A trifunctional self-immolative spacer enables drug release with two non-sequential enzymatic cleavages

نویسندگان

چکیده

The enzymatic dephosphorylation of a self-immolative spacer accelerates cargo release and acts as an additional independent trigger in protease-sensitive prodrugs.

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Modifications of the Self-Immolative Spacer PABOH in Antibody Drug Conjugates

........................................................................................................................................... i Acknowledgements ......................................................................................................................... ii Table of

متن کامل

Self-immolative dendrimer biodegradability by multi-enzymatic triggering.

New self-immolative dendritic molecules have been designed and synthesized. The dendrons are built with a multi-enzymatic triggering mechanism, which initiates their biodegradation through a self-immolative chain fragmentation to release a reporter group from the focal point. The dendritic backbone is constructed from polycarbamate linkages, which are stable to hydrolysis and enhance the dendro...

متن کامل

Self-immolative polymers.

The investigation of synthetic polymers for biological applications is increasing as assembly techniques for generating welldefined macromolecules from artificial building blocks become more sophisticated. Synthesis techniques have now evolved such that a wide variety of functional groups can be tolerated by polymerization catalysts, and a fascinating and diverse range of macromolecular and pol...

متن کامل

Self-immolative aryl phthalate esters.

We report that aryl phthalate esters are robust self-immolative linkers. This linker is easy to conjugate and releases output phenols upon cleaving a fluoride-sensitive mask to yield a benign phthalic acid byproduct, making these linkers potentially useful as fluoride sensors and promising for use in biological and materials applications.

متن کامل

Sterol-Regulated Release of SREBP-2 from Cell Membranes Requires Two Sequential Cleavages, One Within a Transmembrane Segment

Sterol regulatory element binding proteins (SREBPs) are transcription factors attached to the endoplasmic reticulum. The NH2-segment, which activates transcription, is connected to membranes by a hairpin anchor formed by two transmembrane sequences and a short lumenal loop. Using H-Ras-SREBP-2 fusion proteins, we show that the NH2-segment is released from membranes by two sequential cleavages. ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Chemical Communications

سال: 2021

ISSN: ['1359-7345', '1364-548X']

DOI: https://doi.org/10.1039/d1cc02895b