loop to Ala

Comparator

Wild-type activated protein C (APC)

Outcome

Catalytic function (cleavage of Spectrozyme PCa, reaction with protein C inhibitor, inactivation of factor Va, and heparin binding)surrogate

Basic residues of the 70-80-loop (Arg(74), Arg(75), and Lys(78)) are critical for the catalytic function and heparin binding of activated protein C.

Yang et al. (2002) studied this question.

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