NNRTIs Mechanism of Action and Pharmacokinetics

MajesticPlatypus avatar
MajesticPlatypus
·
·
Download

Start Quiz

Study Flashcards

26 Questions

What is the purpose of using protease inhibitors in antiretroviral therapy?

To target multiple stages of the HIV life cycle

What is the mechanism of action of Nucleos(t)ide Reverse Transcriptase Inhibitors (NRTIs)?

By competitively inhibiting the incorporation of native nucleotides

How do NNRTIs act as inhibitors in HIV treatment?

By inducing a conformational change in the enzyme structure

Why are Nucleos(t)ide Reverse Transcriptase Inhibitors important in HIV pharmacokinetics?

To enter cells and be phosphorylated for substrate generation

How do Nucleos(t)ide Reverse Transcriptase Inhibitors (NRTIs) exert their pharmacodynamic effect?

Competitive inhibition of reverse transcriptase enzymes

Which enzyme do Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) act on?

Reverse transcriptase

Why do NRTIs require intra-cytoplasmic activation via phosphorylation by cellular enzymes?

To be converted into their active triphosphorylated form

What is the mechanism of action of NNRTIs?

Noncompetitive inhibition

What is the selective toxicity of NRTIs based on?

Affinity for DNA-polymerase gamma (mitochondrial enzyme)

What adverse effect is commonly associated with Efavirenz use?

Abnormal dreams

Which Nucleos(t)ide Reverse Transcriptase Inhibitor (NRTI) does not require triphosphorylation for activation?

Tenofovir

Which HIV strain are Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) active against?

HIV-1 only

What is a common characteristic of Protease Inhibitors (PIs)?

Associated with lipodystrophy syndrome

What is significant about the resistance development with Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs)?

Rapid resistance (days or weeks) if given as monotherapy

Where is the HBZ gene encoded in relation to the DNA strand?

Complementary negative sense strand

What is the characteristic of HBZ expression during infection?

Continuously expressed throughout the infection

In ATL cells, what effects does Tax-independent cell proliferation lead to?

Recapitulation of the effects of Tax protein

Which cellular transcription factors are constitutively expressed in aggressive ATL cells?

NF-κB, NF-AT, AP-1, STAT-5

What is a genetic predisposition to Adult T-cell Leukemia (ATL) according to the text?

Certain human leukocyte antigen (HLA) alleles

Which feature is characteristic of Adult T-cell Leukemia (ATL) at an advanced stage?

Presence of systemic lymphadenopathy

How is HTLV-1 infection diagnosed according to the text?

Demonstration of antibodies to HTLV-1 in the patient's serum

What is a cellular effect caused by the Tax protein of HTLV-1?

Induction of cell cycle progression

How does the HTLV-1 protein p12I contribute to down-modulation of MHC-I-restricted antigen presentation?

By sequestering MHC-I alpha chain in the endoplasmic reticulum (ER)

What is one of the effects of Tax-dependent cell proliferation of escape mutants?

Low-grade Acute T-cell Leukemia (ATL)

How does HBZ contribute to leukemogenesis in HTLV-1 infection?

Suppressing Tax-mediated proviral transcription

What characterizes the stage of low-grade ATL in HTLV-1 infection?

Presence of skin lesions, lymphadenopathy, and hepatosplenomegaly

Learn about Non-nucleoside Reverse Transcriptase Inhibitors (NNRTI) mechanism of action, which induces a conformational change in the enzyme structure. Understand their pharmacokinetics and pharmacodynamics, including their activity against HIV-1 and HIV-2. Explore how NNRTIs act as noncompetitive inhibitors.

Make Your Own Quizzes and Flashcards

Convert your notes into interactive study material.

Get started for free
Use Quizgecko on...
Browser
Browser