Depsipeptide

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1 2 4 6 (IC50=36 47 510 1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

Dolastatin 15, a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the anti-tubulin agent Dolastatin 10. Dolastatin 15 can be used as an ADC cytotoxin and it induces cell cycle arrest and apoptosis in m

Tasidotin hydrochloride, a peptide analog of the antimitotic depsipeptide dolastatin 15, is an inhibitor of microtubule assembly and microtubule dynamics.

Tasidotin (also known as ILX-651) is an orally active synthetic derivative targeting microtubules, derived from the marine depsipeptide dolastatin-15.

Didemnin A is an antiviral and antitumor depsipeptide from Carribean tunicate.

Didemnin B (Didemnin-B) is a depsipeptide extracted from the marine tunicate Trididemnin cyanophorum that has antiviral and antitumor activity.

Salinamide A is an effective anti-inflammatory bicyclic depsipeptide.

A-83586C is a depsipeptide antibiotic from Streptomyces karnatakensis with potent against Gram-positive activity in vitro. A-83586C acts as a highly potent inhibitor of beta-catenin/TCF4 signaling within cancer cells, while simultaneously downregulating o

elomycin is a cyclic depsipeptide antibiotic with activity against Gram-positive bacteria.

Stevastelin B3 is a depsipeptide isolated from Penicillium.

Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg ml, respectively). It is cytotoxic to B16 F10 and Moser cells (IC50s = 0.0008 and 0.04 μg ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

Enopeptin A, originally isolated from a culture broth of Streptomyces sp. RK-1051, is a depsipeptide antibiotic containing two unusual amino acids (N-methylalanine and 4-methylproline) and features a pentaenone side chain. It is effective against Gram-positive bacteria, including methicillin-resistant S. aureus (MIC = 25 μg ml), and Gram-negative bacteria, including mutant forms of E. coli and P. aeruginosa (MICs = 200 μg ml); however, it is not inhibitory to fungi.

Homodestcardin is a cyclic depsipeptide fungal metabolite that has been found in T. roseum and has immunosuppressant activity. It inhibits concanavalin A-induced proliferation of isolated mouse T cells.

Aurantimycin A (Adipogen), a depsipeptide antibiotic, demonstrates significant efficacy against Gram-positive bacteria and acts as a substrate for the LieAB transporter [1] [2].

Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, exhibits potent antiproliferative activity, induces autophagosome accumulation via an mTOR-independent mechanism, and triggers apoptosis. Furthermore, it inhibits VEGFA VEGFR2 expression, effectively suppressing tumor growth in glioblastoma xenografts [1] [2].

Elisidepsin (PM02734), a cyclic depsipeptide, exhibits antineoplastic activity by inhibiting cancer cell proliferation and is under research for the treatment of various cancers, including non-small cell lung cancer (NSCLC) [1] [2] [3] [4].

PF-1163A, a depsipeptide antifungal compound isolated from Penicillium, blocks ergosterol synthesis with an IC50 of 12 ng/ml. This compound specifically inhibits the enzyme ERG25p, a C-4 methyl oxidase in the ergosterol biosynthetic pathway, leading to its antifungal activity. Notably, in Saccharomyces cerevisiae modified to express ERG biosynthesis genes, PF-1163A exhibits an inhibition concentration (MIC value) of 12.5 µg/ml against ERG25p, though strains overexpressing ERG25p show resistance. Additionally, PF-1163A effectively suppresses the growth of Candida albicans (MIC = 8 µg/ml), without affecting other Candida species, Aspergillus fumigatus, or HepG2 cells. Remarkably, it enhances the efficacy of fluconazole against azole-resistant C. albicans strains, showing a significant decrease in MICs (1 and 0.0078 µg/ml alone and in combination, respectively). PF-1163A distinguishes itself from PF-1163B by its more polar nature.

Valinomycin (NSC-122023) is a cyclic depsipeptide antibiotic and a potassium-specific ionophore.Valinomycin induces PINK1 activation and promotes Parkin phosphorylation at Ser65.

Sporidesmolide II is a cyclic depsipeptide that was initially isolated from P. chartarum.