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2.2 Methods:

2.2.8 Next generation sequencing

2.2.8.5 Sequencing

2.2.8.5.1 Chip preparation

Ion Proton chip adaptor was attached to the chip exit well. 200µL of

100% isopropanol was injected into the chip loading port; the expelled liquid

was removed from the exit well. The isopropanol was aspirated from the chip

for 5-10 secs to ensure that the chip is dry. 100µL of Ion PI chip preparation

solution was injected into the chip loading port; the expelled liquid was removed

from the exit well. The chip was place on a 50°C heat block for 2 mins. 200µL

of 100% isopropanol was injected into the chip loading port; the expelled liquid

was removed from the exit well. This was repeated a total of two times. 200µL

of nuclease free water was injected into the chip loading port; and the expelled

liquid removed. 200µL of 0.1M NaOH was then injected into the chip loading

port, and the expelled liquid was removed from the exit well. The chip was

incubated at room temperature for 1 min then 200µL of nuclease free water was

injected into the chip loading port. These steps were repeated a total of three

times. 200µL of 100% isopropanol was injected into the chip loading port; the

expelled liquid was removed from the exit well. 100µL of 100% isopropanol

was pipetted onto the chip loading well, the liquid was then removed from the

same well. The Ion Proton chip adapter was removed from the chip.

2.2.8.5.2 Loading of sample on the chip

centrifuged for 30 secs in the Ion Chip Minifuge followed by injection of 100µL

of foaming solution and then centrifuged again for 30 secs. The chip was

injected with 100µL of the flushing solution 2 times; the expelled solution was

discarded after each injection. 100µL of 50% annealing buffer was injected into

the chip loading port three times; the expelled liquid was removed between each

injection. 65µL of polymerase solution (6µL Ion PI Sequencing polymerase

with 60µL 50% annealing buffer) was injected; the expelled liquid was

removed. The chip was left to incubate for 5 mins then secured in the Ion Proton

sequencer.

2.2.9 Nucleofection using siRNA

CASMCs were seeded at 100,000 cells/well (5mM DMEM, 10% FBS,

no antibiotics) in a 24 well plate (Nunc). The cells were incubated at 37oC in 5%

CO2 until they reached 70-80% confluency then serum deprived (5mM DMEM,

0.1% FBS, no antibiotics) for 24 hours prior to Nucleofection. Using the Lonza

AD1 4D-Nucleofector Y kit, 1mL of the supplement was mixed with 4.5mL of

AD1 4D-Nucleofector solution. 105pmol of siRNA was made up with 350µL

Nucleofector solution. The media was carefully removed and 350µL of the

siRNA substrate solution was carefully transferred into each well. The 24 well

dripping electrode array was inserted into the 24 well plate. The Nucleofection

process began when the plate was placed in 4D-Nucleofecor core Y-unit using

ER137 pulse. The 24 well dipping electrode array was carefully removed from

24 well plate. The siRNA substrate solution was removed from each well and

immediately replaced with 1mL of pre-warmed medium (5mM DMEM,

stated otherwise) before they were treated with agonists to assess mRNA

expression.

2.2.10 Statistical Analysis

Data was normalised and is shown as the mean ± standard error of the mean of three independent experiments, unless stated otherwise. A one-way ANOVA was used to calculate statistical significance of normalised data as stated followed by least significant difference post-hoc analysis. Results were considered significant when the probability was less than 0.05 and 0.01.

Chapter-3. Proteinase activated

receptor-1 mediated dual kinase

receptor transactivation

stimulates the expression of

glycosaminoglycan synthesizing

3.1 Introduction

Seven transmembrane GPCRs are the largest group of cell surface

receptors in biology. GPCR signalling involves the traditional cascade which

will be referred to as transactivation-independent signalling (Kamato et al.,

2014b) or GPCR mediated transactivation of cell surface PTKR. Two decades

ago the initial finding of transactivation described GPCR activation of the

PTKR, EGFR, stimulating the immediate downstream products phospho-Erk1/2

(Daub et al., 1996). This discovery greatly expanded the known functions of

GPCRs.

The paradigm of GPCR mediated kinase receptor transactivation has

been expanded to include GPCR mediated activation of S/TKR, in particular the

TGFBR1 (Burch et al., 2010, Burch et al., 2013, Little et al., 2010, Ivey and

Little, 2008). PAR-1 transactivation of the TGFBR1 is studied by the

phosphorylation of the immediate downstream intermediate of TGFBR1, Smad2

in the carboxy terminal (phospho-Smad2C) (Burch et al., 2010, Little et al.,

2010). Thrombin stimulation of human VSMCs leads to the synthesis of the

ECM molecules proteoglycans. Recently our lab reported that thrombin

treatment of VSMCs leads to an increase in radio sulphate incorporation into

secreted proteoglycans a response which is approximately equally blocked by

antagonists of the EGFR (AG1478) and the TGFBR1 (SB431542). The two

blocked by the PAR-1 antagonist SCH79797 (Burch et al., 2010, Burch et al.,

2013).

Previous work has shed light on the specific enzymes which mediate the

synthesis of CS/DS GAG chains on proteoglycans (Sugahara and Kitagawa,

2000, Silbert and Sugumaran, 2002). The synthesis of CS/DS GAG chains on

proteoglycans involves the concerted action of a number of GAG synthesizing

genes (Mikami and Kitagawa, 2013). The growth factor and hormone signalling

pathways that control the expression of these enzymes are important because

GAG hyperelongation is a critical step in the early development of

atherosclerosis (Ivey et al., 2008, Getachew et al., 2010a, Ivey and Little, 2008).

During the progression of atherosclerosis, the elongation of CS chains in the

arterial wall involves at least four GAG synthesizing genes specifically

CHST11, CHSY1, CHPF, and chondroitin N-acetylgalactosaminoglycan-2

(Anggraeni et al., 2011) (Refer to Chapter 1 Section 1.3 for more details).

Increased LDL binding in the 8 weeks of the development of atherosclerosis

was associated with an elevated mRNA expression of the four genes. CHST11

and CHST3 are sulfotransferases whereas CHPF and CHSY1 are

glycosyltransferases which are directly involved in the synthesis of the GAG

chains thus the regulation of proteoglycan size (Izumikawa et al., 2011). As

such, the signalling pathways leading to the expression of these GAG

synthesizing enzymes represent potential therapeutic targets for the treatment of

atherosclerosis.

Proteoglycans secreted by VSMCs in vivo are present in early

atherosclerotic lesions (Nakashima et al., 2007). Thrombin treatment of VSMCs

leads to the hyperelongation of GAG chains of proteoglycans such as biglycan

described to be involved in this signalling cascade, however the downstream

gene targets presumably the specific GAG synthesizing enzymes that are

involved remain unknown. This chapter seeks explores the role of

transactivation dependent signalling pathways that mediated GAG gene

expression.

3.2 Materials and Methods

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