Microtubule inhibitors
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Microtubule inhibitors
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Laboratory Value | Result |
Color | Clear |
Specific gravity | 1.013 |
Glucose | Negative |
Blood | Positive |
Leukocyte esterase | Negative |
Nitrites | Negative |
Leukocytes | 1-2/hpf |
Erythrocytes | 60/hpf |
Dysmorphic RBCs | Absent |
Casts | None |
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2024
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2021
Breast cancer
paclitaxel for p. 445
Ovarian cancer
paclitaxel for p. 445
Paclitaxel p. 445
in cell cycle p. 443
microtubules and p. 46
targets of p. 443
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Content Reviewers
Microtubule inhibitors, as their name implies, disrupt the microtubules and inhibit mitosis, which is a specific phase of the cell cycle.
Anticancer agents in this class include the vinca alkaloids and the taxanes.
But first things first.
The cytoskeleton is a network of proteins within the cell that gives each cell its shape, and it anchors organelles in place.
But it’s also a dynamic network, which can change shape when the cell wants to move, contract, divide, or pull in or push out molecules.
It’s made up of three proteins: actin filaments, intermediate filaments, and microtubules.
Microtubules are made of alternating round proteins called α- and β-tubulins, which form long strands called protofilaments.
Thirteen of these protofilaments come together to form a single microtubule.
Microtubules play a super important role in cell division.
During cell division there are two centrosomes inside the cell, and each centrosome is made out of two centrioles.
Each centriole is in turn made up of nine sets of microtubule triplets.
Now cell division, or mitosis, can be divided into four subphases: prophase, metaphase, anaphase, and telophase.
During prophase, the membrane around the nucleus disintegrates, and the chromosomes condense.
During metaphase, chromosomes move towards the middle of the cell, on a line called the metaphase plate.
Each chromosome is made up of a pair of sister chromatids which are joined together in the centromere where there’s a specific protein complex called the kinetochore.
When the chromosomes are in place, each centrosome sends out thread-like projections called spindle fibers, that attach to the centromere of each chromosome.
Spindle fibers consist of microtubules that originate from the centrioles and polymerize in the direction of the kinetochores.
Next, during anaphase, the centrosomes start pulling on the spindle fibers to pull the sister chromatids apart, forming the mitotic spindle.
It looks a bit like a fishing line being cast out to its target, and then the line gets reeled in, pulling the kinetochore and it’s attached sister chromatid away from its partner chromosome.
Finally, there’s the telophase during which a nuclear membrane forms around each new set of 46 single-chromatid chromosomes.
After that, during cytokinesis, the cell membrane pinches in until the two daughter cells separate.
Alright, now cancer cells replicate rapidly so they are constantly undergoing mitosis and the microtubules are always at work.
This means that microtubule inhibitors will affect these cells more than our healthy cells, most of which only divide occasionally.
Summary
Microtubules are a component of the cytoskeleton which are involved in cellular transport and cell division. Microtubule inhibitors work by disrupting the function of microtubules, which stops or slows down cell division and movement. This can be useful in cancer treatment, as it can stop or slow down the spread of cancer cells. Some common microtubule inhibitors include paclitaxel (Taxol) and vincristine.
Sources
- "Katzung & Trevor's Pharmacology Examination and Board Review,12th Edition" McGraw-Hill Education / Medical (2018)
- "Rang and Dale's Pharmacology" Elsevier (2019)
- "Goodman and Gilman's The Pharmacological Basis of Therapeutics, 13th Edition" McGraw-Hill Education / Medical (2017)
- "A microtubule bestiary: structural diversity in tubulin polymers" Molecular Biology of the Cell (2017)
- "Cell division: The renaissance of the centriole" Current Biology (1999)
- "Cancer Management" UBM Medica (2008)
- "Mechanism of taxane neurotoxicity" Breast Cancer (2004)
- "Docetaxel" Drugs (2005)