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HIV/AIDS is a viral infection in which the human immunodeficiency virus that can kill immune cells in our body, and if left untreated, a person can be diagnosed with acquired immunodeficiency virus (AIDS). Hence, it is very important to search for proper treatment that can help eradicate/control the virus to ensure that the virus does not mutate quickly, allowing an individual's chances of survival to be increased.
HIV/AIDS is a viral infection in which the human immunodeficiency virus that can kill immune cells in our body, and if left untreated, a person can be diagnosed with acquired immunodeficiency virus (AIDS). Hence, it is very important to search for proper treatment that can help eradicate/control the virus to ensure that the virus does not mutate quickly, allowing an individual's chances of survival to be increased.
Developing Inhibitors
Developing Inhibitors
Inhibitors are molecules that can be biological or chemical; they help slow down or interfere with a chemical reaction. In this case, the two inhibitors, protease and integrase, that we will talk about are chemical inhibitors. We would also talk about on how they were made with the help of Chemistry!
Protease Inhibitors
Protease Inhibitors
Protease Inhibitors are a kind of antiretroviral therapy (ART) that act as a substrate to the HIV protease (an enzyme that cleaves long viral polyproteins that allow new viruses to mature). As inhibitors reduce and block the process of creating an "enzyme-substrate complex", the PIs can bind with the enzyme as they have a complementary active site which matches the shape of the natural peptide substrates, letting them fit tightly into the enzyme. As a result, the virus cleavages* fewer and defective viruses, halting their function to multiply further in destroy immune cells.
Organic chemistry and biochemistry played a key role in the production as it helped scientists study the chemical reactions it went through when chemically combining with other substances, and emulate its composition and structure.
-Cleavage, in scientific terms, means the splitting or breaking of substances in which helps the virus to penetrate into host cells.
Protease Inhibitors formulated in capsule form
A capsule of Triumeq (made up of two kinds of nucleoside reverse transcriptase inhibitors and one integrase inhibitor)
Integrase Inhibitors
Integrase Inhibitors
Likewise, integrase inhibitors are ARTs that prevent the integrase, a viral enzyme of the virus, from inserting its DNA into the person's DNA, which is essential for the replication of infected cells. The INIs binds to the active site of the integrase, which also chelates the magnesium ions (Mg²⁺) that are required for the integrase to function. This stops the virus from carrying out the strand transfer step, and thus prevents the viral DNA from integrating, and replication of the HIV stops.
Similar to the PI, organic chemistry and medicinal chemistry played a part in its development since it helped medical officers understand its chemical properties upon discovery, as well as know how to prepare and synthesize the drug into the body without causing harm.
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Zidovudine (AZT)
Zidovudine (AZT)
Zidovudine (AZT) is one of the first antiretroviral drugs for AIDS, being approved back in 1987. It's a type of NRTI that prevents the virus from converting its ribonucleic acid (RNA) into DNA, which is then integrated into the host's cells. HIV contains an enzyme called reverse transcriptase (RT) that produces DNA from its substrate (being the RNA). The AZT blocks this process as it mimics thymidine (one of the 4 DNA nucleosides), causing the reverse transcriptase to use it to build viral DNA. This incorporates the AZT instead of real thymidine. Hence, this process prevents the addition of more nucleotides, halting the DNA production.
Goodwill, Sam. 2023. “Article Name Here.” Publication Name, January 1, 2023. Article Link.
Pre-exposure Prophylaxis (PrEP)
Pre-exposure Prophylaxis (PrEP)
This medication is taken by those at high risk of AIDS due to long-term exposure to the virus, allowing greater prevention against it. Like AZT, Truvada, and Descovy, two common classifications of the medicine mimic natural nucleotides that block reverse transcription by terminating the DNA chain. Because of this, PrEP drugs prevent HIV from making copies of itself and prevent AIDS altogether before its symptoms show up - if taken daily, the body already has the drug circulating before exposure.
Like the other treatments, organic, as well as analytical and pharmaceutical chemistry, were involved in creating this drug. Pharmaceutical scientists analyzed the identity, purity, and stability of the drug to ensure it would not cause the constituents within it to react vigorously.
Sources
Sources
Action for AIDS Singapore (n.d.). HIV: All about it. HIV Transmission. https://afa.org.sg/know-more/education-series/hiv-transmission/#:~:text=HIV%E2%80%99s%20DNA%20must%20then%20be%20incorporated%20into%20the%20CD4%20cell%E2%80%99s%20DNA.%20This%20is%20known%20as%20integration.
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