JC 1

Question 1

What is the rationale of the study done by Mahmmud Yar?

Answer 1

In vitro modulatory effects of functionalized pyrimidine and piperidine derivatives (activating or deactivating) on Aryl hydrocarbon receptor (AhR) and glucocortiod receptor (GR) activities

Question 2

what are the biological activities of piperidine?

Answer 2

antibacterial, anti-inflammatory, antimalarial, and also act as enzyme inhibitor for farnesyl transferase

Question 3

what is Aryl receptor and what is its function?

Answer 3

is a ligand-activated transcription factor which links environmental chemical stimuli with adaptive responses such as detoxification (but it also plays a role in mediating toxicity)

Question 4

where is Aryl located?

Answer 4

it resides in cytosol and upon binding of the ligand it translocates into nucleus. When activated by dioxin, the cytosolic AhR protein complex translocates into the nucleus and dimerizes with the ARNT (Ah receptor nuclear translocator) protein. The heteromeric ligand:AhR/Arnt complex then recognizes and binds to its specific DNA recognition site, the dioxin response element (DRE) –> the expression of many genes are increased and also the expression of biotranformation enzyme such as cytochrome P450

Question 5

How does Aryl receptor cause formation of toxin-DNA adducts?

Answer 5

this receptor is mediator of genotoxic or carcinogenic action of some toxicants via their increased biotransformation with consequent facilitating the formation of toxin-DNA adducts

Question 6

what is glucocorticoid receptor (GR)?

Answer 6

is a ligand-dependent transcriptional factor and is involved in phase I, phase II, and indirectly phase III (transmembrane export) of exogenous compounds detoxification.

Question 7

how does the molecular mechanism of endocrine disruption affect GR?

Answer 7

leads to competition of physiological glucocorticoids with exogenous compounds with affinity towards GR

Question 8

What is the function of GR?

Answer 8

toxicity-mediated effects such as apoptosis and lymphocytes and neural degradation in response to stress

Question 9

What is TCL?

Answer 9

Thin-layer chromatography (TLC) is a chromatography technique used to separate non-volatile mixtures. After the sample has been applied on the plate, a solvent or solvent mixture (known as the mobile phase) is drawn up the plate via capillary action

Question 10

why a molecular docking approach was carried out?

Answer 10

to determine with which residues from the binding site from AhR and GR the compounds interact

Question 11

what is molecular docking?

Answer 11

Molecular docking is a kind of bioinformatic modelling which involves the interaction of two or more molecules to give the stable adduct. Depending upon binding properties of ligand and target, it predicts the three-dimensional structure of any complex

Question 12

What is Luciferase activity?

Answer 12

luciferase is commonly used as a reporter to assess the transcriptional activity in cells that are transfected with a genetic construct containing the luciferase gene under the control of a promoter of interest.

Question 13

What is the function of IRCBM1325?

Answer 13

is a weak antagonist towards Ah receptor at relative high concentration

Question 14

What is TCDD?

Answer 14

TCDD is a potent agonist with high binding affinity to the aryl hydrocarbon receptor (AhR), which is extensively used to study the impact of AhR activation on various physiological and immune functions

Question 15

What is reporter assay?

Answer 15

Reporter genes are genes whose products can be readily assayed subsequent to transfection, and can be used as markers for screening successfully transfected cells, for studying regulation of gene expression, or serve as controls for standardizing transfection efficiencies.

Question 16

What is negative control group?

Answer 16

A negative control group is a control group that is not exposed to the experimental treatment or to any other treatment that is expected to have an effect. These sorts of controls are particularly useful for validating the experimental procedure.

Question 17

What is positive control group?

Answer 17

A positive control group is a control group that is not exposed to the experimental treatment but that is exposed to some other treatment that is known to produce the expected effect. These sorts of controls are particularly useful for validating the experimental procedure.

Question 18

what is the difference between positive and negative control group?

Answer 18

“Negative control” is a treatment that by definition is expected not to have any effect (neither positive effect, nor negative effect). “Positive control” is treatment with a well-known chemical that is known to produce the expected effect with the assay that you are studying.

Question 19

What is MTT assay?

Answer 19

The MTT assay is used to measure cellular metabolic activity as an indicator of cell viability, proliferation and cytotoxicity

Question 20

What are HeLa cells?

Answer 20

HeLa cells are first immortal human cells and used by scientists to develop a cancer research method that tests whether a cell line is cancerous or not. This method proves so reliable that scientists use it to this day.

Question 21

What are HpG2 cells?

Answer 21

HepG2 is a human hepatoma that is most commonly used in drug metabolism and hepatotoxicity studies. HepG2 cells are nontumorigenic cells with high proliferation rates and an epithelial-like morphology that perform many differentiated hepatic functions.