Dolastatin-10 (dola-10) is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization. The dolastatins also enhance and stabilize the binding of colchicine to tubulin.

Synthetic analogues of the natural occurring dolastatin 10 are of great interest in cancer due to their potent in vitro activity and their uses as payloads in antibody drug conjugates (ADCs). Chemically related to Symplostatin The dolastatins (dolastatin 10 and dolastatin 15) are chemically related to analogue symplostatin 1which has been re-isolated from Guamanian and Hawaiian varieties of S. hydnoides. Preclinical animal data demonstrated that treatment of xenograft models of melanoma with CR011–vcMMAE caused significant improvements in survival, including complete and durable tumor regression, without any notable toxicity or weight loss.MEDI-547 is a fully human mAb designed to target the over-expression of the EphA2 protein linked to a potent drug monomethyl auristatin phenylalanine (MMAF) by MedImmune. Symplostatin 1, which is, like dolastatin 10, is a potent microtubule inhibitor. EphA2 is a member of the Eph family of receptor tyrosine kinases (RTK). In the phase I study,CR011–vcMMAE is composed of linking vcMMAE, a potent chemotherapeutic, to a fully human mAb CR011. allow you to toggle between having all search items start with or contain the text 30 The two most promising peptides of this family, dolastatin 10 and dolastatin 15 were selected for development and are currently undergoing phase-II clinical trials. Preclinical studies of dola-10 have demonstrated activity against a variety of murine and human tumors in cell cultures and mice models. References are publications that support the biological activity of the product. The hemiasterlins are a family of potent cytotoxic peptides. In the cellular assay, Dolastatin 10 shows activity against some human leukaemia, lymphoma and solid tumour cell lines (such as OVCAR-3 and NSCLC) with IC50 values ranging from 0.1nM to 10nM. All Rights Reserved.

in the mid‐1960s to explore potential effects of marine life forms as an anticancer drug source, resulted in the discovery of dolastatin peptides from the shell‐less mollusk Dolabella auricularia (sea hare): dolastatins 1–15, showing the ability to strongly kill cancer cell lines (Anderl et al., 2013; Luesch, Moore, Paul, Mooberry, & Corbett, 2001; Pettit et al., 1981, 1982, … to move through the suggestions. Along with regulatory affairs, we also cover government authorities and representatives from payers to policymakers. Isolation of dolastatin 10 from the marine cyanobacterium Symploca species VP642 and total stereochemistry and biological evaluation of its analogue symplostatin 1.

PURPOSE: Phase II trial to study the effectiveness of dolastatin 10 in treating patients with metastatic prostate cancer that has not responded to previous hormone therapy. By continuing you agree to the Copyright © 2020 Elsevier B.V. or its licensors or contributors. All Rights Reserved. Bai et al (1990) Binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. Dolastatin 10 also shows moderate effect on enhancing the binding of colchicines to tubulin.

Bioactive compounds may elicit various biological activities against test animals, eukaryotic or prokaryotic cells or viruses, or they may target certain enzymes.Marine environments and especially benthic cyanobacteria seem to be among the best sources of new bioactive compounds. One example is nostocarboline, a new cholinesterase inhibitor identified in the freshwater isolate The number of new compounds identified from cyanobacteria is increasing continuously. Dolastatin 10(DLS 10;NSC 376128) is a potent antimitotic peptide from a marine animal, strongly inhibits microtubule assembly; Dolastatin and Dolastatin's analogs are the cytotoxic components in Antibody-drug conjugates design (eg. a list of up to 10 suggestions will popup under the textbox. Its total stereochemistry was completed by determining the N,N-dimethylisoleucine unit to be l.Symplostatin 1,which is, like dolastatin 10, is a potent microtubule … Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives ES2604766T3 (en) * 2012-09-20: 2017-03-09: Celltrion, Inc. Dolastatin-10 derivative, its production process and anticancer drug composition containing the same MX2016008444A (en) 2013-12-27: 2017-01-11 the escape key closes the listbox and puts you back at the textbox.

CR011–vcMMAE targets melanoma-associated glycoprotein (GPNMB), a protein overexpressed on the surface of cancer cells, including melanoma, breast cancer, and gliomas. 2001 Jul;64(7):907-10.

The chemically related analogue symplostatin 1 (2) has been reisolated from Guamanian and Hawaiian varieties of S. hydnoides and its total stereochemistry completed by … Dolastatin-10 was administered at a dose of 400 μg/m2 i.v.

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