Jetze J. Tepe
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View article: Recent Advancements in 20S Proteasome Enhancement: Degradation of Undruggable Targets
Recent Advancements in 20S Proteasome Enhancement: Degradation of Undruggable Targets Open
The ubiquitin-independent proteasome system has emerged as an attractive point of intervention for a variety of diseases, including neurodegenerative diseases. Though inhibition of this system has been studied for decades, 20S proteasome e…
View article: Tungsten-Enabled Diels–Alder Cycloaddition and Cycloreversion of Arenes and Alkynes: Divergent Synthesis of Highly Functionalized Barrelenes and Arenes
Tungsten-Enabled Diels–Alder Cycloaddition and Cycloreversion of Arenes and Alkynes: Divergent Synthesis of Highly Functionalized Barrelenes and Arenes Open
The Diels-Alder reaction of benzenes remains a significant synthetic challenge, owing to their highly stabilized aromatic cores. In this work, the dearomatization agent {WTp(NO)(PMe3)} is used to promote Diels-Alder reactions of…
View article: A Tetrazine‐Based Synthesis for Accessing Underutilized Aza‐Indole Analogues
A Tetrazine‐Based Synthesis for Accessing Underutilized Aza‐Indole Analogues Open
Aza‐indole functionalities fill an important role in drug discovery. While indoles are considered privileged scaffolds, aza‐indoles allow for better pharmacological properties and on‐target activities. Synthetic approaches to access aza‐in…
View article: Short and High-Yielding Synthesis of a Minimalist Diazirine–Alkyne Photo-Cross-Linker and Photoaffinity Labeling Derivatives
Short and High-Yielding Synthesis of a Minimalist Diazirine–Alkyne Photo-Cross-Linker and Photoaffinity Labeling Derivatives Open
Minimalist photo-cross-linker 1 and its derivatives are extensively utilized in photoaffinity labeling studies. However, obtaining compound 1 in high yield has traditionally required a lengthy synthetic process. In this paper…
View article: 20S proteasome enhancers prevent cytotoxic tubulin polymerization-promoting protein induced α-synuclein aggregation
20S proteasome enhancers prevent cytotoxic tubulin polymerization-promoting protein induced α-synuclein aggregation Open
Synucleinopathies are a class of neurodegenerative diseases defined by the presence of α-synuclein inclusions. The location and composition of these α-synuclein inclusions directly correlate to the disease pattern. The inclusions in Multip…
View article: Advances in the total synthesis of bis- and tris-indole alkaloids containing N-heterocyclic linker moieties
Advances in the total synthesis of bis- and tris-indole alkaloids containing N-heterocyclic linker moieties Open
This review highlights advances in isolation and synthesis of bis- and tris-indole alkaloids containing N -heterocyclic linker moieties. Natural products in this class are of particular significance due to their potent biological activitie…
View article: CCDC 2194100: Experimental Crystal Structure Determination
CCDC 2194100: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Development and Validation of a High-Throughput Cell-Based AlphaLISA Assay to Identify Small Molecule 20S Proteasome Modulators
Development and Validation of a High-Throughput Cell-Based AlphaLISA Assay to Identify Small Molecule 20S Proteasome Modulators Open
View article: CCDC 2196102: Experimental Crystal Structure Determination
CCDC 2196102: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Development of a Cell-Based AlphaLISA Assay for High-Throughput Screening for Small Molecule Proteasome Modulators
Development of a Cell-Based AlphaLISA Assay for High-Throughput Screening for Small Molecule Proteasome Modulators Open
The balance between protein degradation and protein synthesis is a highly choreographed process generally called proteostasis. Most intracellular protein degradation occurs through the ubiquitin-proteasome system (UPS). This degradation ta…
View article: CCDC 2153369: Experimental Crystal Structure Determination
CCDC 2153369: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2151168: Experimental Crystal Structure Determination
CCDC 2151168: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Small Molecule 20S Proteasome Enhancer Regulates MYC Protein Stability and Exhibits Antitumor Activity in Multiple Myeloma
Small Molecule 20S Proteasome Enhancer Regulates MYC Protein Stability and Exhibits Antitumor Activity in Multiple Myeloma Open
Despite the addition of several new agents to the armamentarium for the treatment of multiple myeloma (MM) in the last decade and improvements in outcomes, the refractory and relapsing disease continues to take a great toll, limiting overa…
View article: Advances in Proteasome Enhancement by Small Molecules
Advances in Proteasome Enhancement by Small Molecules Open
The proteasome system is a large and complex molecular machinery responsible for the degradation of misfolded, damaged, and redundant cellular proteins. When proteasome function is impaired, unwanted proteins accumulate, which can lead to …
View article: Perspectives on SARS-CoV-2 Main Protease Inhibitors
Perspectives on SARS-CoV-2 Main Protease Inhibitors Open
The main protease (Mpro) plays a crucial role in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication and is highly conserved, rendering it one of the most attractive therapeutic targets for SARS-CoV-2 inhibi…
View article: CCDC 2081971: Experimental Crystal Structure Determination
CCDC 2081971: Experimental Crystal Structure Determination Open
View article: Dihydroquinazolines enhance 20S proteasome activity and induce degradation of α-synuclein, an intrinsically disordered protein associated with neurodegeneration
Dihydroquinazolines enhance 20S proteasome activity and induce degradation of α-synuclein, an intrinsically disordered protein associated with neurodegeneration Open
View article: Enhancing c-MYC degradation via 20S proteasome activation induces<i>in vivo</i>anti-tumor efficacy
Enhancing c-MYC degradation via 20S proteasome activation induces<i>in vivo</i>anti-tumor efficacy Open
SUMMARY Enhancing proteasome activity is a potential new therapeutic strategy to prevent the accumulation of aberrant high levels of protein that drive the pathogenesis of many diseases. Herein, we examine the use of small molecules to act…
View article: Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors
Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors Open
The 20S proteasome is a valuable target for the treatment of a number of diseases including cancer, neurodegenerative disease, and parasitic infection.
View article: The preparation of (4<i>H</i>)-imidazol-4-ones and their application in the total synthesis of natural products
The preparation of (4<i>H</i>)-imidazol-4-ones and their application in the total synthesis of natural products Open
The first review article summarizing known methodologies for the preparation of (4H)-imidazol-4-ones and their application in the total synthesis of imidazol-4-one containing natural products.
View article: Proteasome Activation to Combat Proteotoxicity
Proteasome Activation to Combat Proteotoxicity Open
Loss of proteome fidelity leads to the accumulation of non-native protein aggregates and oxidatively damaged species: hallmarks of an aged cell. These misfolded and aggregated species are often found, and suggested to be the culpable party…
View article: Regulation of Autophagic Flux by the 20S Proteasome
Regulation of Autophagic Flux by the 20S Proteasome Open
View article: Proteasome Activation as a New Therapeutic Approach To Target Proteotoxic Disorders
Proteasome Activation as a New Therapeutic Approach To Target Proteotoxic Disorders Open
Proteasomes are multienzyme complexes that maintain protein homeostasis (proteostasis) and important cellular functions through the degradation of misfolded, redundant, and damaged proteins. It is well established that aging is associated …
View article: Small Molecule Enhancement of 20S Proteasome Activity Targets Intrinsically Disordered Proteins
Small Molecule Enhancement of 20S Proteasome Activity Targets Intrinsically Disordered Proteins Open
The 20S proteasome is the main protease for the degradation of oxidatively damaged and intrinsically disordered proteins. When accumulation of disordered or oxidatively damaged proteins exceeds proper clearance in neurons, imbalanced pathw…
View article: Regulation of Proteasomal Catalytic Activity by Altering its Protein-Protein Interactions
Regulation of Proteasomal Catalytic Activity by Altering its Protein-Protein Interactions Open
View article: Substituted quinolines as noncovalent proteasome inhibitors
Substituted quinolines as noncovalent proteasome inhibitors Open
View article: From Single Molecules to Single Cells: Biophysics of Interactions between Small Regulators and Proteasome
From Single Molecules to Single Cells: Biophysics of Interactions between Small Regulators and Proteasome Open
View article: CCDC 1491759: Experimental Crystal Structure Determination
CCDC 1491759: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …