Semantic Scholar Open Access 2019 596 sitasi

PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future.

M. Pettersson C. Crews

Lihat Sumber DOI

Abstrak

The majority of currently used therapeutics are small molecule-based and utilize occupancy-driven pharmacology as the mode of action (MOA), in which the protein function is modulated via temporary inhibition. New modalities that operate using alternative MOAs are essential for tapping into the "undruggable" proteome. The PROteolysis Targeting Chimera (PROTAC) technology provides an attractive new approach that utilizes an event-driven MOA. Small molecule-based heterobifunctional PROTACs modulate protein target levels by hijacking the ubiquitin-proteasome system to induce degradation of the target. Here, we address important milestones in the development of the PROTAC technology, as well as emphasize key findings from this previous year and highlight future directions of this promising drug discovery modality.

Topik & Kata Kunci

Medicine Biology

Penulis (2)

M. Pettersson

C. Crews

Format Sitasi

APA MLA BibTeX

Pettersson, M., Crews, C. (2019). PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future.. https://doi.org/10.1016/J.DDTEC.2019.01.002

Akses Cepat

Lihat di Sumber doi.org/10.1016/J.DDTEC.2019.01.002

Informasi Jurnal

Tahun Terbit: 2019
Bahasa: en
Total Sitasi: 596×
Sumber Database: Semantic Scholar
DOI: 10.1016/J.DDTEC.2019.01.002
Akses: Open Access ✓