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Discovery of Drugs That Directly Target the Intrinsically Disordered Region of the Androgen Receptor by Sadar, Marianne D. is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Discovery of Drugs That Directly Target the Intrinsically Disordered Region of the Androgen Receptor about?

: Intrinsically disordered proteins (IDPs) and regions (IDRs) lack stable three-dimensional structure making drug discovery challenging. A validated therapeutic target for diseases such as prostate cancer is the androgen receptor (AR) which has a disordered amino-terminal domain (NTD) that contains all of its transcriptional activity. Drug discovery against the AR-NTD is of intense interest as a potential treatment for disease such as advanced prostate cancer that is driven by truncated constitutively active splice variants of AR that lack the C-terminal ligand-binding domain (LBD).: This article presents an overview of the relevance of AR and its intrinsically disordered NTD as a drug target. AR structure and approaches to blocking AR transcriptional activity are discussed. The discovery of small molecules, including the libraries used, proven binders to the AR-NTD, and site of interaction of these small molecules in the AR-NTD are presented along with discussion of the Phase I clinical trial.: The lack of drugs in the clinic that directly bind IDPs/IDRs reflects the difficulty of targeting these proteins and obtaining specificity. However, it may also point to an inappropriatenes

Who reads Discovery of Drugs That Directly Target the Intrinsically Disordered Region of the Androgen Receptor?

Author

Sadar, Marianne D.

Publisher

Informa plc; Informa UK (Taylor & Francis); Informa Healthcare; Informa UK Limited (ISSN 1746-0441)

Published

2020

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)