ArticleJournal of chemical biology2008
Transient binding patches: a plausible concept for drug binding.
Article in Journal of chemical biology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
6 citing papers in PubMed, 13 citations in OpenAlex.
- Kinetic analysis and molecular modeling of the inhibition mechanism of roneparstat (SST0001) on human heparanase.Glycobiology · 2016Article
- Structural Insights into Binding of the Antifungal Drug Fluconazole to Saccharomyces cerevisiae Lanosterol 14α-Demethylase.Antimicrobial agents and chemotherapy · 2015Article
- Simplification traps.Journal of chemical biology · 2012Article
- Potent family-18 chitinase inhibitors: x-ray structures, affinities, and binding mechanisms.The Journal of biological chemistry · 2011Article
- Hill coefficients of dietary polyphenolic enzyme inhibitiors: can beneficial health effects of dietary polyphenols be explained by allosteric enzyme denaturing?Journal of chemical biology · 2011Article
- Hill coefficients, dose-response curves and allosteric mechanisms.Journal of chemical biology · 2010Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Dose-response curves for inhibitors (drugs) generally are analyzed by means of four-parameter fits, yielding IC(50), background, amplitude, and Hill coefficient. Hill coefficients not equal1 contradict 1:1 competition. If binding of substrates to proteins is a stepwise process where initial binding to initial locations (patches) leads to strong binding on defined sites, then drugs (non-endogenous inhibitors) may bind to those presumably larger patches and need not follow a 1:1 stoichiometry for specific inhibition. This concept was translated into three computable models and successfully fitted to 1,282 phosphatase dose-response curves. The models only required four parameters, namely, the equilibrium dissociation constant K (D)(1) of the first inhibitor binding step, background, amplitude, and a compound interaction factor to quantify the interaction of inhibitors on those patches. Binding of one established inhibitor to the vaccinia virus VH1-related (VHR) phosphatase was directly measured with microcalorimetry, confirming multiple inhibitor binding with equilibrium constants obtained from corresponding inhibition curves.
Identifiers
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.