Computer-Aided Engineering of Staphylokinase Toward Enhanced Affinity and Selectivity for Plasmin
Cardio- and cerebrovascular diseases are leading causes of death and disability, resulting in one of the highest socio-economic burdens of any disease type. The discovery of bacterial and human plasminogen activators and their use as thrombolytic drugs have revolutionized treatment of these pathologies. Fibrin-specific agents have an advantage over non-specific factors because of lower rates…
Oligomerization Alters Binding Affinity Between Amyloid Beta and a Modulator of Peptide Aggregation
The soluble oligomeric form of the amyloid beta (Aβ) peptide is the major causative agent in the molecular pathogenesis of Alzheimer’s disease (AD). We have previously developed a pyrroline-nitroxyl fluorene compound (SLF) that blocks the toxicity of Aβ. Here we introduce the multiparametric surface plasmon resonance (MP-SPR) approach to quantify SLF binding and its effect…
Taste masking effect of chlorogenic acid (CGA) on bitter drugs evaluated by taste sensor and surface plasmon resonance on the basis of CGA-Drug interactions
The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste…
Kinetics of PKCe Activating and Inhibiting Llama Single Chain Antibodies and Their Effect on PKCe Translocation in HeLa Cells
Dysregulation of PKCe is involved in several serious diseases such as cancer, type II diabetes and Alzheimer’s disease.Therefore, specific activators and inhibitors of PKCe hold promise as future therapeutics, in addition to being useful inresearch into PKCe regulated pathways. We have previously described llama single chain antibodies (VHHs) that specificallyactivate (A10, C1 and D1) or…