Inhibitors of Translation

Inhibitors of Translation - OMPATH

# **Inhibitors of Translation** Translation inhibitors are mostly **antibiotics** that target bacterial ribosomes. Since **bacteria rely heavily on protein synthesis**, these drugs disrupt translation and prevent bacterial growth. ## **Differences Between Prokaryotic and Eukaryotic Ribosomes** - **Prokaryotic ribosomes**: **70S**, composed of **30S (small subunit) and 50S (large subunit)**. - **Eukaryotic ribosomes**: **80S**, composed of **40S (small subunit) and 60S (large subunit)**. Most antibiotics **target the differences** between bacterial (prokaryotic) and human (eukaryotic) ribosomes to avoid harming human cells. --- # **Differences Between Translation in Prokaryotes and Eukaryotes** # **Categories of Translation Inhibitors (Antibiotics)** ### **1. Aminoglycosides** - **Mechanism**:Bind to **both 30S and 50S ribosomal subunits**. - **Block codon recognition**, preventing translation. - Cause **misreading of mRNA**, leading to defective proteins. - **Examples**:**Streptomycin**, **Gentamicin**, **Kanamycin**. - **Toxicity & Side Effects**:**Ototoxicity (hearing loss)** – damages the ear. - **Nephrotoxicity (kidney damage)** – inhibits prostaglandins (vasodilators). - **Vestibular damage** – causes dizziness. - **Resistance Mechanisms**:Ribosomal **mutations** preventing drug binding. - Enzymatic modification of the drug (**phosphorylation**). - **Efflux pumps** remove the drug from bacteria. ### **2. Tetracyclines** - **Mechanism**:Bind to **30S ribosomal subunit**. - **Block tRNA binding** to mRNA, preventing elongation. - **Examples**:**Doxycycline**, **Oxytetracycline**, **Chlorotetracycline**. - **Toxicity & Side Effects**:**Photosensitivity** – avoid sun exposure. - **Teeth discoloration** – **should not be given to children**. - **Gastrointestinal distress**. - **Resistance Mechanisms**:**Efflux pumps** remove the drug from bacterial cells. - **Mutations** in ribosomal binding sites. - **Plasmid-coded resistance genes**. ### **3. Macrolides** - **Mechanism**:Bind to **50S ribosomal subunit**. - **Prevent mRNA movement** between the **A-site and P-site**, stopping elongation. - **Examples**:**Erythromycin**, **Clarithromycin**, **Azithromycin**. - **Toxicity & Side Effects**:**Gastrointestinal (GIT) disturbances**. - **Metallic taste**. - **Resistance Mechanisms**:**Methylation of 50S ribosomal subunit**, preventing drug binding. - **Efflux pumps** remove the drug from the cell (plasmid-mediated). ### **4. Chloramphenicol** - **Mechanism**:Binds to **50S ribosomal subunit**. - **Inhibits peptide bond formation**, stopping protein synthesis. - **Toxicity & Side Effects**:**Bone marrow suppression** – can lead to **aplastic anemia**. - **Mitochondrial damage** – causes toxicity in human cells. - **Resistance Mechanisms**:Bacteria produce **enzymes that modify chloramphenicol**, preventing its action. # **Short-Answer Questions and Answers** ### **1. Discuss in detail the mechanisms, actions, toxicity, and effects of translation-inhibiting drugs.** **Answer:** - **Aminoglycosides** bind **both ribosomal subunits**, interfere with **codon recognition**, and cause **misreading of mRNA**. They are **bactericidal** but cause **renal and ear toxicity**. - **Tetracyclines** bind to **30S**, block **tRNA attachment**, and prevent **elongation**. They cause **teeth discoloration** and **photosensitivity**. - **Macrolides** bind **50S**, block **mRNA movement**, and prevent **elongation**. They cause **GIT issues** and **metallic taste**. - **Chloramphenicol** binds **50S**, blocks **peptide bond formation**, but has **high toxicity (anemia, mitochondrial damage)**. ### **2. Differentiate between translation in prokaryotes and eukaryotes. (10 marks)** **Answer:** ### **3. Differentiate between translation and transcription. (10 marks)** **Answer:** **10 key points** differentiating **transcription** and **translation**: ### **Transcription vs. Translation (10 Points)** ## **Recombinant DNA Technology & Cloning** Recombinant DNA technology, also known as **genetic engineering**, involves modifying genetic material to create new combinations of DNA. This technology was developed in the **1970s** after the discovery of **restriction enzymes** in bacteria. ### **Key Components of Recombinant DNA Technology** - **Restriction Enzymes**Found in bacteria. - Function: Cut DNA at specific **restriction sites** (also called **palindromic sequences**). - Example: **EcoRI (from Escherichia coli)** recognizes **5' AATTC 3'** and cuts at this site. - Produces either:**Sticky ends** (cohesive, easier for DNA recombination). - **Blunt ends** (straight cuts). - **Plasmids (Vectors)****Small, circular, extra-chromosomal DNA** in bacteria. - Self-replicating, used to **carry foreign DNA** into host cells. - Contains:**Origin of replication (Ori)** – ensures self-replication. - **Antibiotic resistance gene** – helps in selecting transformed cells. - **Multiple cloning site (M