Affinity-based ranking of ligands for DPP-4 from mixtures.
Affinity-based selection strategies have recently emerged as a complement to traditional high throughput screening for the rapid discovery of lead compounds for the large number of protein targets emerging from--omics technologies. Herein, we describe a method for the ranking of mixtures of ligands by affinity selection and apply it to rank order a set of inhibitors for the enzyme dipeptidyl peptidase IV.
Adam
Gregory C
GC
Department of Target Validation, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. gregory_adam@merck.com
Meng
Juncai
J
Athanasopoulos
John
J
Zhang
Xiaoping
X
Chapman
Kevin T
KT
D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003920:Diabetes Mellitus / Q000188:drug therapy; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D008956:Models, Chemical
D004791:Enzyme Inhibitors; D008024:Ligands; D018819:Dipeptidyl Peptidase 4