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Description

It features two distinct structural modifications: the substitution of a Glutamic acid for an Arginine at position 3 (hence Arg3), and a 13-amino-acid extension piece at the N-terminus (hence Long)

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Illustrative tubulysins are as follows: Compound 100a 100b 100c Tub B R allyl n-butyl n-pentyl IC50 on FR+ KB cell (nM) 1 .2 0.7 0.8 1 .2 EXAMPLE

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doi:10.1016/j.jacc.2018.10.060

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638 Blocking 1R prevents DN in rats and is a potentially effective treatment for peripheral neuropathies in diabetes patients

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