Evidence map›Paper›PMID 23899617›Full record

ArticleBioorganic & medicinal chemistry letters2013

Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.

Mariela Bollini, Kathleen M Frey, José A Cisneros, Krasimir A Spasov, Kalyan Das, Joseph D Bauman, Eddy Arnold, Karen S Anderson, William L Jorgensen

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing 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

16 citing papers in PubMed.

  1. Review
  2. Review
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Article
  9. Article
  10. Article
  11. Computer-aided discovery of anti-HIV agents.Bioorganic & medicinal chemistry · 2016
    Article
  12. Structural biology in antiviral drug discovery.Current opinion in pharmacology · 2016
    Review
  13. Article
  14. Article
  15. Article
  16. 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

9 authors.

Mariela BolliniDepartment of Chemistry, Yale University, New Haven, CT 06520-8107, USA.
Kathleen M Frey
José A Cisneros
Krasimir A Spasov
Kalyan Das
Joseph D Bauman
Eddy Arnold
Karen S Anderson
William L Jorgensen

Funding

STRUCTURES OF HIV REVERSE TRANSCRIPTASE WITH SUBSTRATESR37AI027690 · NIAID · RUTGERS THE ST UNIV OF NJ NEW BRUNSWICK · PI ARNOLD, EDWARD · 1999 to 2018
$14.4M
MECHANISM AND INHIBITION OF HIV REVERSE TRANSCRIPTASER01GM049551 · NIGMS · YALE UNIVERSITY · PI ANDERSON, KAREN S. · 1993 to 2019
$9.0M
POTENTIAL FUNCTIONS FOR WATER PROTEIN INTERACTIONSR01GM032136 · NIGMS · YALE UNIVERSITY · PI JORGENSEN, WILLIAM L. · 1985 to 2023
$8.2M
COMPUTER-AIDED DESIGN OF ANTIHIV DRUGSR01AI044616 · NIAID · YALE UNIVERSITY · PI JORGENSEN, WILLIAM L. · 1999 to 2022
$7.7M
STRUCTURES OF HIV REVERSE TRANSCRIPTASE WITH SUBSTRATESR01AI027690 · NIAID · UNIV OF MED/DENT NJ-R W JOHNSON MED SCH · PI EDWARD ARNOLD · 1989 to 2026
$4.3M
Structure activity and structure property relationships for novel anti-HIV agentsF32AI104334 · NIAID · YALE UNIVERSITY · PI FREY, KATHLEEN MARY · 2013 to 2015
$140k
NIAID NIH HHS AI27690NIAID NIH HHS AI44616NIAID NIH HHS F32 AI104334NIAID NIH HHS R01 AI027690NIAID NIH HHS R01 AI044616NIAID NIH HHS R37 AI027690NIGMS NIH HHS GM32136NIGMS NIH HHS GM49551NIGMS NIH HHS R01 GM032136NIGMS NIH HHS R01 GM049551
6 · The paper itself

Abstract

Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that feature extension into the entrance channel near Glu138. Complexes of the parent anilinylpyrimidine 1 and the morpholinoethoxy analog 2j with HIV-RT have received crystallographic characterization confirming the designs. Measurement of aqueous solubilities of 2j, 2k, the parent triazene 2a, and other NNRTIs demonstrate profound benefits for addition of the morpholinyl substituent.

Indexed as

Anti-HIV AgentsCrystallography, X-RayDose-Response Relationship, DrugEnzyme InhibitorsHIV-1HIV Reverse TranscriptaseModels, MolecularMolecular StructurePyrimidinesSolubilityStructure-Activity RelationshipAnti-HIV AgentsEnzyme InhibitorsHIV Reverse TranscriptasePyrimidinesreverse transcriptase, Human immunodeficiency virus 1Anti-HIV agentCrystal structuresDrug solubilityNNRTI

Identifiers

PMID23899617
PMCPMC3761378

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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.