* CGX1037 is a novel PKC isoform delta selective inhibitor in platelets.
- 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.
=>1.〜に慣れて, 2.用いられた, 中古の
Overview of verb use
The verb use has 6 senses (first 3 from tagged texts)
1. (603) use, utilize, utilise, apply, employ -- (put into service; make work or employ for a
particular purpose or for its inherent or natural purpose; "use your head!"; "we only use Spanish at
home"; "I can't use this tool"; "Apply a magnetic field here"; "This thinking was applied to many
projects"; "How do you utilize this tool?"; "I apply this rule to get good results"; "use the
plastic bags to store the food"; "He doesn't know how to use a computer")
2. (12) use, habituate -- (take or consume (regularly or habitually); "She uses drugs rarely")
3. (8) use, expend -- (use up, consume fully; "The legislature expended its time on school
questions")
4. use -- (seek or achieve an end by using to one's advantage; "She uses her influential friends to
get jobs"; "The president's wife used her good connections")
5. practice, apply, use -- (avail oneself to; "apply a principle"; "practice a religion"; "use care
when going down the stairs"; "use your common sense"; "practice non-violent resistance")
6. use -- (habitually do something (use only in the past tense); "She used to call her mother every
week but now she calls only occasionally"; "I used to get sick when I ate in that dining hall";
"They used to vacation in the Bahamas")
Overview of adj used
The adj used has 3 senses (first 3 from tagged texts)
1. (4) used -- (employed in accomplishing something; "the principle of surprise is the most used and
misused of all the principles of war"- H.H.Arnold & I.C.Eaker)
2. (1) exploited, ill-used, put-upon, used, victimized, victimised -- (of persons; taken advantage
of; "after going out of his way to help his friend get the job he felt not appreciated but used")
3. (1) secondhand, used -- (previously used or owned by another; "bought a secondhand (or used)
car")
--- WordNet end ---