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Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance

Houthuijzen, Julia M ; Oosterom, Ilse ; Hudson, Brian D ; Hirasawa, Akira ; Daenen, Laura G. M ; Mclean, Chelsea M ; Hansen, Steffen V. F ; Van Jaarsveld, Marijn T. M ; Peeper, Daniel S ; Jafari Sadatmand, Sahar ; Roodhart, Jeanine M. L ; Van De Lest, Chris H. A ; Ulven, Trond ; Ishihara, Kenji ; Milligan, Graeme ; Voest, Emile E

The FASEB Journal, 2017, Vol.31(5), p.2195-2209 [Peer Reviewed Journal]

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Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system

Nakamoto, Kazuo ; Nishinaka, Takashi ; Matsumoto, Kengo ; Kasuya, Fumiyo ; Mankura, Mitsumasa ; Koyama, Yutaka ; Tokuyama, Shogo

Brain Research, 2012, Vol.1432, pp.74-83 [Peer Reviewed Journal]

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Activation of tongue-expressed GPR40 and GPR120 by non caloric agonists is not sufficient to drive preference in mice

Godinot, N ; Yasumatsu, K ; Barcos, M.E ; Pineau, N ; Ledda, M ; Viton, F ; Ninomiya, Y ; Le Coutre, J ; Damak, S

Neuroscience, 10 October 2013, Vol.250, pp.20-30 [Peer Reviewed Journal]

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Potentiation of insulin secretion and improvement of glucose intolerance by combining a novel G protein-coupled receptor 40 agonist DS-1558 with glucagon-like peptide-1 receptor agonists

Nakashima, Ryutaro ; Yano, Tatsuya ; Ogawa, Junko ; Tanaka, Naomi ; Toda, Narihiro ; Yoshida, Masao ; Takano, Rieko ; Inoue, Masahiro ; Honda, Takeshi ; Kume, Shoen ; Matsumoto, Koji

European Journal of Pharmacology, 15 August 2014, Vol.737, pp.194-201 [Peer Reviewed Journal]

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Novel GPR40 agonist AS2575959 exhibits glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion

Tanaka, Hirotsugu ; Yoshida, Shigeru ; Minoura, Hideaki ; Negoro, Kenji ; Shimaya, Akiyoshi ; Shimokawa, Teruhiko ; Shibasaki, Masayuki

Life Sciences, 17 January 2014, Vol.94(2), pp.115-121 [Peer Reviewed Journal]

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Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558

Takano, Rieko ; Yoshida, Masao ; Inoue, Masahiro ; Honda, Takeshi ; Nakashima, Ryutaro ; Matsumoto, Koji ; Yano, Tatsuya ; Ogata, Tsuneaki ; Watanabe, Nobuaki ; Hirouchi, Masakazu ; Kimura, Takako ; Toda, Narihiro

Bioorganic & Medicinal Chemistry, 01 September 2015, Vol.23(17), pp.5546-5565 [Peer Reviewed Journal]

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Design, synthesis and structure–activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker

Yang, Jianyong ; Li, Zheng ; Li, Huilan ; Liu, Chunxia ; Wang, Nasi ; Shi, Wei ; Liao, Chen ; Cai, Xingguang ; Huang, Wenlong ; Qian, Hai

Bioorganic & Medicinal Chemistry, 15 April 2017, Vol.25(8), pp.2445-2450 [Peer Reviewed Journal]

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8
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Discovery of novel pyrrole-based scaffold as potent and orally bioavailable free fatty acid receptor 1 agonists for the treatment of type 2 diabetes

Li, Zheng ; Pan, Miaobo ; Su, Xin ; Dai, Yuxuan ; Fu, Mian ; Cai, Xingguang ; Shi, Wei ; Huang, Wenlong ; Qian, Hai

Bioorganic & Medicinal Chemistry, 01 May 2016, Vol.24(9), pp.1981-1987 [Peer Reviewed Journal]

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Asymmetric syntheses of a GPR40 receptor agonist via diastereoselective and enantioselective conjugate alkynylation

Woo, Jacqueline C.S ; Cui, Sheng ; Walker, Shawn D ; Faul, Margaret M

Tetrahedron, 2010, Vol.66(26), pp.4730-4737 [Peer Reviewed Journal]

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10
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Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles

Guo, Bin ; Guo, Shimeng ; Huang, Jing ; Li, Jingya ; Li, Jia ; Chen, Qian ; Zhou, Xianli ; Xie, Xin ; Yang, Yushe

Bioorganic & Medicinal Chemistry, 01 December 2018, Vol.26(22), pp.5780-5791 [Peer Reviewed Journal]

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11
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Discovery of novel free fatty acid receptor 1 agonists bearing triazole core via click chemistry

Li, Zheng ; Yang, Jianyong ; Wang, Xuekun ; Li, Huilan ; Liu, Chunxia ; Wang, Nasi ; Huang, Wenlong ; Qian, Hai

Bioorganic & Medicinal Chemistry, 01 November 2016, Vol.24(21), pp.5449-5454 [Peer Reviewed Journal]

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12
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Agonists and protein kinase C-activation induce phosphorylation and internalization of FFA1 receptors

Sosa-Alvarado, Carla ; Hernández-Méndez, Aurelio ; Romero-Ávila, M. Teresa ; Sánchez-Reyes, Omar B ; Takei, Yoshinori ; Tsujimoto, Gozoh ; Hirasawa, Akira ; García-Sáinz, J. Adolfo

European Journal of Pharmacology, 05 December 2015, Vol.768, pp.108-115 [Peer Reviewed Journal]

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13
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Involvement of GPR40, a long-chain free fatty acid receptor, in the production of central post-stroke pain after global cerebral ischemia

Harada, Shinichi ; Haruna, Yuka ; Aizawa, Fuka ; Matsuura, Wataru ; Nakamoto, Kazuo ; Yamashita, Takuya ; Kasuya, Fumiyo ; Tokuyama, Shogo

European Journal of Pharmacology, 05 December 2014, Vol.744, pp.115-123 [Peer Reviewed Journal]

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14
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Co-localisation and secretion of glucagon-like peptide 1 and peptide YY from primary cultured human L cells

Habib, A. ; Richards, P. ; Rogers, G. ; Reimann, F. ; Gribble, F.

Diabetologia, 2013, Vol.56(6), pp.1413-1416 [Peer Reviewed Journal]

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G protein-coupled receptor (GPR)40-dependent potentiation of insulin secretion in mouse islets is mediated by protein kinase D1

Ferdaoussi, M. ; Bergeron, V. ; Zarrouki, B. ; Kolic, J. ; Cantley, J. ; Fielitz, J. ; Olson, E. ; Prentki, M. ; Biden, T. ; MacDonald, P. ; Poitout, V.

Diabetologia, 2012, Vol.55(10), pp.2682-2692 [Peer Reviewed Journal]

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16
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Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold

Krasavin, Mikhail ; Lukin, Alexey ; Zhurilo, Nikolay ; Kovalenko, Alexey ; Zahanich, Ihor ; Zozulya, Sergey ; Moore, Daniel ; Tikhonova, Irina G

Bioorganic & Medicinal Chemistry, 01 July 2016, Vol.24(13), pp.2954-2963 [Peer Reviewed Journal]

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17
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Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835

Krasavin, Mikhail ; Lukin, Alexey ; Bagnyukova, Daria ; Zhurilo, Nikolay ; Zahanich, Ihor ; Zozulya, Sergey ; Ihalainen, Jouni ; Forsberg, Markus M ; Lehtonen, Marko ; Rautio, Jarkko ; Moore, Daniel ; Tikhonova, Irina G

Bioorganic & Medicinal Chemistry, 01 November 2016, Vol.24(21), pp.5481-5494 [Peer Reviewed Journal]

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18
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A thorough QT/QTc study of the effect of fasiglifam, a GPR40 agonist, on cardiac repolarization in healthy adults

Lee, Ronald D. ; Nudurupati, Sai ; Marcinak, John ; Viswanathan, Prabhakar

Clinical Pharmacology in Drug Development, March 2015, Vol.4(3), pp.175-183 [Peer Reviewed Journal]

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19
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Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist

Agarwal, Sameer ; Sasane, Santosh ; Deshmukh, Prashant ; Rami, Bhadresh ; Bandyopadhyay, Debdutta ; Giri, Poonam ; Giri, Suresh ; Jain, Mukul ; Desai, Ranjit C

ACS medicinal chemistry letters, 08 December 2016, Vol.7(12), pp.1134-1138 [Peer Reviewed Journal]

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20
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DHA promotes the neuronal differentiation of rat neural stem cells transfected with GPR40 gene

Ma, Dexuan ; Zhang, Minmin ; Larsen, Christian P ; Xu, Feng ; Hua, Wei ; Yamashima, Tetsumori ; Mao, Ying ; Zhou, Liangfu

Brain Research, 2010, Vol.1330, pp.1-8 [Peer Reviewed Journal]

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21
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Different effects of GPR120 and GPR40 on cellular functions stimulated by 12-O-tetradecanoylphorbol-13-acetate in melanoma cells

Fukushima, Kaori ; Takahashi, Kaede ; Fukushima, Nobuyuki ; Honoki, Kanya ; Tsujiuchi, Toshifumi

Biochemical and Biophysical Research Communications, 17 June 2016, Vol.475(1), pp.25-30 [Peer Reviewed Journal]

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22
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Rosiglitazone inhibition of calvaria-derived osteoblast differentiation is through both of PPARγ and GPR40 and GSK3β-dependent pathway

Tang, Xiao-Lu ; Wang, Chang-Nan ; Zhu, Xiao-Yan ; Ni, Xin

Molecular and Cellular Endocrinology, 15 September 2015, Vol.413, pp.78-89 [Peer Reviewed Journal]

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23
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Diverse effects of G-protein-coupled free fatty acid receptors on the regulation of cellular functions in lung cancer cells

Kita, Tsubasa ; Kadochi, Yui ; Takahashi, Kaede ; Fukushima, Kaori ; Yamasaki, Eri ; Uemoto, Taiki ; Hirane, Miku ; Fukushima, Nobuyuki ; Honoki, Kanya ; Tsujiuchi, Toshifumi

Experimental Cell Research, 15 March 2016, Vol.342(2), pp.193-199 [Peer Reviewed Journal]

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24
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Design and Synthesis of Novel, Selective GPR40 AgoPAMs

Plummer, Christopher W ; Clements, Matthew J ; Chen, Helen ; Rajagopalan, Murali ; Josien, Hubert ; Hagmann, William K ; Miller, Michael ; Trujillo, Maria E ; Kirkland, Melissa ; Kosinski, Daniel ; Mane, Joel ; Pachanski, Michele ; Cheewatrakoolpong, Boonlert ; Nolting, Andrew F ; Orr, Robert ; Christensen, Melodie ; Campeau, Louis-Charles ; Wright, Michael J ; Bugianesi, Randal ; Souza, Sarah ; Zhang, Xiaoping ; Di Salvo, Jerry ; Weinglass, Adam B ; Tschirret-Guth, Richard ; Nargund, Ravi ; Howard, Andrew D ; Colletti, Steven L

ACS medicinal chemistry letters, 09 February 2017, Vol.8(2), pp.221-226 [Peer Reviewed Journal]

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25
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Design, Synthesis and in Combo Antidiabetic Bioevaluation of Multitarget Phenylpropanoic Acids

Colín-Lozano, Blanca ; Estrada-Soto, Samuel ; Chávez-Silva, Fabiola ; Gutiérrez-Hernández, Abraham ; Cerón-Romero, Litzia ; Giacoman-Martínez, Abraham ; Almanza-Pérez, Julio Cesar ; Hernández-Núñez, Emanuel ; Wang, Zhilong ; Xie, Xin ; Cappiello, Mario ; Balestri, Francesco ; Mura, Umberto ; Navarrete-Vazquez, Gabriel

Molecules (Basel, Switzerland), 06 February 2018, Vol.23(2) [Peer Reviewed Journal]

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26
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Discovery of 2,3‐Dihydro‐1H‐indene Derivatives as Novel GPR40 Agonists

An, Kyung‐Mi ; Hong, Chang‐Hee ; Kwak, Hyun‐Jung ; Cui, Shuolin ; Song, Hyo‐Jung ; Park, Joon‐Tae ; Moon, An‐Na ; Kim, Jeong‐Ah ; Yang, Ji‐Hun ; Yoon, Jongmin ; Lee, Myongjae ; Jeong, Dong‐Gu ; Kim, Dohee ; Lee, Don‐Gil ; Shin, Jeongcheol ; Je, In‐Gyu ; Lee, Hong‐Sub ; Park, Soobong ; Kang, Jae‐Hoon ; Ko, Soo Young

Bulletin of the Korean Chemical Society, August 2017, Vol.38(8), pp.861-868 [Peer Reviewed Journal]

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27
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Free fatty acid receptors as therapeutic targets for the treatment of diabetes

Atsuhiko Eichimura ; Atsuhiko Eichimura ; Sae Ehasegawa ; Mayu Ekasubuchi ; Ikuo Ekimura ; Ikuo Ekimura

Frontiers in Pharmacology, 01 November 2014, Vol.5 [Peer Reviewed Journal]

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28
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Lysophosphatidylcholine and its phosphorothioate analogues potentiate insulin secretion via GPR40 (FFAR1), GPR55 and GPR119 receptors in a different manner

Drzazga, Anna ; Kristinsson, Hjalti ; Sałaga, Maciej ; Zatorski, Hubert ; Koziołkiewicz, Maria ; Gendaszewska-Darmach, Edyta ; Bergsten, Peter

Molecular and Cellular Endocrinology, 05 September 2018, Vol.472, pp.117-125 [Peer Reviewed Journal]

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29
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Opposite effects of GPR120 and GPR40 on cell motile activity induced by ethionine in liver epithelial cells

Ishii, Shuhei ; Hirane, Miku ; Kato, Sayumi ; Fukushima, Nobuyuki ; Tsujiuchi, Toshifumi

Biochemical and Biophysical Research Communications, 02 January 2015, Vol.456(1), pp.135-138 [Peer Reviewed Journal]

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30
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A selective GPR40 (FFAR1) agonist LY2881835 provides immediate and durable glucose control in rodent models of type 2 diabetes

Chen, Yanyun ; Song, Min ; Riley, Jonathan P. ; Hu, Charlie C. ; Peng, Xianbu ; Scheuner, Donalyn ; Bokvist, Krister ; Maiti, Pranab ; Kahl, Steven D. ; Montrose‐Rafizadeh, Chahrzad ; Hamdouchi, Chafiq ; Miller, Anne Reifel

Pharmacology Research & Perspectives, December 2016, Vol.4(6), pp.n/a-n/a [Peer Reviewed Journal]

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31
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3‐Aryl‐3‐(isoxazol‐3‐yl)propanoic Acids and 2‐Aryloxyacetic Acids as Potent GPR40 Agonists

An, Kyung‐Mi ; Hong, Chang‐Hee ; Kwak, Hyun‐Jung ; Cui, Shuolin ; Song, Hyo‐Jung ; Park, Joon‐Tae ; Moon, An‐Na ; Kim, Jeong‐Ah ; Yang, Ji‐Hun ; Yoon, Jongmin ; Lee, Myongjae ; Jeong, Dong‐Gu ; Kim, Dohee ; Shin, Jeongcheol ; Hong, Dahae ; Lee, Hong‐Sub ; Park, Soobong ; Kang, Jae‐Hoon ; Ko, Soo Young

Bulletin of the Korean Chemical Society, August 2017, Vol.38(8), pp.838-844 [Peer Reviewed Journal]

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32
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Different effects of G-protein-coupled receptor 120 (GPR120) and GPR40 on cell motile activity of highly migratory osteosarcoma cells

Takahashi, Kaede ; Fukushima, Kaori ; Onishi, Yuka ; Node, Yusuke ; Inui, Karin ; Fukushima, Nobuyuki ; Honoki, Kanya ; Tsujiuchi, Toshifumi

Biochemical and Biophysical Research Communications, 11 March 2017, Vol.484(3), pp.675-680 [Peer Reviewed Journal]

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33
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Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists

Du, Xiaohui ; Dransfield, Paul J ; Lin, Daniel C-H ; Wong, Simon ; Wang, Yingcai ; Wang, Zhongyu ; Kohn, Todd ; Yu, Ming ; Brown, Sean P ; Vimolratana, Marc ; Zhu, Liusheng ; Li, An-Rong ; Su, Yongli ; Jiao, Xianyun ; Liu, Jiwen Jim ; Swaminath, Gayathri ; Tran, Thanhvien ; Luo, Jian ; Zhuang, Run ; Zhang, Jane ; Guo, Qi ; Li, Frank ; Connors, Richard ; Medina, Julio C ; Houze, Jonathan B

ACS medicinal chemistry letters, 10 April 2014, Vol.5(4), pp.384-9 [Peer Reviewed Journal]

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34
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Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists

Takano, Rieko ; Yoshida, Masao ; Inoue, Masahiro ; Honda, Takeshi ; Nakashima, Ryutaro ; Matsumoto, Koji ; Yano, Tatsuya ; Ogata, Tsuneaki ; Watanabe, Nobuaki ; Toda, Narihiro

Bioorganic & Medicinal Chemistry Letters, 01 July 2014, Vol.24(13), pp.2949-2953 [Peer Reviewed Journal]

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35
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A novel GPR40 agonist, CNX-011-67, suppresses glucagon secretion in pancreatic islets under chronic glucolipotoxic conditions in vitro

Verma, Mahesh Kumar ; Biswas, Sanghamitra ; Chandravanshi, Bhawna ; Neelima, Korrapati ; Oommen, Anup M ; Jagannath, Madanahalli R ; Somesh, Baggavalli P

BMC Research Notes, 2014, Vol.7(1) [Peer Reviewed Journal]

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36
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The G-protein-coupled long-chain fatty acid receptor GPR40 and glucose metabolism

Tsutomu Etomita ; Kiminori Ehosoda ; Junji Efujikura ; Nobuya Einagaki ; Kazuwa Enakao

Frontiers in Endocrinology, 01 September 2014, Vol.5 [Peer Reviewed Journal]

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37
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Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists

Huang, Jing ; Guo, Bin ; Chu, Wen-Jing ; Xie, Xin ; Yang, Yu-She ; Zhou, Xian-Li

Chinese Chemical Letters, January 2016, Vol.27(1), pp.159-162 [Peer Reviewed Journal]

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