Johns Hopkins University

Rapafusyn Pharmaceuticals, Inc.

Sam Hong

Jun O Liu

Jingxin Wang

Zhaoli Sun

Kana Yamamoto

Brett R Ullman

Puneet Kumar

Magesh Sadagopan

Joseph E Semple

Jennifer C Schmitt

Zufeng Guo

Manisha Das

Wukun Liu

Hanjing Peng

Jun Liu

The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.

Rapafucin derivative compounds and methods of use thereof

A compound of Formula I, and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.

Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof

A compound of Formula (I), and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions. 

A Rapafucin library containing compounds of the general structure, (A) and (E), and a synthesis of these compounds are provided. 

Synthesis and composition of rapafucin libraries

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Baltimore, MD, United States of America

Sam Hong