Overexpression, point mutations or translocations of protein lysine methyltransferase NSD2 was occurred in {many|numerous|several|a lot of|quite a few|lots of} {types|kinds|varieties|sorts|forms} of cancer cells. {Therefore|Consequently|As a result|For that reason|Thus|Hence}, it was recognized as onco-protein and {considered|regarded as|deemed|regarded|viewed as|thought of} as a promising anticancer drug target. NSD2 consists of a SET catalytic domain and two PWWP domains binding to methylated histone proteins. {Here|Right here}, we reported our efforts to {develop|create} a series of NSD2-PWWP1 inhibitors, and {further|additional} structure-based optimization resulted a potent inhibitor 38, which has the {high|higher} selectivity towards NSD2-PWWP1 domain. The detailed biological evaluation revealed that compound 38 can bind to NSD2-PWWP1 {and then|and after that|after which|then} {affect|impact|have an effect on|influence} the expression of genes regulated by NSD2. The {current|present|existing} discovery will {provide|offer|supply|give|present|deliver} a {useful|helpful|beneficial|valuable} chemical probe {to the|towards the|for the} future {research|study|analysis|investigation} in understanding the {specific|particular|certain|distinct|precise} regulation mode of NSD2 by PWWP1 recognition, and pave the {way to|method to|approach to|strategy to|technique to|solution to} {develop|create} {potential|possible|prospective} drugs targeting NSD2 protein. 1633667-60-3 Order 2649788-76-9 Price PMID:24202965
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