Evidence map›Paper›PMID 30886166›Full record

ArticleScientific reports2019

Activity and structural analysis of GRL-117C: a novel small molecule CCR5 inhibitor active against R5-tropic HIV-1s.

Hirotomo Nakata, Kenji Maeda, Debananda Das, Simon B Chang, Kouki Matsuda, Kalapala Venkateswara Rao, Shigeyoshi Harada, Kazuhisa Yoshimura, Arun K Ghosh, Hiroaki Mitsuya

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

Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.9field-weighted citation impact, top 31% 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

4 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. 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 4 institutions in 2 countries.

Hirotomo NakataExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, 20892-1868, USA.
Kenji MaedaNational Center for Global Health and Medicine Research Institute, Tokyo, 162-8655, Japan. kmaeda@ri.ncgm.go.jp.ORCID 0000-0002-9424-1491
Debananda DasExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, 20892-1868, USA.ORCID 0000-0001-9943-5888
Simon B ChangExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, 20892-1868, USA.
Kouki MatsudaNational Center for Global Health and Medicine Research Institute, Tokyo, 162-8655, Japan.
Kalapala Venkateswara RaoDepartment of Chemistry and department of Medicinal Chemistry and Molecular pharmacology, Purdue University, West Lafayette, Indiana, USA.
Shigeyoshi HaradaAIDS Research Centre, National Institute of Infectious Diseases, Tokyo, 162-8640, Japan.
Kazuhisa YoshimuraAIDS Research Centre, National Institute of Infectious Diseases, Tokyo, 162-8640, Japan.
Arun K GhoshDepartment of Chemistry and department of Medicinal Chemistry and Molecular pharmacology, Purdue University, West Lafayette, Indiana, USA.
Hiroaki MitsuyaExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, 20892-1868, USA.
National Institutes of Health · USNational Center for Global Health and Medicine · JPNational Institute of Infectious Diseases · JPPurdue University West Lafayette · US

Funding

Study of Structures of CCR5 and Its Interactions with CCR5 InhibitorsZIABC011109 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI MITSUYA, HIROAKI · 2009 to 2019
$2.2M
Design & Synthesis of Nonpeptide Protease InhibitorsR37AI150466 · NIAID · PURDUE UNIVERSITY · PI GHOSH, ARUN K · 2019 to 2020
$969k
NIAID NIH HHS R37 AI150466U.S. Department of Health & Human Services | NIH | National Cancer Institute (NCI) BC011109
6 · The paper itself

Abstract

CCR5 is a member of the G-protein coupled receptor family that serves as an essential co-receptor for cellular entry of R5-tropic HIV-1, and is a validated target for therapeutics against HIV-1 infections. In the present study, we designed and synthesized a series of novel small CCR5 inhibitors and evaluated their antiviral activity. GRL-117C inhibited the replication of wild-type R5-HIV-1 with a sub-nanomolar IC

Indexed as

AnimalsAnti-HIV AgentsBinding SitesBlood Buffy CoatCCR5 Receptor AntagonistsCD4-Positive T-LymphocytesCell LineCHO CellsCricetulusDrug Resistance, ViralHeLa CellsHIV-1HIV InfectionsHumansHydrophobic and Hydrophilic InteractionsInhibitory Concentration 50Anti-HIV AgentsCCR5 protein, humanCCR5 Receptor AntagonistsMaravirocReceptors, CCR5

Identifiers

PMID30886166
PMCPMC6423129
OpenAlexW2922318312

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.