Naphthalimide-Based Template for Inhibitor Screening via Cross-Linking and In-Gel Fluorescence: A Case Study against HCA II | Zendy

Monisha Singha | Zendy; Sayantani Roy | Zendy; Ravina Moirangthem | Zendy; Amit Kumar Das | Zendy; Amit Basak | Zendy

Open Access

Naphthalimide-Based Template for Inhibitor Screening via Cross-Linking and In-Gel Fluorescence: A Case Study against HCA II

Author(s) -

Monisha Singha,

Sayantani Roy,

Ravina Moirangthem,

Amit Kumar Das,

Amit Basak

Publication year - 2019

Publication title -

acs omega

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.779

H-Index - 40

ISSN - 2470-1343

DOI - 10.1021/acsomega.9b01044

Subject(s) - pharmacophore , carbonic anhydrase , chemistry , moiety , fluorescence , combinatorial chemistry , carbonic anhydrase ii , enzyme , biochemistry , chromatography , stereochemistry , physics , quantum mechanics

We describe a rapid electrophoresis-based method for profiling of carbonic anhydrase inhibitors. In addition to the pharmacophore moiety intended for reversible interaction with a target enzyme, a fluorescent template with a built-in azide group for photoaffinity labeling is also included as a part of the inhibitor design. Following incubation and irradiation, gel electrophoresis with visualization under UV allows assessment of the efficiency of cross-linking. The relative efficiency of cross-linking of various probes can be regarded as a reflection of their inhibition potencies, an assumption supported by the trend in their IC 50 / K i values. The method has the advantage of being applicable to impure enzyme preparations and also can be used to screen several inhibitors including their promiscuity in parallel in a short time as has been currently demonstrated with HCA II.

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