Evidence map›Paper›PMID 29943906›Full record

ArticleThe FEBS journal2018

Deciphering the mechanism of potent peptidomimetic inhibitors targeting plasmepsins - biochemical and structural insights.

Vandana Mishra, Ishan Rathore, Anagha Arekar, Lakshmi Kavitha Sthanam, Huogen Xiao, Yoshiaki Kiso, Shamik Sen, Swati Patankar, Alla Gustchina, Koushi Hidaka and 3 more

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

Article in The FEBS journal, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
1.5field-weighted citation impact, top 16% 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

5 citing papers in PubMed, 15 citations in OpenAlex.

  1. Review
  2. Review
  3. Inhibition ofCurrent research in structural biology · 2024
    Article
  4. Article
  5. Structural Insights Into KeyFrontiers in microbiology · 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

13 authors at 6 institutions in 4 countries.

Vandana MishraDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Ishan RathoreDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Anagha ArekarDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Lakshmi Kavitha SthanamDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Huogen XiaoDepartment of Molecular and Cellular Biology, University of Guelph, ON, Canada.
Yoshiaki KisoLaboratory of Peptide Sciences, Nagahama Institute of Bio-Science and Technology, Japan.
Shamik SenDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Swati PatankarDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Alla GustchinaProtein Structure Section, Macromolecular Crystallography Laboratory, National Cancer Institute, Frederick, MD, USA.
Koushi HidakaDivision of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan.
Alexander WlodawerProtein Structure Section, Macromolecular Crystallography Laboratory, National Cancer Institute, Frederick, MD, USA.
Rickey Y YadaFaculty of Land and Food Systems, University of British Columbia, Vancouver, BC, Canada.
Prasenjit BhaumikDepartment of Biosciences and Bioengineering, Indian Institute of Technology Bombay, Powai, Mumbai, India.
Indian Institute of Technology Bombay · INFrederick National Laboratory for Cancer Research · USKobe Gakuin University · JPNagahama Institute of Bio-Science and Technology · JPUniversity of British Columbia · CAUniversity of Guelph · CA

Funding

Protein StructureZIABC010348 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI WLODAWER, ALEXANDER · 2009 to 2025
$27.5M
CCR NIH HHSDepartment of Biotechnology (DBT), Ministry of Science and TechnologyIIT BombayIntramural NIH HHS ZIA BC010348Intramural Research Program of the NIHIRCCNatural Sciences and Engineering Research Council of CanadaNCI NIH HHSNULL ZIA BC010348-17Ramalingaswami Re-entry FellowshipTakeda Science Foundation
6 · The paper itself

Abstract

Malaria is a deadly disease killing worldwide hundreds of thousands people each year and the responsible parasite has acquired resistance to the available drug combinations. The four vacuolar plasmepsins (PMs) in Plasmodium falciparum involved in hemoglobin (Hb) catabolism represent promising targets to combat drug resistance. High antimalarial activities can be achieved by developing a single drug that would simultaneously target all the vacuolar PMs. We have demonstrated for the first time the use of soluble recombinant plasmepsin II (PMII) for structure-guided drug discovery with KNI inhibitors. Compounds used in this study (KNI-10742, 10743, 10395, 10333, and 10343) exhibit nanomolar inhibition against PMII and are also effective in blocking the activities of PMI and PMIV with the low nanomolar K

Indexed as

AntimalarialsAspartic Acid EndopeptidasesCrystallography, X-RayDrug Evaluation, PreclinicalEthylenediaminesHemoglobinsHumansIsoquinolinesMolecular Targeted TherapyPeptidomimeticsPlasmodium falciparumProtease InhibitorsProtein ConformationRecombinant Fusion ProteinsThiazolesAntimalarialsAspartic Acid EndopeptidasesEthylenediaminesHemoglobinsIsoquinolinesKNI 10033KNI 10743PeptidomimeticsplasmepsinProtease InhibitorsRecombinant Fusion ProteinsThiazolescrystal structuresdrug designingKNI inhibitorsmalariaplasmepsins

Identifiers

PMID29943906
PMCPMC6309945
OpenAlexW2811196319

What OpenQuestion holds

Textmetadata
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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.