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Bortezomib Proteasome Inhibition
Detailed mechanism of boronic acid dipeptide bortezomib inhibiting the 26S proteasome in multiple myeloma.
By Encyclopeptide Editorial | 1 min read
bortezomib proteasome multiple-myeloma boronic-acid cancer
Mechanism of Action
Bortezomib reversibly inhibits the 20S proteasome beta5 subunit chymotrypsin-like activity through its boronic acid moiety forming a reversible covalent bond with the catalytic threonine.
Proteasome Subunit Inhibition
| Subunit | Activity | Bortezomib Effect |
|---|---|---|
| Beta5 | Chymotrypsin-like | Strong inhibition |
| Beta1 | Caspase-like | Moderate |
| Beta2 | Trypsin-like | Weak |
Clinical Applications
- Multiple myeloma (first-line and relapsed/refractory)
- Mantle cell lymphoma
- AL amyloidosis
Chemical Identity
| Property | Value |
|---|---|
| Name | Bortezomib Proteasome Inhibition |
| Category | Anticancer Peptides |
References
- Encyclopeptide Database. “Bortezomib Proteasome Inhibition” monograph. encyclopeptide.com.
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