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2. Identification of the critical residues of bradykinin receptor B1 for interaction with the kinins guided by site-directed mutagenesis and molecular modeling

Author

Ha, Sookhee N., Hey, Pat J., Ransom, Rick W., Bock, Mark G., Dai-Shi Su, Murphy, Kathryn L., Ray Chang, Tsing-Bau Chen, Pettibone, Douglas, and Hess, J. Fred

Subjects
Bradykinin -- Physiological aspects, Bradykinin -- Chemical properties, Mutagenesis -- Research, Biological sciences, Chemistry
Abstract

The critical residues for the interaction of the kinins with human bradykinin receptor 1 (B1) using site-directed mutagenesis in conjunction with molecular modeling of the binding modes of the kinins in the homology model of the B1 receptor are reported. Results indicate that the B1 bradykinin binding pocket for agonists and antagonists is similar but the manners in which they interact with the receptor do not completely overlap.

Published
2006

4. Potent bradykinin B1 receptor antagonists: 4-Substituted phenyl cyclohexanes

Author

Su, Dai-Shi, Lim, John L., Markowitz, M. Kristine, Wan, Bang-Lin, Murphy, Kathy L., Reiss, Duane R., Harrell, C. Meacham, O’Malley, Stacy S., Ransom, Rick W., Chang, Raymond S.L., Pettibone, Douglas J., Tang, Cuyue, Prueksaritanont, Thomayant, Freidinger, Roger M., and Bock, Mark G.

Subjects
*LEAD compounds, *INFLAMMATION, *PATHOLOGY, *PAIN
Abstract

Abstract: Selective bradykinin (BK) B1 receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure–activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B1 receptor antagonists. [Copyright &y& Elsevier]

Published
2007
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