The DOI matches its Crossref record; 24 of the 24 references it cites were found in a registry or an index.
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold
Open accessAbstract
Fibroblast activation protein (FAP) is a serine protease that is generally accepted to play an important role in tumor growth and other diseases involving tissue remodeling. Currently there are no FAP inhibitors with reported selectivity toward both the closely related dipeptidyl peptidases (DPPs) and prolyl oligopeptidase (PREP). We present the discovery of a new class of FAP inhibitors with a N-(4-quinolinoyl)-Gly-(2-cyanopyrrolidine) scaffold. We have explored the effects of substituting the quinoline ring and varying the position of its sp(2) hybridized nitrogen atom. The most promising inhibitors combined low nanomolar FAP inhibition and high selectivity indices (>10(3)) with respect to both the DPPs and PREP. Preliminary experiments on a representative inhibitor demonstrate that plasma stability, kinetic solubility, and log D of this class of compounds can be expected to be satisfactory.
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Cites
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Targeting fibroblast activation protein inhibits tumor stromagenesis and growth in mice
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Self-citationFibroblast activation protein is expressed by rheumatoid myofibroblast-like synoviocytes
Bauer, S., Jendro, M. C., Wadle, A., Kleber, S., Stenner, F., Dinser, R., Reich, A., Faccin, E., Gödde, S., Dinges, H., et al. (2006) · Arthritis Research & Therapy · doi:10.1186/ar2080 · Cited by 230
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Cited by
Lindner, T., Loktev, A., Altmann, A., Giesel, F., Kratochwil, C., Debus, J., Jäger, D., Mier, W., & Haberkorn, U. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.118.210443 · Cited by 935
Development of Fibroblast Activation Protein–Targeted Radiotracers with Improved Tumor Retention
Loktev, A., Lindner, T., Burger, E.-M., Altmann, A., Giesel, F., Kratochwil, C., Debus, J., Marmé, F., Jäger, D., Mier, W., et al. (2019) · Journal of Nuclear Medicine · doi:10.2967/jnumed.118.224469 · Cited by 554
Baum, R. P., Schuchardt, C., Singh, A., Chantadisai, M., Robiller, F. C., Zhang, J., Mueller, D., Eismant, A., Almaguel, F., Zboralski, D., et al. (2022) · Journal of Nuclear Medicine · doi:10.2967/jnumed.120.259192 · Cited by 359
Targeting of activated fibroblasts for imaging and therapy
Lindner, T., Loktev, A., Giesel, F., Kratochwil, C., Altmann, A., & Haberkorn, U. (2019) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-019-0069-0 · Cited by 205
Radiotheranostics in oncology: Making precision medicine possible
Aboagye, E. O., Barwick, T. D., & Haberkorn, U. (2023) · CA: A Cancer Journal for Clinicians · doi:10.3322/caac.21768 · Cited by 131
Bismuth-213 for targeted radionuclide therapy: from atom to bedside.
Ahenkorah, S., Cassells, I., Deroose, C. M., Cardinaels, T., Burgoyne, A. R., Bormans, G., Ooms, M., & Cleeren, F. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13050599 · Cited by 120
Metadata
- Authors
- Jansen, K., Heirbaut, L., Cheng, J. D., Joossens, J., Ryabtsova, O., Cos, P., Maes, L., Lambeir, A.-M., De Meester, I., Augustyns, K., & Van der Veken, P.
- Venue
- ACS Medicinal Chemistry Letters
- Publisher
- American Chemical Society (ACS)
- Published
- 2013-03-25
- Volume
- 4
- Issue
- 5
- Pages
- 491-496
- ISSN
- 1948-5875 (ISSN-L)
- OpenAlex
- W1994793426
- Cited by
- 260
- References
- 24
- FWCI
- 1.58
- Type
- journal article
- Language
- en
- Open access
- green
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