Small molecule somatostatin receptor subtype-2 antagonists

被引：11

作者：

Hay, BA ^{[1
]}

Cole, BM ^{[1
]}

DiCapua, F ^{[1
]}

Kirk, GW ^{[1
]}

Murray, MC ^{[1
]}

Nardone, RA ^{[1
]}

Pelletier, DJ ^{[1
]}

Ricketts, AP ^{[1
]}

Robertson, AS ^{[1
]}

Siegel, TW ^{[1
]}

机构：

[1] Pfizer Inc, Groton Labs, Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)00568-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The first potent small molecule sst2 antagonists are reported. Altering known sst2 agonist molecules yielded compounds with high sst2 binding affinity and full antagonist activity. Compound 7a, for example, displaced somatostatin binding to the sst2 receptor with an IC50 = 2.9 nM and antagonized somatostatin action with an IC50 = 29 nM. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2731 / 2734

页数：4

共 50 条

[1] NOVEL SOMATOSTATIN PEPTIDOMIMETICS AS SOMATOSTATIN RECEPTOR SUBTYPE-2 SPECIFIC IMAGING AGENTS
Han, G.
Kung, H. F.
Choi, S. R.
Makonnen, S.
Lee, W.
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2005, 48 : S265 - S265
[2] Antioncogenic role of somatostatin receptor subtype-2 in pancreatic cancer
Bousquet, C
Guillermet, J
Saint-Laurent, N
Fanjul, M
Estève, JP
Pyronnet, S
Susini, C
EUROPEAN JOURNAL OF ENDOCRINOLOGY, 2005, 152
[3] PREVALENCE OF SOMATOSTATIN RECEPTOR SUBTYPE-2 IN SOMATOSTATIN RECEPTOR-POSITIVE, GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS
SCHERUBL, H
JOHN, M
MEYERHOF, W
RICHTER, D
WASER, B
SCHAER, JC
BOESELANDGRAF, J
NEUHAUS, P
RIECKEN, EO
REUBI, JC
WIEDENMANN, B
GASTROENTEROLOGY, 1995, 108 (04) : A535 - A535
[4] Somatostatin Receptor Subtype-2 Targeting System for Specific Delivery of Temozolomide
Aghaamiri, Solmaz
Ghosh, Sukhen C.
Hernandez Vargas, Servando
Halperin, Daniel M.
Azhdarinia, Ali
JOURNAL OF MEDICINAL CHEMISTRY, 2024, 67 (04) : 2425 - 2437
[5] TRANSCRIPTION OF SOMATOSTATIN RECEPTOR SUBTYPE-1 AND SUBTYPE-2 GENES IN LUNG-CANCER
THOMAS, F
BRAMBRILLA, E
FRIEDMANN, A
LUNG CANCER, 1994, 11 (1-2) : 111 - 114
[6] Evans Blue Attachment Enhances Somatostatin Receptor Subtype-2 Imaging and Radiotherapy
Tian, Rui
Jacobson, Orit
Niu, Gang
Kiesewetter, Dale O.
Wang, Zhantong
Zhu, Guizhi
Ma, Ying
Liu, Gang
Chen, Xiaoyuan
THERANOSTICS, 2018, 8 (03): : 735 - 745
[7] ACTIVATION OF SOMATOSTATIN RECEPTOR SUBTYPE-2 INHIBITS ACID-SECRETION IN RATS
LLOYD, KCK
WANG, J
AURANG, K
GRONHED, P
COY, DH
WALSH, JH
AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY, 1995, 268 (01): : G102 - G106
[8] Evans Blue Attachment Enhances Somatostatin Receptor Subtype-2 Imaging and Radiotherapy
Tian, Rui
Jacobson, Orit
Niu, Gang
Kiesewetter, Dale
Wang, Zhantong
Zhu, Guizhi
Ma, Ying
Liu, Gang
Chen, Xiaoyuan
JOURNAL OF NUCLEAR MEDICINE, 2018, 59
[9] Specific Targeting of Somatostatin Receptor Subtype-2 for Fluorescence-Guided Surgery
Vargas, Servando Hernandez
Kossatz, Susanne
Voss, Julie
Ghosh, Sukhen C.
Cao, Hop S. Tran
Simien, Jo
Reiner, Thomas
Dhingra, Sadhna
Fisher, William E.
Azhdarinia, Ali
CLINICAL CANCER RESEARCH, 2019, 25 (14) : 4332 - 4342
[10] Membrane-displayed somatostatin activates somatostatin receptor subtype-2 heterologously produced in Saccharomyces cerevisiae
Hara, Keisuke
Shigemori, Tomohiro
Kuroda, Kouichi
Ueda, Mitsuyoshi
AMB EXPRESS, 2012, 2

← 1 2 3 4 5 →