Evidence map›Paper›PMID 33114525›Full record

ArticleMolecules (Basel, Switzerland)2020

RETRACTED: Synthetic Makaluvamine Analogs Decrease c-Kit Expression and Are Cytotoxic to Neuroendocrine Tumor Cells.

Zviadi Aburjania, Jason D Whitt, Samuel Jang, Dwayaja H Nadkarni, Herbert Chen, J Bart Rose, Sadanandan E Velu, Renata Jaskula-Sztul

RetractedOpen access · goldAbstract readRetracted Publication
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.4field-weighted citation impact, top 34% 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, 5 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Review
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

8 authors at 1 institution in 1 country.

Zviadi AburjaniaDepartment of Surgery, University of Alabama at Birmingham, 1824 6th Avenue S., Birmingham, AL 35233, USA.
Jason D WhittDepartment of Surgery, University of Alabama at Birmingham, 1824 6th Avenue S., Birmingham, AL 35233, USA.
Samuel JangDepartment of Surgery, University of Alabama at Birmingham, 1824 6th Avenue S., Birmingham, AL 35233, USA.
Dwayaja H NadkarniDepartment of Chemistry, University of Alabama at Birmingham, 901 14th Street S., Birmingham, AL 35294, USA.
Herbert ChenDepartment of Surgery, University of Alabama at Birmingham, 1824 6th Avenue S., Birmingham, AL 35233, USA.
J Bart RoseDepartment of Surgery, University of Alabama at Birmingham, 1824 6th Avenue S., Birmingham, AL 35233, USA.
Sadanandan E VeluDepartment of Chemistry, University of Alabama at Birmingham, 901 14th Street S., Birmingham, AL 35294, USA.ORCID 0000-0002-0342-2378
Renata Jaskula-SztulDepartment of Surgery, University of Alabama at Birmingham, 1824 6th Avenue S., Birmingham, AL 35233, USA.
University of Alabama at Birmingham · US

Funding

XRAY CRYSTALLOGRAPHYP30CA013148 · NCI · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI Robert S Welner · 1985 to 2026
$165.9M
Hydrogel encapsulated biofilm inhibitors for dental caries prevention and treatmentR21DE028349 · NIDCR · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI VELU, SADANANDAN E. · 2019 to 2020
$396k
Somatostatin receptor 2 (SSTR2) antibody-drug conjugate for pancreatic neuroendocrine tumor (PanNET) therapyR21CA226491 · NCI · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI JASKULA-SZTUL, RENATA, LIU, XIAOGUANG MARGARET · 2020 to 2021
$364k
S. mutans GTF - a novel target for dental caries preventionR03DE025058 · NIDCR · UNIVERSITY OF ALABAMA AT BIRMINGHAM · PI VELU, SADANANDAN E. · 2015 to 2016
$221k
NCI NIH HHS P30 CA013148NCI NIH HHS R21 CA226491NIDCR NIH HHS R21 DE028349NIH HHS R03DE025058NIH HHS R21CA226491
6 · The paper itself

Abstract

In an effort to discover viable systemic chemotherapeutic agents for neuroendocrine tumors (NETs), we screened a small library of 18 drug-like compounds obtained from the Velu lab against pulmonary (H727) and thyroid (MZ-CRC-1 and TT) neuroendocrine tumor-derived cell lines. Two potent lead compounds (DHN-II-84 and DHN-III-14) identified from this screening were found to be analogs of the natural product makaluvamine. We further characterized the antitumor activities of these two compounds using pulmonary (H727), thyroid (MZ-CRC-1) and pancreatic (BON) neuroendocrine tumor cell lines. Flow cytometry showed a dose-dependent increase in apoptosis in all cell lines. Induction of apoptosis with these compounds was also supported by the decrease in myeloid cell leukemia-1 (MCL-1) and X-chromosome linked inhibitor of apoptosis (XIAP) detected by Western blot. Compound treatment decreased NET markers chromogranin A (CgA) and achaete-scute homolog 1 (ASCL1) in a dose-dependent manner. Moreover, the gene expression analysis showed that the compound treatment reduced c-Kit proto-oncogene expression in the NET cell lines. Induction of apoptosis could also have been caused by the inhibition of c-Kit expression, in addition to the known mechanisms such as damage of DNA by topoisomerase II inhibition for this class of compounds. In summary, makaluvamine analogs DHN-II-84 and DHN-III-14 induced apoptosis, decreased neuroendocrine tumor markers, and showed promising antitumor activity in pulmonary, thyroid, and pancreatic NET cell lines, and hold potential to be developed as an effective treatment to combat neuroendocrine tumors.

Indexed as

Antineoplastic AgentsApoptosisBiomarkers, TumorCell Line, TumorCell ProliferationGene Expression Regulation, NeoplasticHumansNeuroendocrine TumorsProto-Oncogene MasProto-Oncogene Proteins c-kitPyrrolesAntineoplastic AgentsBiomarkers, TumorMAS1 protein, humanProto-Oncogene MasProto-Oncogene Proteins c-kitPyrrolesalkaloidcancermakaluvamineNETneuroendocrinetherapeutictumor

Identifiers

PMID33114525
PMCPMC7663375
OpenAlexW3096120142

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.