Microscale thermophoresis for studying protein-small molecule affinity: Application to hyaluronidase

Indoleamine 2,3-dioxygenase 1 (IDO1) is a key target for the development of small molecule immunotherapies in oncology. In this framework, the screening of chemotherapeutic agents to identify compounds binding to IDO1 represents a valuable strategy for the development of multitarget drug candidates that combine synergic immunoregulatory properties to cytotoxic activity. In this study, we report that two natural compounds endowed with anticancer activity, namely lapachol and auraptene, act as IDO1 ligands with dissociation constant (Kd) in the micromolar range of potency. Docking studies provide plausible binding modes of these compounds to the catalytic cleft of IDO1. Our results support the notion that lapachol and auraptene may be considered interesting lead compounds in the immuno-oncology setting.

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Abstract LB-B17: Characterization of small molecule inhibitors of the Nrf2-Keap1 interaction using MicroScale Thermophoresis

10.1158/1535-7163.targ-17-lb-b17 ◽

2018 ◽

Author(s):

Julie M. Rainard ◽

Angus J. Morrison ◽

Andrew D. Pannifer ◽

Philip S. Jones ◽

Richard J. Mead ◽

...

Keyword(s):

Small Molecule ◽

Small Molecule Inhibitors ◽

Microscale Thermophoresis

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Detection and Characterization of Small Molecule Interactions with Fibrillar Protein Aggregates Using Microscale Thermophoresis

ACS Chemical Neuroscience ◽

10.1021/acschemneuro.7b00228 ◽

2017 ◽

Vol 8 (9) ◽

pp. 2088-2095 ◽

Cited By ~ 5

Author(s):

Emily Fisher ◽

Yanyan Zhao ◽

Robert Richardson ◽

Malgorzata Janik ◽

Alexander K. Buell ◽

...

Keyword(s):

Small Molecule ◽

Protein Aggregates ◽

Microscale Thermophoresis ◽

Molecule Interactions

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A privileged ternary blend enabling non-fullerene organic photovoltaics with over 14% efficiency

Journal of Materials Chemistry C ◽

10.1039/d0tc02778b ◽

2020 ◽

Vol 8 (43) ◽

pp. 15135-15141

Author(s):

Jing Yan ◽

Yuan-Qiu-Qiang Yi ◽

Jianqi Zhang ◽

Huanran Feng ◽

Yanfeng Ma ◽

...

Keyword(s):

Small Molecule ◽

Organic Photovoltaics ◽

Power Conversion ◽

Ternary Blend ◽

Conversion Efficiencies

Two non-fullerene small molecule acceptors, NT-4F and NT-4Cl, were designed and synthesized. Power conversion efficiencies of 11.44% and 14.55% were achieved for NT-4Cl-based binary and ternary devices, respectively.

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