Proteasome Inhibitors: Bortezomib and Carfilzomib Explained
Bortezomib and carfilzomib are peptide-derived proteasome inhibitors; here is how each blocks the proteasome, how reversible and irreversible binding differ, and what the labels warn about.
Bortezomib and carfilzomib are peptide-derived proteasome inhibitors; here is how each blocks the proteasome, how reversible and irreversible binding differ, and what the labels warn about.
Aspartame is a dipeptide of phenylalanine and aspartic acid; here is what it is, how it breaks down, and what the 2023 IARC and JECFA reviews concluded.
Exendin-4, from Gila monster venom, became exenatide, the first US-approved GLP-1 receptor agonist; here are the discovery, trial data and label warnings.
Linaclotide and plecanatide are oral GC-C agonist peptides that act locally in the intestine with negligible systemic absorption, per their labels.
Eptifibatide is a cyclic heptapeptide designed from a snake-venom disintegrin to block platelet GPIIb/IIIa; here is the origin, trial data and label safety information.
Aprotinin (BPTI) is a 58-residue polypeptide that inhibits serine proteases; here is its structure, the BART and Mangano studies, and why regulators suspended and later reconsidered it.
Glatiramer acetate is a mixture of synthetic polypeptides built from four amino acids; here is where it came from, how it is thought to work, and what the trials and label show.
Bivalirudin is a 20-amino-acid synthetic peptide modelled on leech hirudin that blocks thrombin directly; here is how it works and what two large trials showed.
Conotoxins are disulfide-rich peptides from cone-snail venom; here is how they hit ion channels, and how one of them became the approved pain drug ziconotide.
Epidermal growth factor (EGF) is a 53-amino-acid protein that signals through EGFR; here is the structure, the Nobel history and what trials of EGF in diabetic foot ulcers actually show.