Laura Depta
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View article: Identification of a Privileged Scaffold for Inhibition of Sterol Transport Proteins through the Synthesis and Ring Distortion of Diverse, Pseudo-Natural Products
Identification of a Privileged Scaffold for Inhibition of Sterol Transport Proteins through the Synthesis and Ring Distortion of Diverse, Pseudo-Natural Products Open
Sterol transport proteins mediate intracellular sterol transport, organelle contact sites, and lipid metabolism. Despite their importance, the similarities in their sterol-binding domains have made the identification of selective modulator…
View article: Schweinfurthins and their analogues are highly selective cellular probes for oxysterol-binding protein (OSBP)
Schweinfurthins and their analogues are highly selective cellular probes for oxysterol-binding protein (OSBP) Open
Schweinfurthin analogues – SAR, target engagement, MoA.
View article: Identification of a privileged scaffold for inhibition of sterol transport proteins through the synthesis and ring distortion of diverse, pseudo-natural products
Identification of a privileged scaffold for inhibition of sterol transport proteins through the synthesis and ring distortion of diverse, pseudo-natural products Open
Sterol transport proteins mediate intracellular sterol transport, organelle contact sites, and lipid metabolism. Despite their importance, the similarities in their sterol-binding domains have made the identification of selective modulator…
View article: Endogenous and fluorescent sterols reveal the molecular basis for ligand selectivity of human sterol transporters
Endogenous and fluorescent sterols reveal the molecular basis for ligand selectivity of human sterol transporters Open
Sterol transport proteins (STPs) play a pivotal role in cholesterol homeostasis and therefore are essential for healthy human physiology. Despite recent advances in dissecting functions of STPs in the human cell, there is still a significa…
View article: Fluorescent probes and degraders of the sterol transport protein Aster-A
Fluorescent probes and degraders of the sterol transport protein Aster-A Open
Our understanding of sterol transport proteins (STPs) has increased exponentially in the last decades with advances in the cellular and structural biology of these important proteins. However, small molecule probes have only recently been …
View article: Identification of non-conventional small molecule degraders and stabilizers of squalene synthase
Identification of non-conventional small molecule degraders and stabilizers of squalene synthase Open
Graphical abstract Squalene synthase (SQS) is an essential enzyme in the mevalonate pathway whose abundance and activity control cholesterol biosynthesis and homeostasis. Although catalytic inhibitors of SQS have been developed to attenuat…
View article: Selective inhibition of OSBP blocks retrograde trafficking by inducing partial Golgi degradation
Selective inhibition of OSBP blocks retrograde trafficking by inducing partial Golgi degradation Open
Sterol-binding proteins are important regulators of lipid homeostasis and membrane integrity; however, the discovery of selective small molecule modulators can be challenging due to structural similarities in the sterol binding domains. We…
View article: Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting the oxysterol-binding protein OSBP
Orpinolide disrupts a leukemic dependency on cholesterol transport by inhibiting the oxysterol-binding protein OSBP Open
Metabolic alterations in cancer precipitate in associated dependencies that can be therapeutically exploited. To meet this goal, natural product inspired small molecules can provide a resource of invaluable chemotypes. Here, we identify or…
View article: Identification of Biologically Diverse Tetrahydronaphthalen‐2‐ols through the Synthesis and Phenotypic Profiling of Chemically Diverse, Estradiol‐Inspired Compounds
Identification of Biologically Diverse Tetrahydronaphthalen‐2‐ols through the Synthesis and Phenotypic Profiling of Chemically Diverse, Estradiol‐Inspired Compounds Open
Combining natural product fragments to design new scaffolds with unprecedented bioactivity is a powerful strategy for the discovery of tool compounds and potential therapeutics. However, the choice of fragments to couple and the biological…
View article: Identification of non-conventional small molecule degraders and stabilizers of squalene synthase
Identification of non-conventional small molecule degraders and stabilizers of squalene synthase Open
Small molecule degraders and stabilizers of squalene synthase based on the same scaffold are reported, which respectively accelerate or block its natural degradation.
View article: Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions
Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions Open
Misregulation and mutations of the transcription factor Nrf2 are involved in the development of a variety of human diseases. In this study, we employed the technology of stapled peptides to address a protein-DNA-complex and designed a set …
View article: Structure, function and small molecule modulation of intracellular sterol transport proteins
Structure, function and small molecule modulation of intracellular sterol transport proteins Open
Intracellular sterol transport proteins (STPs) are crucial for maintaining cellular lipid homeostasis by regulating local sterol pools. Despite structural similarities in their sterol binding domains, STPs have different substrate specific…
View article: Spotlight on AKT: Current Therapeutic Challenges
Spotlight on AKT: Current Therapeutic Challenges Open
The protein kinase B (Akt) exemplifies an important switch of cell death and survival within the PI3K/Akt signaling pathway, which renders Akt a valuable target in diseases such as cancer. Herein, we give a short overview of clinical appli…
View article: Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity
Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity Open
Isoforms of protein kinase Akt are involved in essential processes including cell proliferation, survival, and metabolism. However, their individual roles in health and disease have not been thoroughly evaluated. Thus, there is an urgent n…
View article: Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity
Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity Open
Isoforms of protein kinase Akt are involved in essential processes including cell proliferation, survival, and metabolism. However, their individual roles in health and disease have not been thoroughly evaluated. Thus, there is an urgent n…
View article: Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt
Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt Open
Structure-based driven synthesis and biological evaluation provide innovative novel covalent-allosteric Akt inhibitors.