A novel affibody-auristatin E conjugate with a potent and selective activity against HER2+ cell lines

AM Sochaj-Gregorczyk… - Journal of …, 2016 - journals.lww.com
… Therefore, we used the Z HER2:2891 affibody to deliver cytotoxic MMAE to cancer cells …
MMAE, which is a synthetic derivative of dolastatin 10, disrupts the formation of mitotic spindle, …

Precision chemoradiotherapy for HER2 tumors using antibody conjugates of an auristatin derivative with reduced cell permeability

DV Hingorani, MK Doan, MF Camargo, J Aguilera… - Molecular cancer …, 2020 - AACR
… To achieve tumor-selective … anti-HER2 antibody–drug conjugates of two auristatin
derivatives with ionizing radiation. Monomethyl auristatin E (MMAE) and monomethyl auristatin F (…

[HTML][HTML] A conjugate based on anti-HER2 diaffibody and auristatin E targets HER2-positive cancer cells

AM Serwotka-Suszczak… - International journal of …, 2017 - mdpi.com
… the maleimide group linked with MMAE to cysteines, which … delivered auristatin E specifically
to HER2-positive tumor cells… of various types of cancer overexpressing HER2 receptors. …

Site-Specific Conjugation of Auristatins onto Engineered scFv Using Second Generation Maleimide to Target HER2-positive Breast Cancer in Vitro

N Aubrey, E Allard-Vannier, C Martin… - Bioconjugate …, 2018 - ACS Publications
… , especially against solid tumors which remain difficult to treat… a single auristatin derivative
onto an engineered anti-HER2auristatin E) or noncleavable (for monomethyl auristatin F). Our …

Antibody–drug conjugate payloads; study of auristatin derivatives

M Akaiwa, J Dugal-Tessier… - Chemical and …, 2020 - jstage.jst.go.jp
… assays with two ADC-relevant human cancer cell lines (HER2-expressing human mammary
ductal carcinoma HCC1954 cell line and HER2-negative human prostate carcinoma cell line…

[HTML][HTML] Comparison of HER2-targeted affibody conjugates loaded with auristatin-and maytansine-derived drugs

W Yin, T Xu, H Ding, J Zhang, V Bodenko… - Journal of Controlled …, 2023 - Elsevier
… to tumors provided a superior anti-tumor effect of Z HER2 -… and conjugated to the maytansine
derivative DM1, was used … was replaced with the auristatin derivatives, MMAE or MMAF. …

The efficient elimination of solid tumor cells by EGFR-specific and HER2-specific scFv-SNAP fusion proteins conjugated to benzylguanine-modified auristatin F

M Woitok, D Klose, J Niesen, W Richter, M Abbas… - Cancer letters, 2016 - Elsevier
… Approximately one third of ADCs undergoing clinical trials are conjugated to auristatin
derivatives, as well as the FDA-approved brentuximab vedotin [15], [33]. Auristatins induce …

Investigation of hydrophilic auristatin derivatives for use in antibody drug conjugates

BA Mendelsohn, SD Barnscher, JT Snyder… - Bioconjugate …, 2017 - ACS Publications
derivative, monomethyl auristatin PYE, showed the greatest potency when tested in vivo.
While only a modest tumor … The compounds were tested for cytotoxicity against the HER2

[HTML][HTML] Purification and in vitro evaluation of an anti-HER2 affibody-monomethyl auristatin E conjugate in HER2-positive cancer cells

I Damiani, S Castiglioni, A Sochaj-Gregorczyk… - Biology, 2021 - mdpi.com
… ) [13], whereas trastuzumab emtansine combines trastuzumab with another antimitotic
cytotoxic agent, derivative of maytansine (DM1), via a chemical linker [14]. Interestingly, a recent …

Novel development strategies and challenges for anti-Her2 antibody-drug conjugates

X Zhang, AC Huang, F Chen, H Chen, L Li… - Antibody …, 2022 - academic.oup.com
… Owing to the high density of Her2 antigens on the tumor cells and high affinity and high …
auristatin derivative with a similar structure to MMAE. The difference between MMAD and MMAE