Incorporation of Non-natural Amino Acids Improves Cell Permeability and Potency of Specific Inhibitors of Proteasome Trypsin-like Sites-Reference-Cited by-同舟云学术

Incorporation of Non-natural Amino Acids Improves Cell Permeability and Potency of Specific Inhibitors of Proteasome Trypsin-like Sites

Published:2013-01-28 Issue:3 Volume:56 Page:1262-1275
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Geurink Paul P.¹,van der Linden Wouter A.¹,Mirabella Anne C.²,Gallastegui Nerea³,de Bruin Gerjan¹,Blom Annet E. M.¹,Voges Mathias J.¹,Mock Elliot D.¹,Florea Bogdan I.¹,van der Marel Gijs A.¹,Driessen Christoph⁴,van der Stelt Mario¹,Groll Michael³,Overkleeft Herman S.¹,Kisselev Alexei F.²

Affiliation:

1. Gorlaeus Laboratories, Leiden Institute of Chemistry and Netherlands Proteomics Centre, Einsteinweg 55, 2333 CC Leiden, The Netherlands

2. Department of Pharmacology and Toxicology, and Norris Cotton Cancer Center, Geisel School of Medicine at Dartmouth, 1 Medical Center Drive HB7936, Lebanon, New Hampshire 03756, United States

3. Center for Integrated Protein Science at the Department Chemie, Lehrstuhl für Biochemie, Technische Unversität München, 85748 Garching, Germany

4. Department of Hematology and Oncology, Kantonsspital St. Gallen, 9007 St. Gallen, Switzerland

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm3016987

Reference43 articles.

1. A Phase 1 Dose Escalation Study of the Safety and Pharmacokinetics of the Novel Proteasome Inhibitor Carfilzomib (PR-171) in Patients with Hematologic Malignancies

2. A novel orally active proteasome inhibitor induces apoptosis in multiple myeloma cells with mechanisms distinct from Bortezomib

3. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib

4. Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer

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