Evidence map›Paper›PMID 24433221›Full record

ArticlePlatelets2015

CGX1037 is a novel PKC isoform delta selective inhibitor in platelets.

Dheeraj Bhavanasi, John C Kostyak, John Swindle, Laurie E Kilpatrick, Satya P Kunapuli

Open access · greenAbstract read
In one paragraph

Article in Platelets, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.2field-weighted citation impact, top 46% 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

7 citing papers in PubMed, 9 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

5 authors at 2 institutions in 1 country.

Dheeraj BhavanasiDepartment of Physiology, Temple University School of Medicine , Philadelphia, PA , USA .
John C Kostyak
John Swindle
Laurie E Kilpatrick
Satya P Kunapuli
Temple University · USCompleGen (United States) · US

Funding

Training in Thrombosis, Hemostasis and Vascular BiologyT32HL007777 · NHLBI · TEMPLE UNIV OF THE COMMONWEALTH · PI KUNAPULI, SATYA P. · 1993 to 2012
$5.2M
Functional PKC Isoforms in PlateletsR01HL093231 · NHLBI · TEMPLE UNIV OF THE COMMONWEALTH · PI KUNAPULI, SATYA P. · 2009 to 2017
$3.6M
Functional G Protein pathways in platelet activationR01HL081322 · NHLBI · TEMPLE UNIV OF THE COMMONWEALTH · PI KUNAPULI, SATYA P. · 2006 to 2010
$2.9M
Regulation and function of PDK1-Akt-Pyk2 axis in plateletsR01HL118593 · NHLBI · TEMPLE UNIV OF THE COMMONWEALTH · PI KUNAPULI, SATYA P. · 2013 to 2016
$1.9M
Novel Protein Kinase C Targeted Therapy for Acute Lung InjuryR01HL111552 · NHLBI · TEMPLE UNIV OF THE COMMONWEALTH · PI KILPATRICK, LAURIE E · 2012 to 2015
$1.5M
A novel therapeutic strategy for Acute Lung Injury: Inhibition of PKC-deltaR41GM103193 · NIGMS · COMPLEGEN, INC. · PI KILPATRICK, LAURIE E, SWINDLE, JOHN T. · 2012 to 2012
$355k
NHLBI NIH HHS HL07777NHLBI NIH HHS HL111552NHLBI NIH HHS HL118593NHLBI NIH HHS HL93231NHLBI NIH HHS R01 HL081322NHLBI NIH HHS R01 HL093231NHLBI NIH HHS R01 HL111552NHLBI NIH HHS R01 HL118593NHLBI NIH HHS T32 HL007777NIGMS NIH HHS R41 GM103193PHS HHS R416M103193
6 · The paper itself

Abstract

Platelets upon activation change their shape, aggregate and secrete alpha and dense granule contents among which ADP acts as a feedback activator. Different Protein Kinase C (PKC) isoforms have specific non-redundant roles in mediating platelet responses including secretion and thrombus formation. Murine platelets lacking specific PKC isoforms have been used to evaluate the isoform specific functions. Novel PKC isoform δ has been shown to play an important role in some pathological processes. Lack of specific inhibitors for PKCδ has restricted analysis of its role in various cells. The current study was carried out to evaluate a novel small molecule PKCδ inhibitor, CGX1037 in platelets. Platelet aggregation, dense granule secretion and western blotting experiments were performed to evaluate CGX1037. In human platelets, CGX1037 inhibited PAR4-mediated phosphorylation on PKD2, a PKCδ-specific substrate. Pre-treatment of human or murine platelets with CGX1037 inhibited PAR4-mediated dense granule secretion whereas it potentiated GPVI-mediated dense granule secretion similar to the responses observed in murine platelets lacking PKCδ· Furthermore, pre-treatment of platelets from PKCδ(-/-) mice with CGX1037 had no significant additive effect on platelet responses suggesting the specificity of CGX1037. Hence, we show that CGX1037 is a selective small molecule inhibitor of PKCδ in platelets.

Indexed as

AnimalsBlood PlateletsHumansInhibitory Concentration 50MiceMice, KnockoutPhosphorylationPlatelet AggregationPlatelet Membrane GlycoproteinsProtein Kinase C-deltaProtein Kinase D2Protein Kinase InhibitorsProtein KinasesProtein TransportSecretory VesiclesPlatelet Membrane Glycoproteinsplatelet membrane glycoprotein VIProtein Kinase C-deltaProtein Kinase D2Protein Kinase InhibitorsProtein KinasesCGX1037GPVIplatelet dense granule secretionprotease activated receptor-4Protein kinase Cδprotein kinase D2

Identifiers

PMID24433221
PMCPMC4101062
OpenAlexW2040195175

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.