“ A REVIEW ON :PROTEASE INHIBIOTORS DRUG IN AIDS”

PRESENTED By : Walunj R. Rasika

Content • Introduction• HIV • Protease• Classification of protease• HIV life cycle • Protease Inhibitors• Enzyme Inhibition• Drugs • Side effects• Applications• Conclusions• References

INTRODUCTION

HIV means……

HIV is the abbreviation for Human Immune-deficiency Virus which cause AIDS (Acquired immune deficiency syndrome) .

The enzymes reverse transcriptase, integrase and protease are involved in the formation of mature HIV virions for infection

HIV proteases cleave the viral polyproteins into individual functional HIV proteins and enzymes. The various structural components then assemble to produce a mature HIV virion which is capable of infecting another cell.

Protease….

Protease is a type of enzyme that functions mainly to help us digest different kinds of proteins. They break down the bonds by a process known as hydrolysis and convert proteins into smaller chains called peptides or even smaller units called amino acids.

CLASSIFICATION OF PROTEASE

Mechanism Action Of Protease

HIV Life Cycle

Steps in the HIV Life Cycle

1. Fusion of the HIV cell to the host cell surface.

2. HIV RNA, reverse transcriptase, integrase, and other viral proteins enter the host cell.

3. Viral DNA is formed by reverse transcription.

4. Viral DNA is transported across the nucleus and integrates into the host DNA.

5. New viral RNA is used as genomic RNA and to make viral proteins.

6. New viral RNA and proteins move to cell surface and a new, immature, HIV virus forms.

7. The virus matures by protease releasing individual HIV proteins.

HIV Life Cycle

• The aim of use of Protease inhibitors in HIV treatment is to keep the amount of HIV in the body at a low level.

• Protease inhibitors were designed to mimic the• transition state of protease.• There are several steps in the HIV life cycle that

may be interfered with ,thus the stopping the replication of the virus is necessary to prevent HIV infection to the other cells.

 

Study of Protease Inhibitors

PROTEASE INHIBIOTRS

Protease Inhibitor: “An agent that can keep a protease from splitting a protein into peptidase.

Protease inhibitors (PIs) are a class of antiviral drugs that are widely used to treat HIV/AIDS and hepatitis caused by hepatitis C virus. Protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles.

ENZYME INHIBITON

Protease Inhibitor Work As To Treat HIV Infection

A) It prevents the release of new viral particles.

B) It prevents the cleavage of host DNA preventing viral DNA from being inserted into host DNA.

C) It cleaves Reverse transcriptase preventing the generation of viral DNA.

D) It prevents the binding of gp120 to the CD4 protein.

E) It cleaves viral proteins interfering with their function.

ascent proteins for final assembly of new virion .

Drugs used as protease inhibitors in HIV .

1. Squinavir.2. Nelfinavir3. Amprenavir4. Lopinavir5. Fosamprenavir.6. Indinavir

Combination therapy• Lopinavir + Ritonavir

Side EffectsPIs may cause:• An increase in blood sugar.• Changes in the distribution of body fat.• Headaches.• Nausea, diarrhea, and vomiting.• Rash.• An increase in cholesterol and triglycerides.• Liver problems, especially if you have liver disease.

1. Inflammatory Bowel Disease2. Skin Burns and Stomach Ulcers3. Sprains and Pain Relief4. Digestion of many foods5. chemical reaction

APLLICATIONS OF PROTEASE ENZYME

CONCULSION

Protease inhibitors are pharmaceutical drugs that are prescribed for the treatment of Human Immunodeficiency Virus (HIV) infections.

This enzyme cures the AIDS from become serious. They play important role in regulate the protein function in body.

They work by specifically binding within the active site of HIV protease - and therefore prevent the active site from acting on the long precursor HIV protein produced during viral infection & help in cure diseases.

Drugs should always be used in optimum dose & preferably combined with other antiviral agents. Whether they should be used in initial combination therapy .

REFERENCES • en.wikipedia.org/wiki/HIV

• en.wikipedia.org/wiki/Protease.

• www.jiaowu.buct.edu.cn/Courseware/Harvard/.../ctw_proteases1.pdf

• www.thewellproject.org › ... › Treatment and Trials › Anti HIV Meds

• en.wikipedia.org/wiki/Protease inhibitor_(pharmacology)

• www.ehow.com › Diseases & Conditions protease inhibitors

• www.webmd.com/hiv-aids/protease-inhibitors-pis-for-hiv

THANK YOU