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A Practical Total Synthesis of the Microbial Alkaline Proteinase Inhibitor (MAPI)
Author(s) -
Haebich Dieter,
Hillisch Alexander,
El Sheikh Sherif
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900346
Subject(s) - proteases , serine , chemistry , alkaline protease , enzyme , biochemistry , cysteine , combinatorial chemistry , function (biology) , computational biology , biology , protease , evolutionary biology
Diverse serine and cysteine proteases as well as alkaline proteinases and elastases play a crucial role in numerous biological processes. Natural peptide aldehydes such as the “microbial alkaline proteinase inhibitor” (MAPI, 1 ) are valuable tools to characterize novel enzymes and to study their function in nature. Within a drug discovery program we wanted to design and explore non‐natural MAPI congeners with novel biological profiles. To that end we devised a simple, practical, and scalable synthesis of MAPI 1 from readily available amino acid building blocks. The modular nature of our approach allows convenient structural modification of the MAPI backbone.