Evidence map›Paper›PMID 32044230›Full record

ArticleBioorganic & medicinal chemistry2020

An increase in side-group hydrophobicity largely improves the potency of ritonavir-like inhibitors of CYP3A4.

Eric R Samuels, Irina F Sevrioukova

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
2.1field-weighted citation impact, top 14% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

6 citing papers in PubMed, 18 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

2 authors at 1 institution in 1 country.

Eric R SamuelsDepartments of Pharmaceutical Sciences, University of California, Irvine, CA 92697-3900, United States.
Irina F SevrioukovaDepartments of Molecular Biology and Biochemistry, University of California, Irvine, CA 92697-3900, United States. Electronic address: sevrioui@uci.edu.
University of California, Irvine · US

Funding

X-ray Absorption Spectroscopy (XAS) pp.711-759P41GM103393 · NIGMS · STANFORD UNIVERSITY · PI HODGSON, KEITH O · 2012 to 2019
$30.6M
Toxicological importance of CYP3A4 catalysis and inhibitionR01ES025767 · NIEHS · UNIVERSITY OF CALIFORNIA-IRVINE · PI SEVRIOUKOVA, IRINA F · 2016 to 2025
$4.0M
NIEHS NIH HHS R01 ES025767NIGMS NIH HHS P41 GM103393
6 · The paper itself

Abstract

Identification of structural determinants required for potent inhibition of drug-metabolizing cytochrome P450 3A4 (CYP3A4) could help develop safer drugs and more effective pharmacoenhancers. We utilize a rational inhibitor design to decipher structure-activity relationships in analogues of ritonavir, a highly potent CYP3A4 inhibitor marketed as pharmacoenhancer. Analysis of compounds with the R

Indexed as

Cytochrome P-450 CYP3ACytochrome P-450 CYP3A InhibitorsDose-Response Relationship, DrugHumansHydrophobic and Hydrophilic InteractionsMolecular StructureRitonavirStructure-Activity RelationshipCYP3A4 protein, humanCytochrome P-450 CYP3ACytochrome P-450 CYP3A InhibitorsRitonavirCrystal structureCYP3A4Inhibitor designLigand bindingStructure-activity relations

Identifiers

PMID32044230
PMCPMC7179874
OpenAlexW3003506636

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.