Pyridazinediones deliver potent, stable, targeted and efficacious antibody–drug conjugates (ADCs) with a controlled loading of 4 drugs per antibody

Autor: Antoine Maruani, Stephen Caddick, Eifion Robinson, Mark E. B. Smith, João P. Nunes, Vessela Vassileva, James R. Baker, R. Barbara Pedley, João C. F. Nogueira, Vijay Chudasama

Publikováno v: RSC Advances. 7:9073-9077

Herein we report the use of pyridazinediones to functionalise the native solvent accessible interstrand disulfide bonds in trastuzumab with monomethyl auristatin E (MMAE). This method of conjugation delivers serum stable antibody–drug conjugates (A

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f284be16884546ad478e386f9a1e0e5
https://doi.org/10.1039/c7ra00788d

A novel synthetic chemistry approach to linkage-specific ubiquitin conjugation

Autor: Stephen Caddick, Rachel E. Morgan, Mark E. B. Smith, Paul Moody, Vijay Chudasama

Publikováno v: Organic & Biomolecular Chemistry. 13:4165-4168

Ubiquitination is of great importance as the post-translational modification of proteins with ubiquitin, or ubiquitin chains, facilitates a number of vital cellular processes. Herein we present a facile method of preparing various ubiquitin conjugate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f715a1e82de5f3721bd8169c2de3fa19
https://doi.org/10.1039/c5ob00130g

Optimisation of the dibromomaleimide (DBM) platform for native antibody conjugation by accelerated post-conjugation hydrolysis

Autor: Maurício, Morais, João P M, Nunes, Kersti, Karu, Nafsika, Forte, Irene, Benni, Mark E B, Smith, Stephen, Caddick, Vijay, Chudasama, James R, Baker

Publikováno v: Organicbiomolecular chemistry. 15(14)

Disulfide bridging offers a convenient approach to generate site-selective antibody conjugates from native antibodies. To optimise the reagents available to achieve this strategy, we describe here the use of dibromomaleimides designed to undergo acce

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::39775d91677efaf4b141088794ca3489
https://pubmed.ncbi.nlm.nih.gov/33885556

Bromo- and thiomaleimides as a new class of thiol-mediated fluorescence ‘turn-on’ reagents

Autor: Andrew Tinker, James R. Baker, Judith Youziel, Qadeer Aziz, Mark E. B. Smith, Ahmed R. Akhbar, Stephen Caddick

Publikováno v: Org. Biomol. Chem.. 12:557-560

Bromo- and thiomaleimides are shown to serve as highly effective quenchers of a covalently attached fluorophore. Reactions with thiols that lead to removal of the maleimide conjugation, or detachment of the fluorophore from the maleimide, result in '

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95bfc6252cbca7d158c428eccbd9f072
https://doi.org/10.1039/c3ob42141d

Evaluating the use of Apo-neocarzinostatin as a cell penetrating protein

Autor: Rachel E. Morgan, Justin E. Molloy, John Offer, Mark E. B. Smith, Stephen R. Martin, Paul Moody, Stephen Caddick, Fabienne Burlina

Publikováno v: Protein Engineering, Design and Selection
Protein Engineering, Design and Selection, 2013, 26 (4), pp.277-281. ⟨10.1093/protein/gzs104⟩
Protein Engineering, Design and Selection, Oxford University Press (OUP), 2013, 26 (4), pp.277-281. ⟨10.1093/protein/gzs104⟩

International audience; Protein-ligand complex neocarzinostatin (NCS) is a small, thermostable protein-ligand complex that is able to deliver its ligand cargo into live mammalian cells where it induces DNA damage. Apo-NCS is able to functionally disp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::237494b9d37197b50553417abda10dab
http://europepmc.org/articles/PMC3601848