Evidence map›Paper›PMID 31812677›Full record

ArticleBiochemical pharmacology2020

Development and preclinical pharmacology of a novel dCK inhibitor, DI-87.

Soumya Poddar, Edmund V Capparelli, Ethan W Rosser, Raymond M Gipson, Liu Wei, Thuc Le, Michael E Jung, Caius Radu, Mina Nikanjam

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

Article in Biochemical pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
0.4field-weighted citation impact, top 44% 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

9 citing papers in PubMed, 18 citations in OpenAlex.

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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

9 authors at 3 institutions in 1 country.

Soumya PoddarDepartment of Molecular and Medical Pharmacology, University of California Los Angeles, Los Angeles, CA, United States.
Edmund V CapparelliDivision of Host-Microbe Systems, University of California San Diego, San Diego, CA, United States.
Ethan W RosserDepartment of Molecular and Medical Pharmacology, University of California Los Angeles, Los Angeles, CA, United States; Department of Chemistry and Biochemistry, University of California Los Angeles, Los Angeles, CA, United States.
Raymond M GipsonDepartment of Chemistry and Biochemistry, Santa Clara University, Santa Clara, CA, United States.
Liu WeiDepartment of Molecular and Medical Pharmacology, University of California Los Angeles, Los Angeles, CA, United States.
Thuc LeDepartment of Molecular and Medical Pharmacology, University of California Los Angeles, Los Angeles, CA, United States.
Michael E JungDepartment of Chemistry and Biochemistry, University of California Los Angeles, Los Angeles, CA, United States.
Caius RaduDepartment of Molecular and Medical Pharmacology, University of California Los Angeles, Los Angeles, CA, United States.
Mina NikanjamDivision of Hematology-Oncology, University of California San Diego, La Jolla, CA, United States. Electronic address: mnikanjam@ucsd.edu.
University of California, Los Angeles · USUniversity of California, San Diego · USSanta Clara University · US

Funding

Women's CancersP30CA016042 · NCI · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI Samuel Wheeler French · 1985 to 2026
$134.5M
TRAINING & OUTREACH COREU54HD071600 · NICHD · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI BRADLEY, JOHN S · 2011 to 2015
$3.6M
Training for Academic HematologyT32HL066992 · NHLBI · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI CHUTE, JOHN P, TIMMERMAN, JOHN M · 2002 to 2017
$3.6M
Safety and Dose Optimization of High-Dose Anakinra in Kawasaki DiseaseU54HD090259 · NICHD · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAPPARELLI, EDMUND VINCENT, NIZET, VICTOR · 2016 to 2018
$2.2M
Developing Pediatric Clinical Pharmacologists for the Advancement of TherapeuticsT32HD087978 · NICHD · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI NIZET, VICTOR, TREMOULET, ADRIANA H · 2016 to 2025
$1.5M
NCI NIH HHS P30 CA016042NHLBI NIH HHS T32 HL066992NICHD NIH HHS T32 HD087978NICHD NIH HHS U54 HD071600NICHD NIH HHS U54 HD090259
6 · The paper itself

Abstract

backgroundDeoxycytidine kinase (dCK) is an essential enzyme for production of nucleotides via the salvage pathway; DI-87 is a novel dCK inhibitor in preclinical development for use in anticancer therapy. The current study utilizes PET imaging to evaluate PK-PD relationships and to determine optimal dosing of the drug.

methodsNSG mice bearing CEM tumors had plasma and tumor PK assessed using mass spectrometry following oral administration of DI-87. dCK inhibition was assessed after a single dose of oral DI-87 followed by a [

resultsDI-87 had an in vitro EC

conclusionsDI-87 is a promising new compound for use in combination therapy against tumors expressing dCK. Utilizing a [

Indexed as

AnimalsAntineoplastic AgentsCell LineCell ProliferationDeoxycytidine KinaseDose-Response Relationship, DrugDrug Therapy, CombinationGene Expression Regulation, EnzymologicHumansMaleMiceMolecular StructureNeoplasms, ExperimentalAntineoplastic AgentsDeoxycytidine KinaseDeoxycytidine kinaseDI-87PET scanPharmacodynamicsPharmacokineticsPreclinical

Identifiers

PMID31812677
PMCPMC6981055
OpenAlexW2991776190

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.