Development of Novel Neurokinin 3 Receptor (NK3R) Selective Agonists with Resistance to Proteolytic Degradation

被引：16

作者：

Misu, Ryosuke ^{[1
]}

Oishi, Shinya ^{[1
]}

Yamada, Ai ^{[1
]}

Yamamura, Takashi ^{[2
]}

Matsuda, Fuko ^{[3
]}

Yamamoto, Koki ^{[1
]}

Noguchi, Taro ^{[1
]}

Ohno, Hiroaki ^{[1
]}

Okamura, Hiroaki ^{[2
]}

Ohkura, Satoshi ^{[3
]}

Fujii, Nobutaka ^{[1
]}

机构：

[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

[2] Natl Inst Agrobiol Sci, Anim Physiol Res Unit, Tsukuba, Ibaraki 3050901, Japan

[3] Nagoya Univ, Grad Sch Bioagr Sci, Nagoya, Aichi 4648601, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 57卷 / 20期

关键词：

PULSE-GENERATOR ACTIVITY; ARCUATE NUCLEUS; HORMONE SECRETION; SUBSTANCE-P; KISSPEPTIN/NEUROKININ B/DYNORPHIN; KISSPEPTIN NEURONS; DYNORPHIN-A; RAT; IDENTIFICATION; HYPOTHALAMUS;

D O I：

10.1021/jm500771w

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Neurokinin B (NKB) regulates the release of gonadotropin-releasing hormone (GnRH) via activation of the neurokinin-3 receptor (NK3R). We evaluated the biological stability of NK3R selective agonists to develop novel NK3R agonists to regulate reproductive functions. On the basis of degradation profiles, several peptidomimetic derivatives were designed. The modification of senktide with (E)-alkene dipeptide isostere generated a novel potent NK3R agonist with high stability and prolonged bioactivity.

引用

页码：8646 / 8651

页数：6

共 50 条

[31] Nk3R blockade has sex-divergent effects on memory in mice
Florido, Antonio
Moreno, Estefania
Canela, Enric, I
Andero, Raul
BIOLOGY OF SEX DIFFERENCES, 2022, 13 (01)
[32] Identification of novel and selective agonists for ABA receptor PYL3
Singh, Rahul
Bhardwaj, Vijay Kumar
Sharma, Jatin
Purohit, Rituraj
PLANT PHYSIOLOGY AND BIOCHEMISTRY, 2020, 154 : 387 - 395
[33] Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor
Carotenuto, Alfonso
Merlino, Francesco
Cai, Minying
Brancaccio, Diego
Yousif, Ali Munaim
Novellino, Ettore
Hruby, Victor J.
Grieco, Paolo
JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (24) : 9773 - 9778
[34] Novel Functional Role of NK3R Expression in the Potentiating Effects on Somatolactin α Autoregulation in grass carp pituitary cells
Guangfu Hu
Mulan He
Anderson On Lam Wong
Scientific Reports, 6
[35] Novel Functional Role of NK3R Expression in the Potentiating Effects on Somatolactin α Autoregulation in grass carp pituitary cells
Hu, Guangfu
He, Mulan
Wong, Anderson On Lam
SCIENTIFIC REPORTS, 2016, 6
[36] Localisation of neurokinin 3 (NK3) receptor immunoreactivity in the rat gastrointestinal tract
Patricia T. Mann
Bridget R. Southwell
Yu-Qiang Ding
Ryuichi Shigemoto
Noboru Mizuno
John B. Furness
Cell and Tissue Research, 1997, 289 : 1 - 9
[37] Localisation of neurokinin 3 (NK3) receptor immunoreactivity in the rat gastrointestinal tract
Mann, PT
Southwell, BR
Ding, YQ
Shigemoto, R
Mizuno, N
Furness, JB
CELL AND TISSUE RESEARCH, 1997, 289 (01) : 1 - 9
[38] Hypotension-induced trafficking of Neurokinin 3 Receptor (NK3-R) to the nucleus of neurons in the supraoptic nucleus (SON)
Sladek, Celia D.
Stevens, Wanida
Levinson, S. Rock
Song, Zhilin
Jensen, Dane D.
Flynn, Francis W.
FASEB JOURNAL, 2011, 25
[39] Localization of kisspeptin, NKB, and NK3R in the hypothalamus of gilts treated with the progestin altrenogest
Lindo, Ashley N.
Thorson, Jennifer F.
Bedenbaugh, Michelle N.
McCosh, Richard B.
Lopez, Justin A.
Young, Samantha A.
Meadows, Lanny J.
Bowdridge, Elizabeth C.
Fergani, Chrysanthi
Freking, Bradley A.
Lehman, Michael N.
Hileman, Stanley M.
Lents, Clay A.
BIOLOGY OF REPRODUCTION, 2021, 105 (04) : 1056 - 1067
[40] CHARACTERIZATION OF THE EFFECTS PRODUCED BY NEUROKININS AND 3 AGONISTS SELECTIVE FOR NEUROKININ RECEPTOR SUBTYPES IN A SPINAL NOCICEPTIVE REFLEX OF THE RAT
LANEUVILLE, O
DORAIS, J
COUTURE, R
LIFE SCIENCES, 1988, 42 (13) : 1295 - 1305

← 1 2 3 4 5 →