37787-90-9Relevant articles and documents
A mimetic of the mSin3-binding helix of NRSF/REST ameliorates abnormal pain behavior in chronic pain models
Ueda, Hiroshi,Kurita, Jun-ichi,Neyama, Hiroyuki,Hirao, Yuuka,Kouji, Hiroyuki,Mishina, Tadashi,Kasai, Masaji,Nakano, Hirofumi,Yoshimori, Atsushi,Nishimura, Yoshifumi
supporting information, p. 4705 - 4709 (2017/09/29)
The neuron-restrictive silencing factor NRSF/REST binds to neuron-restrictive silencing elements in neuronal genes and recruits corepressors such as mSin3 to inhibit epigenetically neuronal gene expression. Because dysregulation of NRSF/REST is related to neuropathic pain, here, we have designed compounds to target neuropathic pain based on the mSin3-binding helix structure of NRSF/REST and examined their ability to bind to mSin3 by NMR. One compound, mS-11, binds strongly to mSin3 with a binding mode similar to that of NRSF/REST. In a mouse model of neuropathic pain, mS-11 was found to ameliorate abnormal pain behavior and to reverse lost peripheral morphine analgesia. Furthermore, even in the less well epigenetically defined case of fibromyalgia, mS-11 ameliorated symptoms in a mouse model, suggesting that fibromyalgia is related to the dysfunction of NRSF/REST. Taken together, these findings show that the chemically optimized mimetic mS-11 can inhibit mSin3-NRSF/REST binding and successfully reverse lost peripheral and central morphine analgesia in mouse models of pain.
Remarkable Optical Induction in the Reduction of α-Keto Esters with B-(3-Pinanyl)-9-borabicyclononane. Synthesis of α-Hydroxy Esters of 100percent Optical Purity
Brown, Herbert C.,Pai, Ganesh G.,Jadhav, Prabhakar K.
, p. 1531 - 1533 (2007/10/02)
-