Evidence map›Paper›PMID 31971799›Full record

ArticleJournal of medicinal chemistry2020

Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.

Karson J Kump, Lei Miao, Ahmed S A Mady, Nurul H Ansari, Uttar K Shrestha, Yuting Yang, Mohan Pal, Chenzhong Liao, Andrej Perdih, Fardokht A Abulwerdi and 6 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
2.0field-weighted citation impact, top 13% 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

10 citing papers in PubMed, 36 citations in OpenAlex.

  1. Article
  2. Article
  3. Small molecule Mcl-1 inhibitor for triple negative breast cancer therapy.Frontiers in cell and developmental biology · 2024
    Review
  4. Article
  5. Going Viral: An Investigation into the Chameleonic Behaviour of Antiviral Compounds.Chemistry (Weinheim an der Bergstrasse, Germany) · 2023
    Article
  6. Review
  7. Review
  8. Article
  9. Targeting MCL-1 in cancer: current status and perspectives.Journal of hematology & oncology · 2021
    Review
  10. 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

16 authors at 3 institutions in 2 countries.

Karson J Kump
Lei Miao
Nurul H Ansari
Uttar K Shrestha
Yuting Yang
Mohan Pal
Chenzhong Liao
Andrej PerdihNational Institute of Chemistry, Ljubljana 1000, Slovenia.
Fardokht A Abulwerdi
Krishnapriya Chinnaswamy
Jennifer L Meagher
Jacob M CarlsonDepartment of Pharmacology, College of Medicine, University of Arizona, Tucson, Arizona 85724, United States.
May KhannaDepartment of Pharmacology, College of Medicine, University of Arizona, Tucson, Arizona 85724, United States.ORCID 0000-0002-9989-6374
Jeanne A Stuckey
Zaneta Nikolovska-ColeskaORCID 0000-0001-6688-4206
University of Michigan · USUniversity of Arizona · USNational Institute of Chemistry · SI

Funding

XenograftP30CA046592 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI THEODORE S LAWRENCE · 1988 to 2026
$178.2M
Proteogenomics of Cancer Training ProgramT32CA140044 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI RAO, ARVIND, SARTOR, MAUREEN AGNES · 2010 to 2024
$3.9M
Novel Mcl-1 inhibitors for overcoming therapeutic resistance in colorectal cancerR01CA217141 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI NIKOLOVSKA-COLESKA, ZANETA, ZHANG, LIN · 2017 to 2021
$2.6M
Novel selective small-molecule inhibitors of Mcl-1 proteinR01CA149442 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI NIKOLOVSKA-COLESKA, ZANETA · 2010 to 2014
$1.5M
Training Program in Translational ResearchT32GM113900 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI LIEBERMAN, ANDREW P, NIKOLOVSKA-COLESKA, ZANETA · 2016 to 2020
$991k
Discovery and characterization of novel small molecule inhibitors of Mcl-1R21NS056915 · NINDS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI NIKOLOVSKA-COLESKA, ZANETA · 2006 to 2008
$229k
NCI NIH HHS P30 CA046592NCI NIH HHS R01 CA149442NCI NIH HHS R01 CA217141NCI NIH HHS T32 CA140044NIGMS NIH HHS T32 GM113900NINDS NIH HHS R21 NS056915
6 · The paper itself

Abstract

Anti-apoptotic Bcl-2 family proteins are overexpressed in a wide spectrum of cancers and have become well validated therapeutic targets. Cancer cells display survival dependence on individual or subsets of anti-apoptotic proteins that could be effectively targeted by multimodal inhibitors. We designed a 2,5-substituted benzoic acid scaffold that displayed equipotent binding to Mcl-1 and Bfl-1. Structure-based design was guided by several solved cocrystal structures with Mcl-1, leading to the development of compound

Indexed as

AnimalsAntineoplastic AgentsApoptosisBenzoic AcidCell Line, TumorHumansLymphomaMiceMice, TransgenicMinor Histocompatibility AntigensMolecular Docking SimulationMyeloid Cell Leukemia Sequence 1 ProteinProto-Oncogene Proteins c-bcl-2Antineoplastic AgentsBCL2-related protein A1Benzoic AcidMCL1 protein, humanMinor Histocompatibility AntigensMyeloid Cell Leukemia Sequence 1 ProteinProto-Oncogene Proteins c-bcl-2

Identifiers

PMID31971799
PMCPMC8024114
OpenAlexW3002208767

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.