At the forefront of life sciences today is the emerging discipline of chembiomolecular science. This new term describes the integration of the frontier fields of chemical biology, chemistry, and pharmacology. Chembiomolecular science aims to elucidate new biological mechanisms as potential drug targets and enhance the creation of new drug therapies. This book comprises the proceedings of the Uehara Memorial Foundation Symposium 2011, which focused on the most recent advances in chembiomolecular science made by leading experts in the field. The book is divided into three main topics. The first is the chemical approach to understanding complex biological systems on a molecular level using chemical compounds as a probe. The second describes the biological approach used to develop new lead drug compounds. The third focuses on the biological system that serves as the potential drug target, the beginning step in the process of developing new drugs. Replete with the latest research, the book will draw the attention of all scientists interested in the synergies between chemistry and biology to elucidate life on a molecular level and to promote drug discovery. Ultimately, the book helps promote the understanding of biological functions at the molecular level and create new pharmaceuticals that can contribute to improving human health.