A colleague pointed out to me this week that there’s a new edition of Copeland’s Evaluation of Enzyme Inhibitors in Drug Discovery. I haven’t seen this expanded and updated version, but the previous one was excellent. From the new preface:
. . .I have attempted to improve upon the first edition by substantially expanding most of the chapters with two overarching aims: to cover more completely the experimental aspects of the evaluation methods contained in each chapter and to enhance the clarity of the presentation, especially for the newcomer to applied enzymology. Toward these ends, a number of additional appendices have been added to the text, providing ready sources of useful information as they apply to quantitative biochemistry in drug discovery.
There are also two new chapters – one on residence time as a factor in enzyme inhibitor action, and another on the connections between in vitro enzymology and the factors in vivo that have to be considered for drug candidate selection. I have no problem recommending this one just on this basis.
And on a different (but still very useful) level, Erland Stevens of Davidson College has sent along a new textbook on medicinal chemistry that he’s written for the advanced undergraduate/grad student market. I’ve looked it over, and it’s a fine intro to the field, covering an impressively wide range of topics. All the classic stuff is there, but you’ll also find references up to at least 2010, including things like George Whitesides’ paper on linkers in fragment-based drug design, the structure of the P2X4 ion channel, and screening of crystallization conditions for API synthesis. If I were teaching a survey course on medicinal chemistry, I would be glad to use this as a text.