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Date of Award

Spring 2024

Document Type

Masters Thesis

Department or Program Affiliation

Chemistry

Degree Name

Master of Science (MS)

Department

Chemistry

First Advisor

Spiegel, P. Clint

Second Advisor

Smirnov, Sergey L.

Third Advisor

Anthony-Cahill, Spencer J.

Abstract

Blood coagulation factor VIII (FVIII) is an essential cofactor in the tenase complex of the blood coagulation cascade for the proteolytic activation of factor X (FX) by activated factor IX (FIXa). FVIII binds to the surface of phosphatidylserine containing membranes via the C1 and C2 domains, increasing the efficiency of FX activation by FIXa 200,000 fold. Structural studies have suggested that FVIII membrane binding is mediated through both hydrophobic and electrostatic interactions between the C domains and lipid surfaces. Many proposed FVIII membrane binding models indicate conflicting binding orientations, highlighting the need for continued structural and biophysical characterization of FVIII lipid binding.This thesis reports thermodynamic, kinetic, and structural data on the C1 and C2 domains binding to lipid nanodiscs (ND). Thermodynamic studies showed that the C1 domain’s binding to lipids is enthalpically driven, whereas the C2 domains binding to lipids is entropically driven. Mutational studies were performed on the C2 domain to understand the membrane binding orientation. Mutants K2183A, D2187A, Q2213A, L2251A, and L2252A had minimal impact on lipid binding, whereas M2199A and F2200A had a significant decrease in lipid binding. Nuclear magnetic resonance (NMR) studies of C2 and ND have highlighted residues interacting with lipids. Molecular dynamics simulations on FVIII and ND have demonstrated novel residues interacting with lipids and support our working model of FVIII membrane binding. This study has provided insight into the ongoing investigation of how FVIII binds to platelet membranes to increase FIXa activity.

Type

Text

Keywords

X-ray Crystallography, NMR, Biochemistry, Molecular Dynamics, Structural Biology, Blood Coagulation Factor VIII (FVIII)

Publisher

Western Washington University

OCLC Number

1435634853

Subject – LCSH

Blood coagulation factor VIII; Blood coagulation factors; Glycoproteins--Structure; Blood proteins--Structure; Blood platelets--Activation; Membrane proteins; Membrane lipids; Nanostructures

Format

application/pdf

Genre/Form

masters theses

Language

English

Rights

Copying of this document in whole or in part is allowable only for scholarly purposes. It is understood, however, that any copying or publication of this document for commercial purposes, or for financial gain, shall not be allowed without the author’s written permission.

Available for download on Thursday, June 05, 2025

Included in

Chemistry Commons

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