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Questions and Answers
What technique was used to identify the residues that form the protein-membrane interface?
What technique was used to identify the residues that form the protein-membrane interface?
Where does the PLA2 homologue myotoxin II (MT-II) bind?
Where does the PLA2 homologue myotoxin II (MT-II) bind?
What part of β-Bungarotoxin is responsible for recognizing and binding to the presynaptic voltage-gated K+ channel?
What part of β-Bungarotoxin is responsible for recognizing and binding to the presynaptic voltage-gated K+ channel?
What happens to the active site of the PLA2 domain in β-Bungarotoxin when it binds to the neuronal membrane?
What happens to the active site of the PLA2 domain in β-Bungarotoxin when it binds to the neuronal membrane?
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What is the effect of the C-terminal region of myotoxin II on the membrane?
What is the effect of the C-terminal region of myotoxin II on the membrane?
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What is the name of the thrombin-like serine protease purified from the venom of the Brazilian lancehead pit viper (Bothrops moojeni)?
What is the name of the thrombin-like serine protease purified from the venom of the Brazilian lancehead pit viper (Bothrops moojeni)?
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Which country approves the use of Haemocoagulase for treating internal and external hemorrhages?
Which country approves the use of Haemocoagulase for treating internal and external hemorrhages?
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In which country is Batroxobin (Defibrase) marketed for the treatment of acute cerebral infarction?
In which country is Batroxobin (Defibrase) marketed for the treatment of acute cerebral infarction?
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What is the primary function of α-Cobrotoxin?
What is the primary function of α-Cobrotoxin?
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What is the potential side effect associated with high bioactivity of α-Cobrotoxin?
What is the potential side effect associated with high bioactivity of α-Cobrotoxin?
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Which of these venom toxins is approved for use in the treatment of ischemia caused by vascular occlusive diseases?
Which of these venom toxins is approved for use in the treatment of ischemia caused by vascular occlusive diseases?
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Which venom toxin is specifically mentioned as being purified from the venom of the Chinese cobra (Naja atra)?
Which venom toxin is specifically mentioned as being purified from the venom of the Chinese cobra (Naja atra)?
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Which of these venom toxins is NOT specifically mentioned as being approved for use in any country?
Which of these venom toxins is NOT specifically mentioned as being approved for use in any country?
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Which of these is a characteristic found in both captopril and enalapril?
Which of these is a characteristic found in both captopril and enalapril?
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The venom of which snake inspired the development of tirofiban?
The venom of which snake inspired the development of tirofiban?
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What is the role of the angiotensin-converting enzyme (ACE) in the body?
What is the role of the angiotensin-converting enzyme (ACE) in the body?
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What is the significance of the Zn2+ cofactor in the ACE protein?
What is the significance of the Zn2+ cofactor in the ACE protein?
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What is the primary target of the BPPs?
What is the primary target of the BPPs?
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What is the connection between echistatin and tirofiban?
What is the connection between echistatin and tirofiban?
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What is a potential advantage of using drugs inspired by snake venom components?
What is a potential advantage of using drugs inspired by snake venom components?
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Based on the given information, which of these statements is TRUE?
Based on the given information, which of these statements is TRUE?
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What is Anfibatide?
What is Anfibatide?
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Which of the following is NOT a characteristic of Anfibatide?
Which of the following is NOT a characteristic of Anfibatide?
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How does Anfibatide function as an anticoagulant?
How does Anfibatide function as an anticoagulant?
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What is the significance of the seven disulfide bonds in Anfibatide?
What is the significance of the seven disulfide bonds in Anfibatide?
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What is the primary target of Anfibatide in the coagulation cascade?
What is the primary target of Anfibatide in the coagulation cascade?
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What is the primary function of RVV-X in relation to blood coagulation?
What is the primary function of RVV-X in relation to blood coagulation?
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Which domain of RVV-X is responsible for its catalytic activity?
Which domain of RVV-X is responsible for its catalytic activity?
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What is the role of the Zn2+ cofactor in RVV-X's activity?
What is the role of the Zn2+ cofactor in RVV-X's activity?
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Which of the following accurately describes daborhagin's mechanism of action?
Which of the following accurately describes daborhagin's mechanism of action?
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What is the primary difference between SVSPs that are classified as thrombin-like enzymes and other SVSPs?
What is the primary difference between SVSPs that are classified as thrombin-like enzymes and other SVSPs?
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What is the approximate molecular weight range of SVSPs?
What is the approximate molecular weight range of SVSPs?
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How does daborhagin's interaction with collagen IV contribute to its hemorrhagic effects?
How does daborhagin's interaction with collagen IV contribute to its hemorrhagic effects?
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Which of the following statements accurately describes the role of SVSPs in the regulation of homeostasis?
Which of the following statements accurately describes the role of SVSPs in the regulation of homeostasis?
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Crotamine exhibits potent antinociceptive activity, being how many times more potent than morphine?
Crotamine exhibits potent antinociceptive activity, being how many times more potent than morphine?
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What is the primary mode of action of crotamine that makes it a promising antitumour agent?
What is the primary mode of action of crotamine that makes it a promising antitumour agent?
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Which of these bioactivities is NOT mentioned as being exhibited by crotamine?
Which of these bioactivities is NOT mentioned as being exhibited by crotamine?
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What is a critical step needed to enhance the therapeutic potential of crotamine?
What is a critical step needed to enhance the therapeutic potential of crotamine?
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Why are mambalgins considered promising new analgesics?
Why are mambalgins considered promising new analgesics?
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Which of the following is NOT a significant advantage of mambalgins as potential analgesics?
Which of the following is NOT a significant advantage of mambalgins as potential analgesics?
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What is the primary mechanism by which mambalgins exert their antinociceptive effects?
What is the primary mechanism by which mambalgins exert their antinociceptive effects?
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What aspect of crotamine makes it particularly valuable for potential therapeutic applications?
What aspect of crotamine makes it particularly valuable for potential therapeutic applications?
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Flashcards
RVV-X
RVV-X
A protein that activates blood coagulation factor X through hydrolysis.
Factor X
Factor X
A key enzyme in the blood coagulation pathway activated by RVV-X.
SVMP
SVMP
Snake venom metalloproteinases involved in hemorrhage.
Collagen IV
Collagen IV
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Daborhagin
Daborhagin
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Zn2+ cofactor
Zn2+ cofactor
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Cysteine-rich domain (CR)
Cysteine-rich domain (CR)
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Thrombin-like enzymes
Thrombin-like enzymes
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Phospholipid colors
Phospholipid colors
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PLA2 homologue myotoxin II
PLA2 homologue myotoxin II
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β-Bungarotoxin function
β-Bungarotoxin function
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C-terminal KKYRYYLKPLCKK sequence
C-terminal KKYRYYLKPLCKK sequence
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Mutagenesis, fluorescence, X-ray crystallography
Mutagenesis, fluorescence, X-ray crystallography
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Bradykinin Potentiating Peptides (BPPs)
Bradykinin Potentiating Peptides (BPPs)
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Captopril
Captopril
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Enalapril
Enalapril
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Angiotensin-Converting Enzyme (ACE)
Angiotensin-Converting Enzyme (ACE)
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WAP Motif
WAP Motif
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Tirofiban
Tirofiban
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Disintegrin
Disintegrin
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PDB ID 6QS1
PDB ID 6QS1
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Anfibatide
Anfibatide
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Human platelet glycoprotein Ib α-chain (GPIbα)
Human platelet glycoprotein Ib α-chain (GPIbα)
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Von Willebrand factor (VWF)
Von Willebrand factor (VWF)
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Thrombin
Thrombin
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Disulfide bonds in proteins
Disulfide bonds in proteins
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Haemocoagulase
Haemocoagulase
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Batroxobin
Batroxobin
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Acute cerebral infarction
Acute cerebral infarction
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α-Cobrotoxin
α-Cobrotoxin
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Nicotinic acetylcholine receptors
Nicotinic acetylcholine receptors
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Analgesic
Analgesic
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Respiratory arrest
Respiratory arrest
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Crotamine
Crotamine
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Natriuresis
Natriuresis
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Antitumour agent
Antitumour agent
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Mambalgins
Mambalgins
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Antinociceptive activity
Antinociceptive activity
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Analgesic effect
Analgesic effect
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Chemical synthesis
Chemical synthesis
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Oral administration
Oral administration
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Study Notes
The Chemistry of Snake Venom and its Medicinal Potential
- Snake venom is a complex mixture of toxins, mainly peptides and proteins (over 90%)
- Venom composition varies greatly between species and even within the same species based on factors like environment, age, sex and prey
- Venom has a wide range of bioactivities, including neurotoxicity, hemotoxicity, and cytotoxicity; determined by the species
- There are an estimated 2.7 million snakebites annually, leading to >100,000 deaths and >400,000 victims experiencing severe and permanent sequelae
- Venom composition diversity is a benefit, providing a diverse pool of compounds for medicinal chemists to explore
- Venom is an incredible source of bioactive compounds with many potential therapeutic applications.
Venom Composition
- Data from >200 snake species indicate >30 families of venom toxins.
- Some venom families include phospholipases A2 (PLA2s), snake venom metalloproteinases (SVMPs), snake venom serine proteases (SVSPs) and three-finger toxins (3FTxs)
- Venom toxin variation exists even between siblings
- There are almost 3,000 known isoforms of snake toxins
- Variability in venom composition exists across genera and within a single species
Toxin Action
- Toxins often act synergistically, with toxin combinations determining the severity of snakebite.
- Neurotoxic venom affects the nervous system, causing paralysis, muscle fasciculations and cardiac arrest. This is more common with Elapids.
- Myotoxic and hemotoxic venom affects the muscles and/or circulatory system to cause hemorrhage and necrosis (tissue death), typically more common with Viperidae.
- Toxins can act on various targets, including ion channels, receptors and other proteins.
Medicinal Potential of Snake Venom
- Venom's diverse chemical and biological activities make it a rich source potentially effective in many therapies
- Captopril, a drug for hypertension, was developed by replicating a snake venom component (bradykinin potentiating factor-BPP).
- Ziconotide, an analgesic for chronic pain for intrathecal administration, is derived from a cone snail toxin
- Tirofiban and eptifibatide, antiplatelet drugs, obtained through modifications of snake venom disintegrins that target specific platelet receptors.
- Many venom-based drugs are being researched, some in clinical trials.
Challenges in Drug Development
- Variability in venom composition is a challenge. There is limited supply with significant challenges for production scale-up
- Effective delivery methods are necessary due to nature of toxins (peptides/proteins). Oral delivery is problematic.
- The need for extensive research to identify specific targets will accelerate the identification of these targets and lead to more effective toxin-mimicking agents. Computational chemistry can play a key role.
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Description
Test your knowledge on the mechanisms of venom toxins, including PLA2 homologue myotoxin II and β-Bungarotoxin. This quiz covers the binding sites, effects on membranes, and clinical uses of various toxins derived from snake venoms. Explore the fascinating interactions of these proteins and their implications in medicine.