Detailed description page of ThPDB2

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16180 details
Primary information
ID16180
Therapeutic IDTh1693
Protein NameP113D
SequenceNA
Molecular WeightNA
Chemical FormulaNA
Isoelectric PointNA
HydrophobicityNA
Melting pointNA
Half-lifeNA
DescriptionP113D is a novel 12 amino-acid antimicrobial peptide drug derived from histatins, which are compounds found naturally in human saliva. It is being pursued as a potential treatment for cystic fibrosis by Demegen, Inc.
Indication/DiseaseFor the potential treatment of cystic fibrosis and bacterial infections.
PharmacodynamicsP113D has demonstrated activity against CF patient clinical isolates of bacteria that are resistant to traditional antibiotics. The compound is stable and maintains activity in sputum of CF patients. P113 was determined to be the smallest histatin fragment which retained antimicrobial activity equivalent to that of the parent compound. Interestingly, synthesizing P113 with D-amino acids gave rise P113D, a compound that was impervious to enzymatic degradation and maintained the antimicrobial activity of the parent compound. P113D also has very potent in vitro activity against a variety of Gram negative and positive bacteria including P. aeruginosa, S. aureus, H. influenzae, S. typhimurium, E. coli, S. epidermidis, S. mutans and S. sobrinus. In the case of P. aeruginosa and S. aureus, antibacterial activity has been demonstrated against a variety of CF patient clinical isolates which are resistant to traditional antibiotics. P. aeruginosa isolates that produce thick alginate secretions (mucoid phenotype) are also susceptible to killing by P113D.
Mechanism of ActionFor both bacteria and fungi such as Candida albicans, P113D has been shown to kill cells as opposed to simply inhibiting their growth. It has been demonstrated that P113D acts by binding to the cell surface and increasing the permeability of both the outer and inner membranes of the cells of Gram negative bacteria, killing them within seconds.
ToxicityNA
MetabolismNA
AbsorptionNA
NA
ClearanceNA
CategoriesNA
Patents NumberNA
Date of IssueNA
Date of ExpiryNA
Drug InteractionNA
TargetNA
Brand NameNA
CompanyNA
Brand DescriptionNA
Prescribed ForNA
Chemical NameNA
FormulationNA
Physical Appearance NA
Route of AdministrationNA
Recommended DosageNA
ContraindicationNA
Side EffectsNA
Useful Link 1Link
Useful Link 2NA
RemarksNA