Expression and analysis and human G6PD

Human glucose-6-phosphate dehydrogenase (G6PD)

  • at Xq28 region, 18 kb 13 exons

  • 515 amino acids, 59.2 kDa

  • catalyses the first and rate limiting step in pentose phosphate pathway for the production of NADPH

    • protect cells from oxidative damage

G6PD deficiency

  • → reduced production of NADPH selectively affect RBCs

    • they rely solely on pentose phosphate pathway for NADPH as they do not have mitochondria

    • oxidative stress may damage membrane protein of RBCs → hemolysis

  • G6PD deficiency patients: acute haemolytic anaemia when

    • injection of oxidant drugs

    • infections

    • ingestion of fava beans

  • ~160 mutations reported

    • mutations may reduce activity or stability of G6PD

    • most G6PD-deficients are asymptomatic

    • HK: 4.3% male ; 0.5% female

Common G6PD variants in Chinese population

  • G6PD Canton

    • CGT → CTT

    • Arg459Leu

  • G6PD Kaiping

    • CGT → CAT

    • Arg463His

  • G6PD Gaohe

    • CAC → CGC

    • His32Arg

Recombinant DNA technology

Recombinant DNA

  • biologically active DNA

    • formed by the in vitro joining of segments of DNA from different sources

  • purpose

    • to clone genes

    • to make recombinant proteins when introduce to host cells

Traditional cloning process

  1. vector preparation

  2. insert preparation

  3. ligation

  4. transformation

  5. colony screening

Restriction enzyme-based cloning

Restriction enzyme

  • restriction endonucleases

  • recognise and cut DNA at secific nucleotide sequences

  • Types of end cut

    • cohesive (sticky) end: fragments with short single-stranded overhanging ends

    • blunt ends: even-length ends from both strands

Cloning vector

  • a replicating DNA molecule that carries a foreign NDA fragment to be introduced into cell

    • e.g. plasmid DNA

  • properties

    • replicate independently of the host cells

    • unique restriction enzyme cleavage sites

    • ︎ a reporter gene/ selectable marker to determine which host cells contain the recombinant DNA

  • elements contains

    • multiple cloning sites: for insertion of foreign DNA

    • origin of replication: allow recombinant DNA to replicate in bacteria

    • selectable marker: for identification of cells that have taken up the plasmid

      • e.g. antibiotic resistance gene

  • expression vector

    • cloning vectors that includes sequences needed for expression of the foreign DNA

      • for transcription and translation

    • composition

      • promoter

      • ribosome binding site

      • transcription termination

    • usage

      • foreign gene is inserted to to cloning site

        • i.e. between ribosome-binding sequence & terminator of transcription

      • promoter and other regulatory sequences from the host cell are also required

Procedures

  • cut DNA from different sources with the same restriction enzyme

    • → produce DNA fragments with compatible ends

  • join DNA fragments with compatible ends by DNA ligase

  • recombinant DNA is created

Common strategies

  • double digest

    • using 2 enzymes with non-compatible ends

    • insert ligated to vector in one orientation only

  • single digest

    • insert ligated to vector in either orientation

    • using 2 enzymes with non-compatible ends or compatible ends or 1 enzyme only

Plasmid subcloning

prepare insert DNA containing coding sequence of G6PD

  • digest pGEM-T-G6PD DNA (parent vector) with NdeI and XhoI (restriction enzymes) to release the coding sequencing

prepare vector DNA for cloning G6PD

  • digest pET28a vector DNA with NdeI & XhoI → create DNA ends compatible for ligation to G6PD insert DNA

  • as the sticky ends produced by NdeI and XhoI are not compatible → vector DNA do not religate

construct G6PD expression vector

  • G6PD (1.5kb) DNA insert is ligated to pET28a (5.3 kb) vector DNA by DNA ligase

    • ligated in only one orientation → ensure proper expression using vector-encoded T7 promoter

    • coding sequence is fused in-frame to His-tag

      • His-tag is a tag made up of 6 consecutive histadine residues

    • insert DNA to vector DNA molar ratio= 3: 1 or 1: 1

  • recombinant expression plasmid is formed, containing

    • origin replication

    • antibiotic resistance gene

    • G6PD coding sequence

introduce the recombinant expression plasmid to bacteria——E. coli

  • characteristics of E. coli

    • most widely used as it has simple and well-understood genetic environment in which to isolate foreign

    • universal genetic code → accept foreign DNA derived from any organism

    • replicate very 22 min → amplify foreign DNA rapidly

    • each bacterium can carry up to several hundred copies of cloned gene

  • induce transformation by

    • pre-treatment with CaCl2 to render cells susceptible (competent cells) to take up exogenous DNA

    • electroporation (short electric pulse)

  • DNA uptake

    • DNA pass through channels formed at adhesion zone (where outer and inner cell membranes are used to form pores in the cell wall)

    • heat shock create a thermal imbalance on either side of membrane → help pump DNA via the adhesion zone

selection, identification and characterisation of the recombinant clone

  • transformation efficiency

    • a measurement of the quality of competent cells

    • defined as the number of colonies formed per μg of uncut plasmid DNA

    • 10^5 per μg is adequate for simple cloning or subcloning

  • circular plasmid are more efficient for transformation than linear

  • bacteria can be transformed with

    • vector ligated to insert

    • self-ligated/uncut vector (w/o insert DNA)

    • uncut/nicked vector (w/o ligase)

  • identification methods

    • restriction enzyme analysis

      • recognition sequence in pET28a

        • one BglI, one EcoRV and one EcoRI

      • recognition sequence in pET28a-G6PD

        • two BglI and one EcoRV

  • colony PCR

    • insert-specific primer: positive applification confirms the insert’s presence

    • vector-specific primer: amplicon length determine the insert’s presence

    • insert- and vector-specific primer: PCR analysis of insert detection and amplicon length reveals cloning success

  • blue-white selection

    • insert DNA contains lacZ

    • product of lacZ turns X-gal to blue pigment

    • only bacteria that have taken up the plasmid grow in the presence of antibiotics

    • white colonies: bacteria that carry recombinant plasmid

    • blue colonies: bacteria that carry intact plasmid vector

  • DNA sequencing

    • positive clones should be confirmed by this method: ensure reading frame is correct and no extra mutations due to cloning process

pET expression system

Characteristics

  • high level of expression of recombinant protein → deleterious to cell

  • ︎ inducible system:

    • expression of gene of interest is normally repressed

    • induced to express after cell culture has grown to appropriately high density

  • expression of cloned gene is controlled by T7 promoter: specific to T7 RNA polymerase but not E. coli RNA polymerase

  • require bacterial strain to express T7 RNA polymerase: cloned into bacterial chromosome

    • expression is controlled by the operator site in promoter

Inducible operon

  • structural genes (lacZ, lacY, lacA for metabolism of lactose): encoding proteins to be transcribed

  • promoter (lacP): for binding of RNA polymerase to initiate transcription

    • regulated by operator sequence

  • operator (lacO): regulate transcription, binding of repressor to operator blocks transcription → RNA polymerase cannot bind to the operator

Repressor protein (lacI)

  • has to binding sites: for operator and inducer (lactose/ ITPG)

  • ╳ lactose → bind to operator → no transcription of operon

  • regulatory protein is synthesizd as an active repressor (constitutively expressed)

  • it becomes inactive when bind to inducer (lactose) → ︎ transcription of structural gene

Types of induction

ITPG induction

  • ╳ ITPG: repressor protein is binding on the operator

    • no gene is transcribed

  • ︎ ITPG: repressor is removed from the lac operator

    • induce gene expression

Auto induction

  • auto-induction medium

    • glucose:

      • preferentially used by bacteria → increase cells density

      • repress induction pof operator

    • lactose:

      • converted into allolactose in cell after glucose is depleted

      • auto induction of lac operon

    • glycerol:

      • support growth of cells

      • does not prevent induction

  • expression of recombinant protein in E. coli is induced when cells reached saturation

  • catabolite repression

    • presence of glucose lowers the cell concentration of cAMP

      • → less CAP protein bind to promoter

      • less efficient transcription of operon

    • regulatory protein CAP (catabolite activator protein)

      • bind to cAMP (cyclic adenosine monophosphate) → complex

      • complex bind to DNA (upstream of promoter) → more efficient binding of RNA polymerase to promoter and activate transcription

    • availability of glucose represses the enzyme for lactose utilisation

Protein purification

Considerations

  • identify a suitable source of the desired protein or overexpress the the protein as recombinant protein (usually tagged) in a suitable host organism

Cell extraction preparation

  • collect cells by centrifugation

  • cell distruption

    • lyse the cells by using

      • detergent or enzyme (lysozyme)

      • sonication

      • mechanical homogenisation

    • use protease inhibitors and low temperatures to minimise proteolysis

    • centrifugation to remove cell debris

Selective precipitation (crude separation)

  • add ammonium sulphate

    • highly hydrated: reduce protein solubility by decreasing concentration of water available for protein-solvent interaction

    • more hydrophilic proteins precipitate at a higher concentration of ammonium sulphate

  • add water-miscible organic solvent

    • change solvent polarity → increase protein-protein electrostatic interaction

    • allow protein aggregation & facilitate precipitation

  • alter pH

    • affect ionisation of amino, carboxyl and side chain group of amino acid

    • protein aggregate and precipitate at isoelectric point

      • pH=pI (number of -ve & +ve charge is equal)→ protein net charge =0

      • pH > pI → protein is negatively charged

      • pH < pI → protein is positively charged

Chromatography

  • general principle: components are separated by the affinity to the stationary phase or distribution between stationary and mobile phase

  • affinity chromatography

    • specific interaction between protein and ligand on matrix

    • elution condition depends on specific protein and ligand

    • examples

      • glutathione (ligand) & GST fusion protein (target protein)→ elute when reduced glutathione & low ionic strength

      • Ni2+ (ligand) & His-tagged protein (target protein)→ elute if high ionic strength and imidazole

      • antigen (ligand) & antibody (target protein)→ elution condition depends

Purification of his-tagged protein by Ni-NTA agarose column
  • affinity medium (Ni-NTA) is equilibrated in binding buffer

    • Ni-NTA= Ni2+ coupled with nitrilotriacetic (NTA)→ ︎ couple to agarose resin

  • target protein (his-tagged G6PD) binds to column; unbound material eluted from column

  • target protein is recovered by changing the condition: adding imidazole to favour elution of the bound proteins

    • imidazole compete with histamine for binding to Ni2+

  • affinity medium is re-equilibrated with binding buffer

  • Ion-exchange chromatography

    • based on electrostatic interaction between protein & matrix

    • selective elution by changing pH (net charge) or increasing ionic strength of elution buffer to compete with protein in binding to matrix

  • hydrophobic interaction chromatography

    • separate proteins according to surface hydrophobicity

    • high salt: promote adsorption of hydrophobic protein surface to hydrophobic matrix

      • reduce solvation of sample solutes & expose the hydrophobic regions along the surface of protein molecule

    • elute by decreasing ionic strength of buffer

  • gel filtration

    • separate proteins by size

    • larger proteins do not enter matrix→ elute first

    • smaller proteins enter pores of matrix → retarded differentially

Dialysis or ultrafiltration

  • force sample across a semipermeable membrane by gas pressure or centrifugal force

  • purpose

    • remove salt

    • exchange buffer and concentration of protein

Biological activity assay

Purpose

  • to detect the protein

Types

Continuous assay

  • continuously monitor wither the disappearance of a substrate or appearance of product

  • measure directly by

    • change in absorbance

    • fluorescence

    • pH

Discontinuous assay

  • product measured after reaction manually stopped or quenched at different time

Coupled assay

  • for substrate-product pairs wit o spectroscopic properties

  • product from reaction catalysed by enzyme of interest: substrate in a second enzymatic reaction → give a compound that an be detected directly

  • example:

    • hexokinase converts D-glucose to DG6P

    • DG6P is converted to 6PGL and NADPH

    • measure hexokinase activity by measuring the increase in NADPH

Measuring G6PD activity by continuous assay

Principle

  • NADPH absorb radiation at 340 nm but not NADP

  • absorbance at 340nm increase when NADPH accumulate

  • determine inițial rate by determining the slope of the linear portion of the curve

  • dilute enzyme preparation if the initial rate is too high to accurately determined

Purification summary table

  • enzyme activity (U): (ΔA340/min)*reaction vol/(6.22*enzyme vol)

    • amount of enzyme that convert 1 μmole substrate to product in 1 min

  • specific activity (U/mg): activity per unit weight

    • indicate protein purity and quality

    • should increase after each purification step

  • overall yield or recovery= total target protein or activity in fraction / total target protein or activity in crude extract

  • purification factor= specific activity of fraction/ specific activity in crude extract

Protein concentration determination

UV spectromentry

  • Absorbance at 280 nm by tryptophan and tyrosine and cystine

  • extinction coefficient of a protein at 280 nm (M^-1 cm^-1)= $ of tyrosine*ext(tyrosine) + # of tryptophan*ext(tryptophan) + # of cystine*ext(cystine)

  • disadvantage: can measure pure protein only

Dye-based method——Bradford method

  • protonated form of Coomassie Brilliant Blue G-250: orange or brown

  • dye becomes deprotonated when bind to side chain NH3+ group of protein→ blue

    • can be detected at 595nm

    • dye binds to proteins at Arg, His, Tyr, Trp, Phe

  • Disadvantage: affected by detergent in sample

  • sensitivity: 1-50 μg

Copper-based method

  • Lowry method

    • chelation(multiple bonds between organic molecules and metal) of Cu2+ by peptide bonds → reduction of Cu2+ to Cu+

    • Cu+ facilitate reduction of Folin reagent to a blue product → measured at 750nm

    • sensitivity: 5-100 μg

  • Bicinchoninic acid (BCA) method

    • Cu2+ in BCA reagent forms complexes with peptide bonds → reduce Cu2+ to Cu+

    • Cu+ interact with BCA to form a purple BCA-Cu+ complex → measured at 562nm

    • not compatible for samples with racing agent or copper chelating agents

    • sensitivity: 0.2-50 μg

SDS-PAGE

Purpose

  • check for purity of protein preparation

  • estimate protein molecular mass

  • for imumunodetection of protein

Procedures

  • Cast gel——stacking and resolving gel

  • sample preparation

    • determine sample protein concentration

    • pipet correct sample volume

    • add 2X or 4X loading buffer and boil sample for 5min

    • sample contains

      • DDT: reduce disulphate bridges

        • denature protein completely→ migration is not affected by protein secondary structure

        • protein subunits can separate independently

      • SDS

      • glycerol: add density to sample→ sink to bottom of wells

      • bromophenol blue: visualise samples in well & act as tracking dye

  • mount gel cassette into a vertical electrophoresis and apple gel running buffer

  • load the sample by electrophoresis

    • electrophoretic mobility of proteins in SDS-PAGE is inversely proportional to the logarithm of their mass

  • stain gel to visualise proteins

Discontinuous buffer system

  • buffer in tank is different from buffer in gel

  • different pH and % of acrylamide between stacking gel and resolving gel

stacking gel

  • concentrate all different seized proteins into a compact horizontal zone

  • proteins sandwiched between glycine molecules above and Cl- below

  • prevent protein bands from smearing and ensure good resolution

  • pH 6.8→ majority of glycine is zwitterionic (having both charges of functional groups) → lower mobility

  • mobility of ions: Cl- (completely ionised) > SDS > glycine

    • Cl- move away from Gly- to develop a voltage gradient → accelerate Gly-

    • → all ionic spices move at the same speed

    • protein samples are stacked between the Cl- and Gly- into a very thin zone before separation in resolving gel

resolving gel

  • separate gel by size

  • at pH8.8: Gly- is predominantly -ve charged → increase mobility and overtake protein (move directly behind Cl-)

  • when Gly- move pat protein molecules: unstacking protein

formation of polyacrylamide gel

  • polymerisation of acrylamide monomer with cross-linking agent bis-acrylamide

  • reaction is initiated by APS and TEMED

  • average pore size is determined by the concentration of acrylamide and proportion of the cross-linking bis-acrylamide

Sodium dodecyl sulphate (SDS)

  • an anionic detergent

  • confers constant -ve charge : size ratio

  • SDS-protein is a uniform rod shape→ ︎migrate according to size

Immunoblot——Western blot

Purpose

  • confirm the identity of a target protein by

    • size (from SDS-PAGE)

    • binding to specific antibody

  • monitor column fractions during protein purification

  • compare protein expression in different tissue disease conditions or response to drug treatment

  • for diagnosis of diseases (e.g. HIV)

Procedures

  • separate proteins by electrophoresis

  • visualise protein separation by Coomassie blue staining or colloidal gold

  • transfer protein from gel to membrane (wet tank transfer or semi-dry transfer)

    • proteins are eluted from the gel and adsorb onto membrane

  • verify protein transfer

    • prestained markers transferred to blot

    • total protein detection on membranes

      • Ponceau S (100-1000ng)

        • anionic dye

        • can be removed after visualisation

        • blots can be used for immunodetection

      • Colloidal gold (100og-1ng)

        • interfere with subsequent immnuodetection of proteins on western blots

      • fluorescent protein stains (2-8 ng)

  • blocking unbound site on membrane

    • to prevent non-specific binding of antibodies→ reduce background signals

  • antibody binding (primary and secondary antibodies) and detection

  • visualise data

Detection method

Antibodies

  • primary antibody

    • against the target protein or specific epitope on protein

    • e.g. anti-His antibody, anti-G6PD

  • secondary antibody

    • recognise and bind primary antibody

    • unusually conjugated to enzyme (AP or HRP) and detected by enzyme-substrate reaction

    • can also be conjugated to biotin, fluorophere r radioisotope

Direct vs indirect detection

  • direct: primary antibody is labeled or tagged with a enzyme

    • no secondary antibody is required

  • indirect: unlabeled primary antibody against target protein is used

    • primary antibody is detected by secondary antibody

Detection of His-tagged G6PD

  • primary antibody: rabbit anti-G6PD polyclonal antibody is used → raise against a peptide corresponding to human-G6PD amino acid positions 50-100

  • secondary antibody: goat anti-rabbit polyclonal antibody conjugated with AP

    • insoluble purple NBT diformazan product is produced when substrate NBT/BCIP is incubated with AP

  • enzymatic dephosphosrylation of CSPD by AP → emission of light at a max wavelength of 477 nm

    • detected using CCD camera or exposing the blot to X-ray film