Evidence map›Paper›PMID 28958624›Full record

ArticleBioorganic & medicinal chemistry letters2017

Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.

Arun K Ghosh, W Sean Fyvie, Margherita Brindisi, Melinda Steffey, Johnson Agniswamy, Yuan-Fang Wang, Manabu Aoki, Masayuki Amano, Irene T Weber, Hiroaki Mitsuya

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.5field-weighted citation impact, top 36% 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

3 citing papers in PubMed, 9 citations in OpenAlex.

  1. Article
  2. Article
  3. Proteases: Pivot Points in Functional Proteomics.Methods in molecular biology (Clifton, N.J.) · 2019
    Review
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

10 authors at 3 institutions in 2 countries.

Arun K GhoshDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA; Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA. Electronic address: akghosh@purdue.edu.
W Sean FyvieDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Margherita BrindisiDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Melinda SteffeyDepartment of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Johnson AgniswamyDepartments of Biology and Chemistry, Georgia State University, Atlanta, GA 30303, USA.
Yuan-Fang WangDepartments of Biology and Chemistry, Georgia State University, Atlanta, GA 30303, USA.
Manabu AokiDepartments of Hematology and Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan.
Masayuki AmanoDepartments of Hematology and Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan.
Irene T WeberDepartments of Biology and Chemistry, Georgia State University, Atlanta, GA 30303, USA.
Hiroaki MitsuyaDepartments of Hematology and Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch National Cancer Institute, Bethesda, MD 20892, USA; Center for Clinical Sciences, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan.
Purdue University West Lafayette · USGeorgia State University · USKumamoto University · JP

Funding

Development of Antiviral Therapy of HIV-1 InfectionZIASC006738 · NCI · DIVISION OF CLINICAL SCIENCES - NCI · PI MITSUYA, HIROAKI · 2009 to 2025
$10.0M
Design & Synthesis of Nonpeptide Protease InhibitorsR37GM053386 · NIGMS · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2011 to 2018
$3.9M
DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSR01GM053386 · NIGMS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI GHOSH, ARUN K · 1995 to 2010
$3.7M
ACTIVITY OF RESISTANT VARIANTS OF HIV PROTEASER01GM062920 · NIGMS · GEORGIA STATE UNIVERSITY · PI WEBER, IRENE T · 2000 to 2012
$3.3M
Inhibition of Resistant Variants of HIV ProteaseU01GM062920 · NIGMS · GEORGIA STATE UNIVERSITY · PI HARRISON, ROBERT WILSON, WEBER, IRENE T · 2013 to 2018
$2.1M
NIGMS NIH HHS R01 GM053386NIGMS NIH HHS R01 GM062920NIGMS NIH HHS R37 GM053386NIGMS NIH HHS U01 GM062920
6 · The paper itself

Abstract

Design, synthesis, and evaluation of a new class of HIV-1 protease inhibitors containing diverse flexible macrocyclic P1'-P2' tethers are reported. Inhibitor 5a with a pyrrolidinone-derived macrocycle exhibited favorable enzyme inhibitory and antiviral activity (K

Indexed as

Drug DesignBinding SitesCrystallography, X-RayHIV-1HIV ProteaseHIV Protease InhibitorsInhibitory Concentration 50LigandsMacrocyclic CompoundsMolecular Dynamics SimulationMutationProtein Structure, TertiaryPyrrolidinonesStructure-Activity RelationshipHIV ProteaseHIV Protease InhibitorsLigandsMacrocyclic Compoundsp16 protease, Human immunodeficiency virus 1PyrrolidinonesDrug resistanceHIV proteaseMacrocyclic inhibitorsP1′-P2′ ligandsStructure-based design

Identifiers

PMID28958624
PMCPMC5647257
OpenAlexW2753545875

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.