September 1, 1997Journal of Medicinal ChemistryOpen Access

NMR-Based Discovery of Lead Inhibitors That Block DNA Binding of the Human Papillomavirus E2 Protein

Q: What is the clinical evidence from this study?

Study design: Other. Population: Human papillomavirus (HPV). Intervention: Biphenyl and biphenyl ether compounds (e.g., 5-(3'-(3",5"-dichlorophenoxy)-phenyl)-2,4-pentadienoic acid). Primary outcome: Inhibition of E2 binding to DNA (IC50 ~10 microM).

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Key result

An NMR-based screen identified a biphenyl ether compound that inhibits the DNA binding of the HPV-E2 protein with an IC50 of approximately 10 microM, serving as a lead for antiviral development.

Population

DNA-binding domain of the human papillomavirus (HPV) E2 protein

Design

Preclinical

Authors

PHPhilip J. HajdukAbbVie (United States)JDJürgen DingesAbbVie (United States)GMGregory F. MiknisAbbott Fund

Discussion

Member takes

Overview

Offers an early lead for HPV antivirals; hypothesis-generating and requires optimization before any clinical consideration.

Structured PICO

Population

DNA-binding domain of the human papillomavirus (HPV) E2 protein

Intervention

Biphenyl and biphenyl ether compounds containing a carboxylic acid, including [5-(3'-(3",5"-dichlorophenoxy)-phenyl)-2,4-pentadienoic acid]

Outcome

Binding to the DNA-binding domain of the HPV-E2 protein and inhibition of E2 binding to DNAsurrogate

Main Result

Effect estimate: IC50 ~10 microM

The study identifies a lead compound that inhibits HPV E2 protein binding to DNA, providing a potential basis for developing antiviral agents against HPV.

Cite This Study

Hajduk et al. (1997) studied Human papillomavirus (HPV). Biphenyl and biphenyl ether compounds (e.g., 5-(3'-(3",5"-dichlorophenoxy)-phenyl)-2,4-pentadienoic acid) was evaluated on Inhibition of E2 binding to DNA (IC50 ~10 microM). An NMR-based screen identified a biphenyl ether compound that inhibits the DNA binding of the HPV-E2 protein with an IC50 of approximately 10 microM, serving as a lead for antiviral development.

synapsesocial.com/papers/6a9394b950daee6a3ee1bed9 https://doi.org/10.1021/jm9703404

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September 1, 1997Journal of Medicinal ChemistryOpen Access

NMR-Based Discovery of Lead Inhibitors That Block DNA Binding of the Human Papillomavirus E2 Protein

View Full Paper

Ask AI

Bookmark

Key result

An NMR-based screen identified a biphenyl ether compound that inhibits the DNA binding of the HPV-E2 protein with an IC50 of approximately 10 microM, serving as a lead for antiviral development.

Population

DNA-binding domain of the human papillomavirus (HPV) E2 protein

Design

Preclinical

Authors

PHPhilip J. HajdukAbbVie (United States)JDJürgen DingesAbbVie (United States)GMGregory F. MiknisAbbott Fund

Discussion

Member takes

Overview

Offers an early lead for HPV antivirals; hypothesis-generating and requires optimization before any clinical consideration.

Structured PICO

Population

DNA-binding domain of the human papillomavirus (HPV) E2 protein

Intervention

Biphenyl and biphenyl ether compounds containing a carboxylic acid, including [5-(3'-(3",5"-dichlorophenoxy)-phenyl)-2,4-pentadienoic acid]

Outcome

Binding to the DNA-binding domain of the HPV-E2 protein and inhibition of E2 binding to DNAsurrogate

Main Result

Effect estimate: IC50 ~10 microM

The study identifies a lead compound that inhibits HPV E2 protein binding to DNA, providing a potential basis for developing antiviral agents against HPV.

Cite This Study

synapsesocial.com/papers/6a9394b950daee6a3ee1bed9 https://doi.org/10.1021/jm9703404

Also Consider

Synapse has enriched 3 closely related papers on similar clinical questions. Consider them for comparative context:

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