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Literature DB >> 29185561

Near infrared imaging of Mer tyrosine kinase (MERTK) using MERi-SiR reveals tumor associated macrophage uptake in metastatic disease.

Miles A Miller¹, Eunha Kim, Michael F Cuccarese, Alec L Plotkin, Mark Prytyskach, Rainer H Kohler, Mikael J Pittet, Ralph Weissleder.

Abstract

The receptor tyrosine kinase Mer (MERTK) is a promising drug target in cancer, where it can influence the metastasis-promoting signaling of both tumor cells and immune cells alike; however, no small molecule probes currently exist to selectively image Mer. In this work, we design and synthesize a selective near-infrared fluorescent molecular probe of Mer (MERi-SiR). Confocal microscopy of metastases in mice reveals predominant probe accumulation in Mer-expressing tumor-associated macrophages.

Entities: CellLine Chemical Disease Gene Species

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Year: 2017 PMID： 29185561 PMCID： PMC5736449 DOI： 10.1039/c7cc07581b

Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222

13 in total

1. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.

Authors: Jing Liu; Chao Yang; Catherine Simpson; Deborah Deryckere; Amy Van Deusen; Michael J Miley; Dmitri Kireev; Jacqueline Norris-Drouin; Susan Sather; Debra Hunter; Victoria K Korboukh; Hari S Patel; William P Janzen; Mischa Machius; Gary L Johnson; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang
Journal: ACS Med Chem Lett Date: 2012-02-09 Impact factor: 4.345

2. MerTK receptor cleavage promotes plaque necrosis and defective resolution in atherosclerosis.

Authors: Bishuang Cai; Edward B Thorp; Amanda C Doran; Brian E Sansbury; Mat J A P Daemen; Bernhard Dorweiler; Matthew Spite; Gabrielle Fredman; Ira Tabas
Journal: J Clin Invest Date: 2017-01-09 Impact factor: 14.808

3. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.

Authors: Alexis Mollard; Steven L Warner; Lee T Call; Mark L Wade; Jared J Bearss; Anupam Verma; Sunil Sharma; Hariprasad Vankayalapati; David J Bearss
Journal: ACS Med Chem Lett Date: 2011-12-08 Impact factor: 4.345

4. Imaging the emergence and natural progression of spontaneous autoimmune diabetes.

Authors: James F Mohan; Rainer H Kohler; Jonathan A Hill; Ralph Weissleder; Diane Mathis; Christophe Benoist
Journal: Proc Natl Acad Sci U S A Date: 2017-08-24 Impact factor: 11.205

5. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models.

Authors: Deborah DeRyckere; Alisa B Lee-Sherick; Madeline G Huey; Amanda A Hill; Jeffrey W Tyner; Kristen M Jacobsen; Lauren S Page; Gregory G Kirkpatrick; Fatma Eryildiz; Stephanie A Montgomery; Weihe Zhang; Xiaodong Wang; Stephen V Frye; H Shelton Earp; Douglas K Graham
Journal: Clin Cancer Res Date: 2016-09-20 Impact factor: 12.531

Review 6. Silicon-substituted Xanthene Dyes and Their Unique Photophysical Properties for Fluorescent Probes.

Authors: Takayuki Ikeno; Tetsuo Nagano; Kenjiro Hanaoka
Journal: Chem Asian J Date: 2017-06-05

7. UNC1062, a new and potent Mer inhibitor.

Authors: Jing Liu; Weihe Zhang; Michael A Stashko; Deborah Deryckere; Christopher T Cummings; Debra Hunter; Chao Yang; Chatura N Jayakody; Nancy Cheng; Catherine Simpson; Jacqueline Norris-Drouin; Susan Sather; Dmitri Kireev; William P Janzen; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang
Journal: Eur J Med Chem Date: 2013-04-02 Impact factor: 6.514

8. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.

Authors: Weihe Zhang; Deborah DeRyckere; Debra Hunter; Jing Liu; Michael A Stashko; Katherine A Minson; Christopher T Cummings; Minjung Lee; Trevor G Glaros; Dianne L Newton; Susan Sather; Dehui Zhang; Dmitri Kireev; William P Janzen; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang
Journal: J Med Chem Date: 2014-08-06 Impact factor: 7.446

9. TAM receptors Tyro3 and Mer as novel targets in colorectal cancer.

Authors: Robin Schmitz; Aida Freire Valls; Rosario Yerbes; Sophie von Richter; Christoph Kahlert; Sonja Loges; Jürgen Weitz; Martin Schneider; Carmen Ruiz de Almodovar; Alexis Ulrich; Thomas Schmidt
Journal: Oncotarget Date: 2016-08-30

10. A near-infrared fluorophore for live-cell super-resolution microscopy of cellular proteins.

Authors: Gražvydas Lukinavičius; Keitaro Umezawa; Nicolas Olivier; Alf Honigmann; Guoying Yang; Tilman Plass; Veronika Mueller; Luc Reymond; Ivan R Corrêa; Zhen-Ge Luo; Carsten Schultz; Edward A Lemke; Paul Heppenstall; Christian Eggeling; Suliana Manley; Kai Johnsson
Journal: Nat Chem Date: 2013-01-06 Impact factor: 24.427

7 in total

Near infrared imaging of Mer tyrosine kinase (MERTK) using MERi-SiR reveals tumor associated macrophage uptake in metastatic disease.

1. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.

2. MerTK receptor cleavage promotes plaque necrosis and defective resolution in atherosclerosis.

3. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.

4. Imaging the emergence and natural progression of spontaneous autoimmune diabetes.

5. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models.

Review 6. Silicon-substituted Xanthene Dyes and Their Unique Photophysical Properties for Fluorescent Probes.

7. UNC1062, a new and potent Mer inhibitor.

8. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.

9. TAM receptors Tyro3 and Mer as novel targets in colorectal cancer.

10. A near-infrared fluorophore for live-cell super-resolution microscopy of cellular proteins.

1. Single-Cell Intravital Microscopy of Trastuzumab Quantifies Heterogeneous in vivo Kinetics.

2. Imaging of Tie2 with a Fluorescently Labeled Small Molecule Affinity Ligand.

Review 3. Chemical Probes and Activity-Based Protein Profiling for Cancer Research.

4. SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C.

Review 5. Fluorescent kinase inhibitors as probes in cancer.

6. Macrophage imaging and subset analysis using single-cell RNA sequencing.

Review 7. Targeted Optical Imaging Agents in Cancer: Focus on Clinical Applications.