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Calcineurin inhibitors (Immunosuppressants): Mechanism of action

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This video explain the mechanism of action of Calcineurin Inhibitors a major category of immunosuppressants. I hope you will enjoy the learning with us. If you have any doubt or want any topic explained by us then let me know…

Good morning friends today we will see the mechanism of action of kelsey newton inhibitors so kelsey newton inhibitors calcineurin inhibitors is the main therapy for immunosuppression so they are the immunosuppressant agents which are used in the organ transplant or in the autoimmune diseases this is the main first set of first-line therapy for that and we have the

Two drugs in it one is they cyclosporine and another is a true limas so we have two drug in it one is cyclosporine and another is a cro limas this both drug is inhibiting the galaxy nuran inside the helper t cells so when the cyclosporine is taken it enters into the helper t cell where it will bind with the protein called as the cycle of filling and this complex is

Inhibiting the calcineurin activity while d’ĂȘtre limors is when it is given it binds with the protein fk bp it’s a fk506 binding protein so it makes a complex with this protein and this whole complex is inhibiting the calcineurin so this both drug cyclosporine and tacrolimus they both have inhibiting the canary so once this calcineurin is inhibited they causes

The inhibition of the phosphorylation of one another protein b phosphorylation of and fed this inside is the nuclear factor of activated t cells so inhibition of the calcium causes the inhibition of the phosphorylation of n fact that leads to the in the mrna synthesis of interleukin 2 so decrease in the mrna synthesis for interleukin 2 and that’s why they causes

A decrease in the interleukin 2 synthesis so interleukin 2 synthesis is reduced and because of that the t cell proliferation p cell proliferation is reduced and t cell proliferation so amount of t cell is reduced and that causes a decrease in the immunity so calcineurin inhibitor as we have discussed the calcineurin inhibitors they are the me immunosuppressant

Agent and we have the two drugs in it one is the cyclosporine and another is the nectar of slimmest this cyclosporine when it is taken it enters into the helper t cell where it binds the t cyclo filling and this whole complex is inhibiting the activity of calcineurin while when the dekker illumise is given that a trolleybus enters into the helper t cell when it

Binds with the f kbp that’s a sk binding fk506 binding protein so the mines with them and this whole complex is inhibiting the activity of calcium earrings so because of this so because of this the lis phosphorylation of this protein is inhibited so this phosphorylation of this n fat will occur in fact is a nuclear factor of activated t cells so this is this d

Phosphorylation is inhibited that leads to the decrease in the synthesis of mrna for the interleukin 2 so the transcription of interleukin 2 is inhibited that causes the inhibition in the translation of interleukin 2 which is a inhibition in the synthesis of interlinking 2 that causes a decrease in the t cell proliferation and that leads to the decrease in the

Number of cells and causes the decrease in the immunity so this is the way how they generate inhibitors works so cyclosporine and tacrolimus thank you guys

Transcribed from video
Calcineurin inhibitors (Immunosuppressants): Mechanism of action By Pharmacology Guru Coaching Institute