Evidence map›Paper›PMID 30015488›Full record

ArticleJournal of medicinal chemistry2018

Discovery, Synthesis, Pharmacological Profiling, and Biological Characterization of Brintonamides A-E, Novel Dual Protease and GPCR Modulators from a Marine Cyanobacterium.

Fatma H Al-Awadhi, Bowen Gao, Mohammad A Rezaei, Jason C Kwan, Chenglong Li, Tao Ye, Valerie J Paul, Hendrik Luesch

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
3.2field-weighted citation impact, top 9% 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

17 citing papers in PubMed, 24 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Article
  6. Article
  7. Article
  8. Heterologous production of cyanobacterial compounds.Journal of industrial microbiology & biotechnology · 2021
    Review
  9. Review
  10. Review
  11. Article
  12. Article
  13. Advances in CXCR7 Modulators.Pharmaceuticals (Basel, Switzerland) · 2020
    Review
  14. Review
  15. Review
  16. Article
  17. 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

8 authors at 3 institutions in 3 countries.

Fatma H Al-AwadhiDepartment of Medicinal Chemistry, Center for Natural Products, Drug Discovery and Development (CNPD3) , University of Florida , 1345 Center Drive , Gainesville , Florida 32610 , United States.
Bowen GaoState Key Laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology , Peking University Shenzhen Graduate School , Xili, Nanshan District , Shenzhen , 518055 , China.
Mohammad A RezaeiDepartment of Medicinal Chemistry, Center for Natural Products, Drug Discovery and Development (CNPD3) , University of Florida , 1345 Center Drive , Gainesville , Florida 32610 , United States.
Jason C KwanDepartment of Medicinal Chemistry, Center for Natural Products, Drug Discovery and Development (CNPD3) , University of Florida , 1345 Center Drive , Gainesville , Florida 32610 , United States.
Chenglong LiDepartment of Medicinal Chemistry, Center for Natural Products, Drug Discovery and Development (CNPD3) , University of Florida , 1345 Center Drive , Gainesville , Florida 32610 , United States.
Tao YeState Key Laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology , Peking University Shenzhen Graduate School , Xili, Nanshan District , Shenzhen , 518055 , China.ORCID 0000-0002-2780-9761
Valerie J PaulSmithsonian Marine Station , Fort Pierce , 701 Seaway Drive , Fort Pierce , Florida 34949 , United States.
Hendrik LueschDepartment of Medicinal Chemistry, Center for Natural Products, Drug Discovery and Development (CNPD3) , University of Florida , 1345 Center Drive , Gainesville , Florida 32610 , United States.ORCID 0000-0002-4091-7492
University of Florida · USPeking University · CNSmithsonian Marine Station · US

Funding

Novel Targeted Anticancer Agents from Marine CyanobacteriaR01CA172310 · NCI · UNIVERSITY OF FLORIDA · PI HENDRIK LUESCH · 2013 to 2026
$5.8M
NCI NIH HHS R01 CA172310
6 · The paper itself

Abstract

Five novel modified linear peptides named brintonamides A-E (1-5) were discovered from a marine cyanobacterial sample collected from Brinton Channel, Florida Keys. The total synthesis of 1-5 in addition to two other structurally related analogues (6 and 7) was achieved, which provided more material to allow rigorous biological evaluation and SAR studies. Compounds were subjected to cancer-focused phenotypic cell viability and migration assays and orthogonal target-based pharmacological screening platforms to identify their protease and GPCR modulatory activity profiles. The cancer related serine protease kallikrein 7 (KLK7) was inhibited to similar extents with an IC

Indexed as

Drug DesignAmidesCell Line, TumorCell MovementCell ProliferationChemistry Techniques, SyntheticCyanobacteriaHumansInhibitory Concentration 50KallikreinsModels, MolecularProtease InhibitorsProtein ConformationReceptors, G-Protein-CoupledAmidesKallikreinsKLK7 protein, humanProtease InhibitorsReceptors, G-Protein-Coupled

Identifiers

PMID30015488
PMCPMC7341966
OpenAlexW2884684345

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.