Incorporation of the Constrained Peptidomimetic, 5-Methylpyridin-2-one into Peptide Vinyl Sulfones and Peptide Epoxy Ketones is Detrimental for Proteasome Inhibition

Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays

(2014) Wenmin Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives

(2014) Karam Chand et al.   BIOORGANIC CHEMISTRY

Structure-Based Design of β1i or β5i Specific Inhibitors of Human Immunoproteasomes

(2014) Gerjan de Bruin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 5-Chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an Antidiabetic Clinical Candidate Targeting GPR119

(2014) Dean A. Wacker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploring dual electrophiles in peptide-based proteasome inhibitors: carbonyls and epoxides

(2014) Bo-Tao Xin et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Synthesis and Pharmacology of Proteasome Inhibitors

(2013) Andreas Rentsch et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Molecular Architecture and Assembly of the Eukaryotic Proteasome

(2013) Robert J. Tomko et al.   Annual Review of Biochemistry

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

(2013) Paul P. Geurink et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibitors for the Immuno- and Constitutive Proteasome: Current and Future Trends in Drug Development

(2012) Eva Maria Huber et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Proteasome Inhibitors: An Expanding Army Attacking a Unique Target

(2012) Alexei F. Kisselev et al.   CHEMISTRY & BIOLOGY

Development of Novel Peptidomimetics Containing a Vinyl Sulfone Moiety as Proteasome Inhibitors

(2011) Roberta Ettari et al.   ChemMedChem

In Vitro and In Vivo Selective Antitumor Activity of a Novel Orally Bioavailable Proteasome Inhibitor MLN9708 against Multiple Myeloma Cells

(2011) Dharminder Chauhan et al.   CLINICAL CANCER RESEARCH

Sugar amino acid based peptide epoxyketones as potential proteasome inhibitors

(2010) Martijn D.P. Risseeuw et al.   BIOORGANIC CHEMISTRY

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

(2010) E. Kupperman et al.   CANCER RESEARCH

Recognition and Processing of Ubiquitin-Protein Conjugates by the Proteasome

(2009) Daniel Finley   Annual Review of Biochemistry

Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome

(2009) F. Parlati et al.   BLOOD

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

(2009) O. A. O'Connor et al.   CLINICAL CANCER RESEARCH