What is protease drug inhibitors its type, how to they inhibit and drug available in market.

1. “ A REVIEW ON :PROTEASE
INHIBIOTORS DRUG IN AIDS”
PRESENTED By : Walunj R. Rasika

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

3. INTRODUCTION

4. 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.

5. 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.

6. CLASSIFICATION OF PROTEASE

7. Mechanism Action Of Protease

8. HIV Life Cycle

9. 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.

10. HIV Life Cycle

11. • 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

12. 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.

13. ENZYME INHIBITON

14. 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 .

15. Drugs used as protease inhibitors in HIV .
1. Squinavir.
2. Nelfinavir
3. Amprenavir
4. Lopinavir
5. Fosamprenavir.
6. Indinavir
Combination therapy
• Lopinavir + Ritonavir

16. Side Effects
PIs 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.

17. 1. Inflammatory Bowel Disease
2. Skin Burns and Stomach Ulcers
3. Sprains and Pain Relief
4. Digestion of many foods
5. chemical reaction
APLLICATIONS OF PROTEASE ENZYME

18. 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 .

19. 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

20. THANK YOU