Trypsin inhibitors for the treatment of pancreatitis

被引：15

作者：

Brandl, Trixi ^{[1
]}

Simic, Oliver ^{[1
]}

Skaanderup, Philip R. ^{[1
]}

Namoto, Kenji ^{[1
]}

Berst, Frederic ^{[1
]}

Ehrhardt, Claus ^{[1
]}

Schiering, Nikolaus ^{[1
]}

Mueller, Irene ^{[1
]}

Woelcke, Julian ^{[2
]}

机构：

[1] Novartis Pharma AG, Novartis Inst BioMed Res, Novartis Campus, CH-4002 Basel, Switzerland

[2] Novartis Pharma AG, Cardio Metab Dev Franchise, Novartis Campus, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 17期

关键词：

Trypsin inhibitor; Pancreatitis; hERG inhibition; X-ray crystal structure; HEREDITARY PANCREATITIS; DISCOVERY; MUTATIONS; DIAGNOSIS; GENE;

D O I：

10.1016/j.bmcl.2016.07.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Proline-based trypsin inhibitors occupying the S1-S2-S1' region were identified by an HTS screening campaign. It was discovered that truncation of the P1' moiety and appropriate extension into the S4 region led to highly potent trypsin inhibitors with excellent selectivity against related serine proteases and a favorable hERG profile. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：4340 / 4344

页数：5

共 50 条

[21] Changes of trypsin in activity and secondary structure induced by complex with trypsin inhibitors and tea polyphenol
Huihua Huang
Mouming Zhao
European Food Research and Technology, 2008, 227 : 361 - 365
[22] Immunosuppressive drugs for the treatment of autoimmune pancreatitis
Pezzilli, Raffaele
IMMUNOTHERAPY, 2014, 6 (04) : 477 - 483
[23] Treatment Strategies for Chronic Pancreatitis (CP)
Tlustochowicz, Katarzyna
Krajewska, Agnieszka
Kowalik, Adrianna
Malecka-Wojciesko, Ewa
PHARMACEUTICALS, 2025, 18 (03)
[24] The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis
Liddle, John
Beaufils, Benjamin
Binnie, Margaret
Bouillot, Anne
Denis, Alexis A.
Hann, Michael M.
Haslam, Carl P.
Holmes, Duncan S.
Hutchinson, Jon P.
Kranz, Michael
McBride, Andrew
Mirguet, Olivier
Mole, Damian J.
Mowat, Christopher G.
Pal, Sandeep
Rowland, Paul
Trottet, Lionel
Uings, Iain J.
Walker, Ann L.
Webster, Scott P.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (09) : 2023 - 2028
[25] In Vivo Imaging with Fluorescent Smart Probes to Assess Treatment Strategies for Acute Pancreatitis
Agarwal, Abhiruchi
Boettcher, Andreas
Kneuer, Rainer
Sari-Sarraf, Farid
Donovan, Adriana
Woelcke, Julian
Simic, Oliver
Brandl, Trixi
Krucker, Thomas
PLOS ONE, 2013, 8 (02):
[26] Clinical and Morphological Characteristics of Sporadic Genetically Determined Pancreatitis as Compared to Idiopathic Pancreatitis: Higher Risk of Pancreatic Cancer in CFTR Variants
Hamoir, Coralie
Pepermans, Xavier
Piessevaux, Hubert
Jouret-Mourin, Anne
Weynand, Birgit
Habyalimana, Jean-Baptiste
Leal, Teresinha
Geubel, Andre
Gigot, Jean-Francois
Deprez, Pierre H.
DIGESTION, 2013, 87 (04) : 229 - 239
[27] Tyrosine Kinase Inhibitors and Acute Pancreatitis
Pezzilli, Raffaele
Corinaldesi, Roberto
Morselli-Labate, Antonio Maria
JOURNAL OF THE PANCREAS, 2010, 11 (03): : 291 - 293
[28] TRYPSIN-INHIBITORS ANALYSIS - DIRECT CHROMATOGRAPHIC TITRATION
RASPI, G
LOMORO, A
SPINETTI, M
ANALYST, 1990, 115 (05) : 641 - 644
[29] EFFECTS OF STEAMING ON SOYBEAN PROTEINS AND TRYPSIN-INHIBITORS
ANDERSON, RL
JOURNAL OF THE AMERICAN OIL CHEMISTS SOCIETY, 1992, 69 (12) : 1170 - 1176
[30] STUDIES ON NATURAL AND MODIFIED PEPTIDE Trichosanthes TRYPSIN INHIBITORS
钱岳伟
谭复隆
戚正武
Science in China,SerB., 1990, Ser.B.1990 (05) : 599 - 605

← 1 2 3 4 5 →