title: Analysis of protein acetyltransferase structure-function relation by surface-enhanced raman scattering (SERS): a tool to screen and characterize small molecule modulators.
abstract: Among the different posttranslational modifications (PTMs) that significantly regulate the protein function, lysine acetylation has become the major focus, especially to understand the epigenetic role of the acetyltransferases, in cellular physiology. Furthermore, dysfunction of these acetyltransferases is well documented under pathophysiological conditions. Therefore, it is important to understand the dynamic structure-function relationship of acetyltransferases in a relatively less complicated and faster method, which could be efficiently exploited to design and synthesis of small molecule modulators (activators/inhibitors) of these enzymes for in vivo functional analysis and therapeutic purposes. We have developed surface-enhanced Raman scattering (SERS) method, for acetyltransferases towards this goal. By employing SERS, we have not only demonstrated the autoacetylation induced structural changes of p300 enzyme but also could use this technique to characterize and design potent, specific inhibitors as well as activators of the p300. In this chapter we shall describe the methods in detail which could be highly useful for other classes of HATs and PTM enzymes.
authors: Transcription and Disease Laboratory, Molecular Biology and Genetics Unit, Jawaharlal Nehru Centre for Advanced Scientific Research, Bangalore, India.
authors: Mohammed
authors: M
authors: Arif
authors: Dhanasekaran
authors: D
authors: Karthigeyan
authors: Soumik
authors: S
authors: Siddhanta
authors: G V Pavan
authors: GV
authors: Kumar
authors: Chandrabhas
authors: C
authors: Narayana
authors: Tapas K
authors: TK
authors: Kundu
mesh_terms: D000107:Acetylation; D000123:Acetyltransferases / Q000737:chemistry* / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D011499:Protein Processing, Post-Translational; D013059:Spectrum Analysis, Raman / Q000379:methods*; D013329:Structure-Activity Relationship; D050880:p300-CBP Transcription Factors / Q000737:chemistry / Q000378:metabolism; D000099224:p300-CBP-Associated Factor
chemical_list: D000123:Acetyltransferases; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor