Conformationally restricted short peptides inhibit human islet amyloid polypeptide (hIAPP) fibrillization† †Electronic supplementary information (ESI) available: Experimental procedures, list of all the synthesized peptides and their % hIAPP fibrillization inhibition, MTT cytotoxicity assay, crystallization, details of X-ray structure determination, in silico docking of FGAΔFI with hIAPP, CD studies, Tables S1–S4, and Fig. S1–S6. CCDC 822015 and 904790. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c3cc38982kClick here for additional data file. Click here for additional data file.
نویسندگان
چکیده
hIAPP fibrillization implicated in Type 2 diabetes pathology involves formation of oligomers toxic to insulin producing pancreatic β-cells. We report design, synthesis, 3D structure and functional characterization of dehydrophenylalanine (ΔF) containing peptides which inhibit hIAPP fibrillization. The inhibitor protects β-cells from hIAPP induced toxicity.
منابع مشابه
Conformationally restricted short peptides inhibit human islet amyloid polypeptide (hIAPP) fibrillization†
Type 2 Diabetes Mellitus (T2DM) is one of the most prevalent endocrine disorders underlining the importance of developingmolecular therapies to mitigate T2DM. It is characterized by a significant decrease in b-cell mass, insulin resistance and presence of amyloid plaques in which human islet amyloid polypeptide (hIAPP) is the major protein component. hIAPP is a 37-residue polypeptide co-secrete...
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PCFM Lab, GD HPPC Lab, Guangdong Eng High-performance Organic and Polymer P Laboratory of Opto-electronic Material and Chemical Engineering, Sun Yet-sen Univers [email protected]; [email protected] 20 84112222; Tel: +86 20 84112712 State Key Laboratory of Optoelectronic Mat and Engineering, Sun Yat-sen University, Gu Shenzhen China Star Optoelectronics Techn TCL Corporate Research, Guangdon...
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School of Pharmaceutical Sciences, Southe Avenue North, Guangzhou 510515, China. E Department of Physics, The Hong Kong Un Water Bay, Kowloon, Hong Kong. E-mail: ph Guangdong Innovative Research Team, Materials and Devices, South China Unive China Department of Chemistry, State Key Labora of Molecular Functional Materials, The Technology, Clear Water Bay, Kowloon, Hon † Electronic supplementary...
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