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Chapter 2 – Materials and Methods

2.6 Confocal microscopy

HEPES-buffered saline solution (HBSS; 147 mM NaCl, 24 mM KCl, 1.3 mM

CaCl2, 1 mM MgSO4, 10 mM HEPES, 2 mM sodium pyruvate, 1.43 mM NaHCO3,

pH 7.45) containing 4.5 mM D-glucose was used as the imaging buffer in all

experiments outlined below and was pre-warmed before use to the stated

temperature in which the experiments were carried out. Imaging buffer was

used to dilute both BODIPY-TMR-CGP and BODIPY630/650-S-PEG(8)-

propranolol fluorescent ligands from a 1 mM DMSO stock to achieve the

DMSO

0.01 % (v/v; final concentrations), reducing potential harmful effects of this

solvent on the cells (Brayton, 1986). Incubation of cells in a cell culture

incubator refers to a 5 % CO2/95 % air atmosphere.

SNAP-tag labelling

C SNAP D A 1-adrenoceptors

were grown to confluence in 8-well plates as described above (see Cell

culture). Prior to experimentation, the growth medium was removed off the

cells and replaced with fresh medium containing 1 µM of the cell

impermeable SNAP-tag substrate SNAP-Surface® 488 (BG-488; New England

Biolabs, Ipswich, MA). The cells were then incubated at 37 °C in a cell culture

the medium containing the SNAP-tag substrate was removed and the cells

were washed twice in imaging buffer (pre-warmed to 37 °C), before

incubating the cells in 200 µL imaging buffer in a cell culture incubator (37 °C)

for a further 30 minutes in the dark. Finally, the imaging buffer was replaced

with 400 µL fresh imaging buffer and the cells used immediately for imaging.

Saturation binding experiments

The protocol used here was based on that described by Baker et al. (2003d)

BODIPY TMR CGP CHO 2-adrenoceptor.

BODIPY-TMR-CGP and BODIPY630/650-S-PEG8-propranolol saturation binding

experiments were performed at room temperature (circa 21 °C) using CHO-

1 CS CHO 2-CS cells seeded into 8-well plates (as described in Cell

culture). Immediately prior to experimentation, the growth medium was

removed and the cells were then washed once with imaging buffer, before

the addition of 360 µL imaging buffer to each well. The 8-well plate was

placed onto the microscope stage and 40 µL (i.e. 10x dilution to final

concentration) of a range of concentrations from 3-100 nM (final

concentrations) of either BODIPY-TMR-CGP or BODIPY630/650-S-PEG8-

propranolol were added to designated wells. The cells were exposed to the

fluorescent ligand for 10 minutes before imaging. To ensure strict exposure

time for all cells and to allow circa 5 minutes to image each well, the addition

of fluorescent ligands to designated wells was staggered.

This method was also based on that described by Baker et al. (2003d) for the

BODIPY TMR CGP CHO 2-adrenoceptors. BODIPY-

TMR-CGP and BODIPY630/650-S-PEG(8)-propranolol inhibition binding

experiments were performed at room temperature (circa 21 °C) using CHO-

1 CS CHO 2-CS cells seeded into 8-well plates (as described in Cell

culture). CHO-CS cells were used as a negative control. On the day of

experimentation, the growth medium was removed and the cells washed

once with pre-warmed imaging buffer, before 360 µL of imaging buffer was

added to the positive control well, measuring total binding, and the negative

control well (containing CHO-CS cells), measuring non-specific binding levels.

360 µL of imaging buffer containing increasing concentrations of the

competitor (0.01-1000 nM) was added to the designated wells. The cells were

then incubated for 30 minutes at 37 °C in a cell culture incubator. Following

this, the plate was mounted on the microscope stage and the experiment

started by the addition of 40 µL of the desired concentration of the

fluorescent ligand to the first well, which was imaged after a further 10

minutes. To ensure the same exposure time of cells to the fluorescent ligand

in all wells and to allow a 5 minute imaging time for each well, the addition of

the fluorescent ligand and imaging of the wells was staggered and carefully

timed. Where cells expressing SNAP-tagged receptors were used, the SNAP-

tag labelling was performed first (as described above) and the 30 minute

incubation step following the washout of the SNAP-tag substrate was

Internalisation experiments

F SNAP 1-adrenoceptor cells were

seeded into 8-well plates as described in Cell culture and the SNAP-tagged

receptors were labelled as described above, but using 360 µL imaging buffer

in the final incubation step. Next, the 8-well plate was mounted onto the

microscope stage. The unlabelled ligands to be used were diluted in imaging

buffer to the desired concentrations (10x final concentration). Before addition

of any ligands, the first well was imaged to allow optimisation of microscope

settings (laser power, gain and offset), which were then kept constant for all

other wells throughout the experiment. Following this, 40 µL of the ligand

was added to the first well and imaged immediately (at a different site than

that used to determine the microscope settings; time point 0 minutes). After

60 minutes incubation of the ligand, the well was imaged again (time point 60

minutes).

Bimolecular fluorescence complementation (BiFC) experiments

Using the bimolecular fluorescence complementation (BiFC) approach, two

non-fluorescent N- and C-terminal halves of a fluorescence protein (e.g.

yellow fluorescence protein, YFP) are attached to two potentially interacting

proteins (e.g. dimerising receptors). Upon receptor dimerisation, the two non-

fluorescent YFP halves then come together and reconstitute the full length

fluorescent YFP, thus the detection of YFP fluorescence indicates an

interaction of the two proteins studied and was used in this thesis to detect

seeded into wells of an 8-well plate (day 1) and transiently transfected with

YFPN-tagged and YFPC 1-adrenoceptor recombinant DNA the

following day (day 2) as described in Generation of new cell lines. The next

day (day 3), the transfection medium was removed off the cells and replaced

with fresh growth medium, before the cells were placed back into the cell

culture incubator (37 °C, 5 % CO2/95 % air atmosphere). After circa 6 hours,

the cells were then moved into a 30 °C incubator (5 % CO2/95 % air

atmosphere) to allow the maturation of the fluorophore following correct

protein folding. On day 4, the cells were used for experimentation.

Confocal imaging

All confocal imaging experiments were performed on the Zeiss LSM710

confocal microscope (unless otherwise stated) with a Zeiss 40x1.3NA oil

immersion lens (Zeiss, Jena, Germany). The laser that emits light at a

wavelength closest to the wavelength needed to cause maximum excitation

of the chosen fluorophore was used. Upon excitation, the fluorophore then

emits light itself at a longer wavelength, which is captured using the

appropriate wavelength filter. The fluorophores, lasers and microscope

settings used throughout this thesis are summarized in Table 2.2. The pinhole

diameter used in all confocal experiments was 1 airy unit (AU), which

represents a near optimal setting that reduces out-of-focus emission

contributions without the loss of intensity of the measured fluorophore. The

pinhole setting and the laser wavelength used determine the optical slice

the thinner the optical slice). The first well of an 8-well plate was used for

calibration in each experiment. The cells were imaged and the range indicator

was set to determine brightness (detector gain) of the bound ligand and the

contrast (amplitude offset) such that pixels were either over-saturated or

below the detection limit. The maximal image brightness was then set to a

value greater than that achieved with the control well so that brighter binding

could be detected. The confocal settings (laser power, digital values for image

brightness, background and contrast) were then kept constant for the rest of

the experimental day. This allowed direct comparisons between wells to be

made. This area of the first well used to determine the settings was subjected

to laser exposure much more than any other area and hence had potential for

more photobleaching. A second area of the well was therefore selected for

Table 2.2 Excitation and emission wavelengths of the fluorescent molecules used in studies within this thesis are listed together with the lasers and microscope settings used to image cells treated with these fluorescent molecules.

fluorophore excitation/emission laser type laser wavelength

Microscope settings used

emission filter gain offset optical slice

BG-488 506/526 Argon 488 nm 505 nm long-pass 600-1100 0-1 0.37 µm

BODIPY-TMR-CGP 545/570 Helium-Neon 543 nm 550 nm long-pass 600-1100 0-1 0.40 µm

BODIPY-TMR-CGP 545/570 Helium-Neon 561 nm 565 nm long-pass 600-1100 0-1 0.41 µm

BODIPY630/650-S-PEG(8)-propranolol 630/650 Helium-Neon 633 nm 650 nm long-pass 600-1100 0-1 0.46 µm

Where two lasers were used at the same time (e.g. 488 nm and 561 nm lasers

BODIPY TMR CGP SNAP 1-adrenoceptors), the

multitracking facility in the Zeiss imaging software was used. This allowed the

sample to be illuminated with one laser at a time in order to avoid any bleed

through of the laser used (e.g. 488 nm) causing excitation of the fluorophore

used (e.g. BODIPY-TMR-CGP). For the same reason, the emission filter of the

higher energy fluorophore was also adjusted (e.g. 505-550 nm band-pass

filter was used to capture BG-488 fluorescence). Furthermore, the pinhole

(thus the optical slice thickness) was set for the highest wavelength laser used

(i.e. 561 nm laser, if both 488 and 561 nm laser where used) and the optical

slice thickness was then matched for the second laser. Using two lasers also

increased the total well laser exposure time. To correct for that, fewer frames

were taken (4-8 frame scans, 1024x1024 pixels), thus limiting each image to

approximately one minute laser exposure.

Data collection

Using 8-well plates limits the number of experimental conditions that can be

tested in a given experiment. In the experiments described above, every well

represented a different experimental condition (e.g. different concentration

of fluorescent ligand or inhibitor ligand or internalising ligand). However, 2-4

different areas were imaged within a given well and each image was analysed

as described below, thus providing duplicate to quadruplicate measures per

thesis for these experiments, however, refer to number of separate

experiments set up and carried out (i.e. different experimental days).

Total image intensity analysis

All images taken on the Zeiss LSM710 microscope were captured using an 8bit

greyscale, which allows for 256 different intensity levels of a given pixel (from

0-255; where 0 represents the weakest and 255 the strongest fluorescence

intensity). All data analysis was carried out using Zeiss Zen2010 software (Carl

Zeiss, Jena, Germany). This provides the frequency of pixels recorded at each

of the 256 greyscale intensities for each image taken. The total image

intensity (arbitrary units) is calculated as the sum of the product of frequency

x greyscale intensity for each of the 256 grey scale intensity values. This value

was then divided by the total number of pixels per image (1024x1024 for the

total image) to give the average pixel intensity.

Region of interest (ROI) analysis

Where stated, regions of interest were drawn around the membrane of a

given number of cells (stated for each experiment) in each image taken. The

Zeiss software provides the frequency of pixels recorded at the 256 greyscale

intensities and the number of pixels in the combined area of the drawn

regions of interest of one image, and thus allows quantitative analysis as

described above using average pixel intensities that refer to the regions of

Co-localisation analysis

Where two different wavelengths were used to image two different

fluorescently labelled molecules (e.g. SNAP-tagged 1-adrenoceptor using 488

nm and BODIPY-TMR-CGP binding using 561 nm excitation wavelengths), the

individual images obtained for each wavelength were merged. These images

are shown in colour, where yellow pixels clearly identify regions of spatial

overlap of the two fluorescently labelled molecules. The fluorescence

intensities of each individual channel, however, are shown in monochrome to

allow better visualisation of the greyscale intensities of the pixels in each

channel (from 0, i.e. black, to 255, i.e. white pixels).

Where used, a co-localisation plot was obtained and a crosshair placed on this

plot to highlight the region of co-localised pixels (region 3). To do this, a

region of interest was drawn on the background of the image away from the

cells and the average intensity and its standard deviation (SD) of this region

were collected in each of the two channels. The crosshair was then placed to

the intensity levels calculated from adding the average background pixel

intensity to 2x its standard deviation. This represents the background

fluorescent intensity. Pixels with intensity values greater than those

calculated in both channels will be located in region 3 and represent co-