The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.
本发明涉及具有共同
化学结构的新化合物和探针,这种结构对于获得强大的对KLK4的抑制活性是必要的,或者可用于检测KLK4肽及其活性。它进一步涉及利用这些化合物和方法通过利用所述的探针或
抑制剂来抑制和/或检测体外和体内的KLK4活性。本发明的化合物与先前的化合物不同,至少在于存在
苯基胍(而不是
苄基胍等)和/或尾基中存在杂原子,它们的共同存在意外地导致强大和选择性的KLK4抑制活性。