Rachel E. Heap
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View article: A chemoproteomic platform for selective deubiquitinase inhibitor discovery
A chemoproteomic platform for selective deubiquitinase inhibitor discovery Open
Chemoproteomics is a powerful method capable of detecting interactions between smallmolecules and the proteome; however, its use as a high-throughput screening method for chemical libraries has so far been limited. To address this need, we…
View article: Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments
Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments Open
Sulfur(VI) fluorides (SFs) have emerged as valuable electrophiles for the design of "beyond-cysteine" covalent inhibitors and offer potential for expansion of the liganded proteome. Since SFs target a broad range of nucleophilic amino acid…
View article: A chemoproteomic platform for reactive fragment profiling against the deubiquitinases
A chemoproteomic platform for reactive fragment profiling against the deubiquitinases Open
Summary Chemoproteomics is a powerful method capable of detecting interactions between small molecules and the proteome, however its use as a high-throughput screening method for chemical libraries has so far been limited. To address this …
View article: Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments
Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments Open
Sulfur(VI) fluorides (SFs) have emerged as valuable electrophiles for the design of 'beyond cysteine' covalent inhibitors, and offer potential for expansion of the liganded proteome. Since SFs target a broad range of nucleophilic amino aci…
View article: Advances in high‐throughput mass spectrometry in drug discovery
Advances in high‐throughput mass spectrometry in drug discovery Open
View article: Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments
Efficient Ligand Discovery Using Sulfur(VI) Fluoride Reactive Fragments Open
Sulfur(VI) fluorides (SFs) have emerged as valuable electrophiles for the design of 'beyond cysteine' covalent inhibitors, and offer potential for expansion of the liganded proteome. Since SFs target a broad range of nucleophilic amino aci…
View article: A high-throughput MALDI-TOF MS biochemical screen for small molecule inhibitors of the antigen aminopeptidase ERAP1
A high-throughput MALDI-TOF MS biochemical screen for small molecule inhibitors of the antigen aminopeptidase ERAP1 Open
MALDI-TOF MS is a powerful analytical technique that provides a fast and label-free readout for in vitro assays in the high-throughput screening (HTS) environment. Here, we describe the development of a novel, HTS compatible, MALDI-TOF MS-…
View article: Complement membrane attack complex is an immunometabolic regulator of NLRP3 activation and IL-18 secretion in human macrophages
Complement membrane attack complex is an immunometabolic regulator of NLRP3 activation and IL-18 secretion in human macrophages Open
The complement system is an ancient and critical part of innate immunity. Recent studies have highlighted novel roles of complement beyond lysis of invading pathogens with implications in regulating the innate immune response, as well as c…
View article: A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia
A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia Open
Inflammatory responses are important in cancer, particularly in the context of monocyte-rich aggressive myeloid neoplasm. We developed a label-free cellular phenotypic drug discovery assay to identify anti-inflammatory drugs in human monoc…
View article: Sublytic membrane attack complex drives glycolysis and mitochondrial dysfunction with inflammatory consequences in human monocyte-derived macrophages
Sublytic membrane attack complex drives glycolysis and mitochondrial dysfunction with inflammatory consequences in human monocyte-derived macrophages Open
The complement system is an ancient and critical element of the innate immune system. The terminal step in the complement pathway, the membrane attack complex (MAC), has previously been linked to inflammasome activation and is linked to th…
View article: Altered ceramide metabolism is a feature in the extracellular vesicle-mediated spread of alpha-synuclein in Lewy body disorders
Altered ceramide metabolism is a feature in the extracellular vesicle-mediated spread of alpha-synuclein in Lewy body disorders Open
Mutations in glucocerebrosidase ( GBA ) are the most prevalent genetic risk factor for Lewy body disorders (LBD)—collectively Parkinson’s disease, Parkinson’s disease dementia and dementia with Lewy bodies. Despite this genetic association…
View article: Proteomics characterisation of the L929 cell supernatant and its role in BMDM differentiation
Proteomics characterisation of the L929 cell supernatant and its role in BMDM differentiation Open
BMDMs are a key model system to study macrophage biology in vitro. Commonly used methods to differentiate macrophages from BM are treatment with either recombinant M-CSF or the supernatant of L929 cells, which secrete M-CSF. However, littl…
View article: A Direct-to-Biology High-Throughput Chemistry Approach to Reactive Fragment Screening
A Direct-to-Biology High-Throughput Chemistry Approach to Reactive Fragment Screening Open
Methods for rapid identification of chemical tools are essential for the validation of emerging targets and to provide medicinal chemistry starting points for the development of new medicines. Here, we report a screening platform that comb…
View article: A Direct-to-Biology High-Throughput Chemistry Approach to Reactive Fragment Screening
A Direct-to-Biology High-Throughput Chemistry Approach to Reactive Fragment Screening Open
Methods for rapid identification of chemical tools are essential for the validation of emerging targets and to provide medicinal chemistry starting points for the development of new medicines. Here, we report a screening platform that comb…
View article: A direct-to-biology high-throughput chemistry approach to reactive fragment screening
A direct-to-biology high-throughput chemistry approach to reactive fragment screening Open
A photoreactive fragment screening platform employing direct-to-biology high-throughput chemistry (D2B-HTC) for the rapid iterative synthesis and screening of libraries of photoaffinity bits.
View article: Proteomics characterisation of the L929 cell supernatant and its role in BMDM differentiation
Proteomics characterisation of the L929 cell supernatant and its role in BMDM differentiation Open
Bone marrow-derived macrophages (BMDMs) are a key model system to study macrophage biology in vitro . Commonly used methods to differentiate macrophages from bone marrow are treatment with either recombinant M-CSF or the supernatant of L92…
View article: Profiling embryonic stem cell differentiation by MALDI TOF mass spectrometry: development of a reproducible and robust sample preparation workflow
Profiling embryonic stem cell differentiation by MALDI TOF mass spectrometry: development of a reproducible and robust sample preparation workflow Open
A fast and robust sample preparation method for MALDI TOF MS analysis of whole mammalian cells and phenotypic profiling of mESCs.
View article: Identifying Inhibitors of Inflammation: A Novel High-Throughput MALDI-TOF Screening Assay for Salt-Inducible Kinases (SIKs)
Identifying Inhibitors of Inflammation: A Novel High-Throughput MALDI-TOF Screening Assay for Salt-Inducible Kinases (SIKs) Open