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View article: Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis
Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis Open
Metastasis is one of the defining features of pancreatic ductal adenocarcinoma (PDAC) that contributes to poor prognosis. In this study, the palmitoyl transferase ZDHHC20 was identified in an in vivo short hairpin RNA (shRNA) screen as cri…
View article: A palmitoyl transferase chemical genetic system to map ZDHHC-specific<i>S</i>-acylation
A palmitoyl transferase chemical genetic system to map ZDHHC-specific<i>S</i>-acylation Open
The 23 human ZDHHC S -acyltransferases catalyze long-chain S -acylation at cysteine residues across an extensive network of hundreds of proteins important for normal physiology or dysregulated in disease. Here we present a technology platf…
View article: Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis
Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis Open
Metastasis is one of the defining features of pancreatic ductal adenocarcinoma (PDAC) that contributes to poor prognosis. In this study, the palmitoyl transferase ZDHHC20 was identified in an in vivo shRNA screen as critical for metastatic…
View article: Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis
Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis Open
Metastasis is one of the defining features of pancreatic ductal adenocarcinoma (PDAC) that contributes to poor prognosis. In this study, the palmitoyl transferase ZDHHC20 was identified in an in vivo shRNA screen as critical for metastatic…
View article: Genotoxicity and Epigenotoxicity of Carbazole-Derived Molecules on MCF-7 Breast Cancer Cells
Genotoxicity and Epigenotoxicity of Carbazole-Derived Molecules on MCF-7 Breast Cancer Cells Open
The carbazole compounds PK9320 (1-(9-ethyl-7-(furan-2-yl)-9H-carbazol-3-yl)-N-methylmethanamine) and PK9323 (1-(9-ethyl-7-(thiazol-4-yl)-9H-carbazol-3-yl)-N-methylmethanamine), second-generation analogues of PK083 (1-(9-ethyl-9H-carbazol-3…
View article: Wheat pathogen<i>Zymoseptoria tritici N</i>-myristoyltransferase inhibitors: on-target antifungal activity and an unusual metabolic defense mechanism
Wheat pathogen<i>Zymoseptoria tritici N</i>-myristoyltransferase inhibitors: on-target antifungal activity and an unusual metabolic defense mechanism Open
Zymoseptoria tritici is the causative agent of Septoria tritici blotch (STB), which costs billions of dollars annually to major wheat-producing countries in terms of both fungicide use and crop loss. Agricultural pathogenic fungi have acqu…
View article: Wheat pathogen <i>Zymoseptoria tritici N</i> -myristoyltransferase inhibitors: on-target antifungal activity and an unusual metabolic defense mechanism
Wheat pathogen <i>Zymoseptoria tritici N</i> -myristoyltransferase inhibitors: on-target antifungal activity and an unusual metabolic defense mechanism Open
Investigation of the downstream effects of NMT inhibition identified novel defense mechanism against chemical toxicity in fungal pathogen Z. tritici.
View article: Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor
Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor Open
(+)-JD1, a rationally designed ferrocene analogue of the BET bromodomain (BRD) probe molecule (+)-JQ1, has been synthesized and evaluated in biophysical, cell-based assays as well as in pharmacokinetic studies. It displays nanomolar activi…
View article: Acylation-coupled lipophilic induction of polarisation (Acyl-cLIP): a universal assay for lipid transferase and hydrolase enzymes
Acylation-coupled lipophilic induction of polarisation (Acyl-cLIP): a universal assay for lipid transferase and hydrolase enzymes Open
A highly accurate and versatile fluorescence polarisation assay for any enzyme adding or removing lipid posttranslational modifications, with the potential to accelerate drug discovery against these targets.
View article: Correction: Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety
Correction: Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety Open
Correction for ‘Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety’ by Supojjanee Sansook et al. , Org. Biomol. Chem. , 2017, 15 , 8655–8660.
View article: Pojamide: An HDAC3-Selective Ferrocene Analogue with Remarkably Enhanced Redox-Triggered Ferrocenium Activity in Cells
Pojamide: An HDAC3-Selective Ferrocene Analogue with Remarkably Enhanced Redox-Triggered Ferrocenium Activity in Cells Open
A ferrocene containing ortho-aminoanilide, N1-(2-aminophenyl)-N8-ferrocenyloctanediamide, 2b (Pojamide) displayed nanomolar potency vs. HDAC3. Compared to RGFP966, a potent and selective HDAC3 inhibitor, Pojamide displayed superior activit…
View article: CCDC 1528186: Experimental Crystal Structure Determination
CCDC 1528186: 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 1528185: Experimental Crystal Structure Determination
CCDC 1528185: 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 1564152: Experimental Crystal Structure Determination
CCDC 1564152: 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 1564150: Experimental Crystal Structure Determination
CCDC 1564150: 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 1564153: Experimental Crystal Structure Determination
CCDC 1564153: 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 1564151: Experimental Crystal Structure Determination
CCDC 1564151: 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: Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety
Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety Open
A series of 3-methylidene-1H-indol-2(3H)-ones substituted with a 5- or 6-pentafluorosulfanyl group has been synthesized by a Knoevenagel condensation reaction of SF5-substituted oxindoles with a range of aldehydes.
View article: A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct
A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct Open
MASTL (microtubule-associated serine/threonine kinase-like), more commonly known as Greatwall (GWL), has been proposed as a novel cancer therapy target. GWL plays a crucial role in mitotic progression, via its known substrates ENSA/ARPP19,…
View article: CCDC 1485123: Experimental Crystal Structure Determination
CCDC 1485123: 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 1485122: Experimental Crystal Structure Determination
CCDC 1485122: 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 1485121: Experimental Crystal Structure Determination
CCDC 1485121: 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: Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors
Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors Open
Tetrasubstituted aromatic scaffolds have been elaborated and a number of EGFR inhibitors have been synthesised and their activity rationalised by docking studies.