Evidence map›Paper›PMID 33668938›Full record

ArticleMolecules (Basel, Switzerland)2021

Optimization and Anti-Cancer Properties of Fluoromethylketones as Covalent Inhibitors for Ubiquitin C-Terminal Hydrolase L1.

Aaron D Krabill, Hao Chen, Sajjad Hussain, Chad S Hewitt, Ryan D Imhoff, Christine S Muli, Chittaranjan Das, Paul J Galardy, Michael K Wendt, Daniel P Flaherty

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.7field-weighted citation impact, top 32% 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

3 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Article
  3. 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

10 authors at 2 institutions in 1 country.

Aaron D KrabillDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.ORCID 0000-0001-9265-4201
Hao ChenDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.ORCID 0000-0002-2070-5062
Sajjad HussainDivision of Pediatric Hematology-Oncology, Mayo Clinic, 200 First St. Guggenheim 15, Rochester, MN 55905, USA.
Chad S HewittDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.
Ryan D ImhoffDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.ORCID 0000-0002-8510-8437
Christine S MuliDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.
Chittaranjan DasDepartment of Chemistry, College of Science, 560 Oval Dr., West Lafayette, IN 47907, USA.ORCID 0000-0002-0567-7753
Paul J GalardyDivision of Pediatric Hematology-Oncology, Mayo Clinic, 200 First St. Guggenheim 15, Rochester, MN 55905, USA.
Michael K WendtDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.ORCID 0000-0002-3665-7413
Daniel P FlahertyDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, 575 Stadium Mall Dr., West Lafayette, IN 47907, USA.
Purdue University West Lafayette · USMayo Clinic · US

Funding

Purdue Drug Discovery Training ProgramT32GM125620 · NIGMS · PURDUE UNIVERSITY · PI DYKHUIZEN, EMILY CARLA, WEI, ALEXANDER · 2019 to 2023
$891k
NIGMS NIH HHS T32 GM125620
6 · The paper itself

Abstract

The deubiquitinating enzyme (DUB) UCHL1 is implicated in various disease states including neurodegenerative disease and cancer. However, there is a lack of quality probe molecules to gain a better understanding on UCHL1 biology. To this end a study was carried out to fully characterize and optimize the irreversible covalent UCHL1 inhibitor VAEFMK. Structure-activity relationship studies identified modifications to improve activity versus the target and a full cellular characterization was carried out for the first time with this scaffold. The studies produced a new inhibitor,

Indexed as

Antineoplastic AgentsCell Line, TumorCell ProliferationCell SurvivalDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansModels, MolecularMolecular StructureProtease InhibitorsStructure-Activity RelationshipUbiquitin ThiolesteraseAntineoplastic AgentsProtease InhibitorsUbiquitin ThiolesteraseUCHL1 protein, humancovalent inhibitorsdeubiquitinasesfluoromethylketonesUCHL1 inhibitors

Identifiers

PMID33668938
PMCPMC7956625
OpenAlexW3131313991

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.