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Total Synthesis of Thielocin B1 as a Protein-Protein Interaction Inhibitor of PAC3 Homodimer

Part of the Springer Theses Book Series

DOI: 10.1007/978-4-431-55447-9

ISBN: 978-4-431-55446-2

Publisher: Springer Japan - Springer Journals

Jan 14, 2015

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Chapter 1Introduction

Ohsawa, Kosuke

Pages: 1 –23

[Protein–protein interactions (PPIs) play a vital role in numerous cellular functions, and have consequently been identified as novel drug discovery targets. However, it is quite difficult to find suitable drug-like lead compounds that behave as PPI inhibitors because small-molecule inhibitors...
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Chapter 2Total Synthesis of Thielocin B1 and NMR Chemical Shift Perturbation Experiments with PAC3 Homodimer

Ohsawa, Kosuke

Pages: 25 –62

[The first total synthesis of thielocin B1 has been achieved. The 2,2′,6,6′-tetrasubstituted diphenyl ether moiety of thielocin B1 was constructed by the oxidative lactonization of 2,2′-dihydroxybenzophenon, followed by the chemoselective reduction of the resulting lactone. During the process of...
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Chapter 3Synthesis of Spin-Labeled Thielocin B1 and Observation of Paramagnetic Relaxation Enhancement Effects

Ohsawa, Kosuke

Pages: 63 –87

[A new method has been developed for the synthesis of spin-labeled thielocin B1 to allow for further structural validation of the interaction between thielocin B1 and proteasome-assembling chaperone 3 (PAC3). A spin-labeling reagent was introduced to the left-hand side of thielocin B1 and...
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Chapter 4An Improved Method for the Direct Formylation of Substituted Benzenes Using Dichloromethyl Methyl Ether-Silver Trifluoromethanesulfonate

Ohsawa, Kosuke

Pages: 89 –106

[An improved procedure has been developed for the Rieche formylation of substituted benzenes using dichloromethyl methyl ether and silver trifluoromethanesulfonate. This reaction proceeds smoothly at low temperatures (−78 to 0 °C) over short reaction times (10–30 min), and allows for the...
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Chapter 5Conclusions

Ohsawa, Kosuke

Pages: 107 –108

[Thielocin B1 has been identified as a protein–protein interaction (PPI) inhibitor of proteasome-assembling chaperone 3 (PAC3), and the first total synthesis of thielocin B1 and its spin-labeled derivative have been described in detail.]

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