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Inhibitors of the Ubiquitin Ligase Nedd4-1 Discovered by Covalent Fragment Screening

Description:

The FDA approvals of afatinib and ibrutinib in 2013 led to a heightened interest in cysteine-reactive covalent inhibitors. However, there are few methods to discover new cysteine-reactive inhibitors for enzymes for which reversible binding scaffolds are not known. To this end, we rationally designed a chemical system to attach a...

Keyword:

Electrophile, Covalent, Fragment, Ubiquitin, and Nedd4-1

Subject:

Chemistry

Creator:

Stefan Kathman

Owner:

Scholarly Digital Publishing

Date Uploaded:

02/19/2018

Date Modified:

02/19/2018

Date Created:

2016-01-01

Resource Type:

Dissertation