Evidence map›Paper›PMID 28434781›Full record

ArticleBioorganic & medicinal chemistry2017

Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: Synthesis, biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex.

Arun K Ghosh, Margherita Brindisi, Prasanth R Nyalapatla, Jun Takayama, Jean-Rene Ella-Menye, Sofiya Yashchuk, Johnson Agniswamy, Yuan-Fang Wang, Manabu Aoki, Masayuki Amano and 2 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2017. 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
–field-weighted citation impact
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.

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

12 authors.

Arun K GhoshDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA. Electronic address: akghosh@purdue.edu.
Margherita BrindisiDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Prasanth R NyalapatlaDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Jun TakayamaDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Jean-Rene Ella-MenyeDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Sofiya YashchukDepartment of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Johnson AgniswamyDepartment of Biology, Georgia State University, Atlanta, GA 30303, USA.
Yuan-Fang WangDepartment of Biology, Georgia State University, Atlanta, GA 30303, USA.
Manabu AokiDepartment of Hematology, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Department of Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan.
Masayuki AmanoDepartment of Hematology, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Department of Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan.
Irene T WeberDepartment of Biology, Georgia State University, Atlanta, GA 30303, USA; Department of Chemistry, Georgia State University, Atlanta, GA 30303, USA.
Hiroaki MitsuyaDepartment of Hematology, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Department of 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; Department of Refractory Viral Infection, National Center for Global Health and Medicine Research Institute, Shinjuku, Tokyo 162-8655, Japan.

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

Based upon molecular insights from the X-ray structures of inhibitor-bound HIV-1 protease complexes, we have designed a series of isophthalamide-derived inhibitors incorporating substituted pyrrolidines, piperidines and thiazolidines as P2-P3 ligands for specific interactions in the S2-S3 extended site. Compound 4b has shown an enzyme K

Indexed as

Drug DesignAmidesCrystallography, X-RayHIV-1HIV InfectionsHIV ProteaseHIV Protease InhibitorsHumansMolecular Docking SimulationPhthalic AcidsAmidesHIV ProteaseHIV Protease Inhibitorsp16 protease, Human immunodeficiency virus 1Phthalic AcidsDrug-resistanceHIV-1 proteaseIsophthalamideSynthesisX-ray structure

Identifiers

PMID28434781
PMCPMC5617771

What OpenQuestion holds

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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.