Protein tyrosine phosphatases (PTPases) are a general class of enzymes that are involved in a variety of disease processes, including diabetes and obesity. In a study by Z.-Y. Zhang and coworkers [J. Medicinal Chemistry 43 (2000): 146], computational techniques were used to identify potential competitive inhibitors of a specific PTPase known as PTP1B. The structure of one of the identified potential competitive inhibitors is shown here:

The reaction rate was determined in the presence and absence of inhibitor, I, and revealed the following initial reaction rates as a function of substrate concentration:

a. Determine Km and rate _max for PTP1B.

b. Demonstrate that the inhibition is competitive, and determine K_i.

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но, Но-С" N. Н PTP1B inhibitor [S] (AM) Rateo (pM s), ц - 0 Rateo (uM s), 1 % 200 иМ %3D 0.299 0.071 0.018 0.500 0.100 0.030 0.820 0.143 0.042 1.22 0.250 0.070 1.75 0.286 0.105 2.85 0.333 0.159 5.00 0.400 0.200 5.88 0.500 0.250