Jay H. Kalin
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View article: The Allosteric Regulator Inositol Phosphate Dramatically Affects the Efficacy and Selectivity of Inhibitors for Different HDAC Complexes
The Allosteric Regulator Inositol Phosphate Dramatically Affects the Efficacy and Selectivity of Inhibitors for Different HDAC Complexes Open
Class I histone deacetylases regulate gene transcription and are established therapeutic targets. HDAC1-3 form the catalytic subunit in several distinct multiprotein complexes; however, HDAC inhibitors are rarely studied in the context of …
View article: Targeting NEDD9-SH3 with a Covalent Peptide Controls Endothelial Phenotype
Targeting NEDD9-SH3 with a Covalent Peptide Controls Endothelial Phenotype Open
Src homology 3 (SH3) proteins regulate numerous fibroproliferative pathophenotypes including pulmonary arterial hypertension (PAH) but are challenging to target therapeutically. We innovated a peptidomimetic that occupies the canonical foc…
View article: Discovery of a non-nucleoside inhibitor that binds to a novel site in the palm domain of the respiratory syncytial virus RNA-dependent RNA polymerase
Discovery of a non-nucleoside inhibitor that binds to a novel site in the palm domain of the respiratory syncytial virus RNA-dependent RNA polymerase Open
Respiratory syncytial virus (RSV) is a major cause of severe respiratory tract infections in infants, young children, and the elderly. We report herein the discovery and characterization of a novel RSV polymerase (RSVpol) non-nucleoside in…
View article: The CoREST repressor complex mediates phenotype switching and therapy resistance in melanoma
The CoREST repressor complex mediates phenotype switching and therapy resistance in melanoma Open
Virtually all patients with BRAF-mutant melanoma develop resistance to MAPK inhibitors largely through nonmutational events. Although the epigenetic landscape is shown to be altered in therapy-resistant melanomas and other cancers, a speci…
View article: Supplementary Figures 1-7 and Table S1 from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer
Supplementary Figures 1-7 and Table S1 from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer Open
Supplementary Table S1: Mutational status of common oncogenes in CRC and STAD cell lines. Supplementary Figure S1: Mutant PIK3CA does not regulate LSD1 expression. Supplementary Figure S2: DNase signal is not generally depleted at TSS's, a…
View article: Data from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer
Data from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer Open
Activation of the epithelial-to-mesenchymal transition (EMT) program is a critical mechanism for initiating cancer progression and migration. Colorectal cancers contain many genetic and epigenetic alterations that can contribute to EMT. Mu…
View article: Supplementary Materials and Methods from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer
Supplementary Materials and Methods from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer Open
Contains additional details on bioinformatic analyses, including references for packages used.
View article: Supplementary Figures 1-7 and Table S1 from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer
Supplementary Figures 1-7 and Table S1 from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer Open
Supplementary Table S1: Mutational status of common oncogenes in CRC and STAD cell lines. Supplementary Figure S1: Mutant PIK3CA does not regulate LSD1 expression. Supplementary Figure S2: DNase signal is not generally depleted at TSS's, a…
View article: Data from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer
Data from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer Open
Activation of the epithelial-to-mesenchymal transition (EMT) program is a critical mechanism for initiating cancer progression and migration. Colorectal cancers contain many genetic and epigenetic alterations that can contribute to EMT. Mu…
View article: Supplementary Materials and Methods from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer
Supplementary Materials and Methods from Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i>-Mutant Colorectal Cancer Open
Contains additional details on bioinformatic analyses, including references for packages used.
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes Open
Background: Schistosoma mansoni, a parasitic worm species responsible for the neglected tropical disease schistosomiasis, undergoes strict developmental regulation of gene expression that is carefully controlled by both genetic and epigene…
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures Open
Extended data This project contains the following extended data: - Fig S1. Dose response titrations of compounds 15, 16, 33, 35 and 36 against schistosomula. - Fig S2. Compound 33 treatment induces the release of oocytes, spermatozoa and v…
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures Open
Extended data This project contains the following extended data: - Fig S1. Dose response titrations of compounds 15, 16, 33, 35 and 36 against schistosomula. - Fig S2. Compound 33 treatment induces the release of oocytes, spermatozoa and v…
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures Open
Extended data This project contains the following extended data: - Fig S1. Dose response titrations of compounds 15, 16, 33, 35 and 36 against schistosomula. - Fig S2. Compound 33 treatment induces the release of oocytes, spermatozoa and v…
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures Open
Extended data This project contains the following extended data: - Fig S1. Dose response titrations of compounds 15, 16, 33, 35 and 36 against schistosomula. - Fig S2. Compound 33 treatment induces the release of oocytes, spermatozoa and v…
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary Figures Open
Extended data This project contains the following extended data: - Fig S1. Dose response titrations of compounds 15, 16, 33, 35 and 36 against schistosomula. - Fig S2. Compound 33 treatment induces the release of oocytes, spermatozoa and v…
View article: Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary tables and movies
Chemical modulation of Schistosoma mansoni lysine specific demethylase 1 (SmLSD1) induces wide-scale biological and epigenomic changes - Supplementary tables and movies Open
Extended data This project contains the following extended data: Table S1. Chemical structures of the 39 compounds included in this study. Table S2. Z´ values for both phenotype and motility of the Roboworm screens performed on the 39 com…
View article: Structure of human spermine oxidase in complex with a highly selective allosteric inhibitor
Structure of human spermine oxidase in complex with a highly selective allosteric inhibitor Open
Human spermine oxidase (hSMOX) plays a central role in polyamine catabolism. Due to its association with several pathological processes, including inflammation and cancer, hSMOX has garnered interest as a possible therapeutic target. There…
View article: Development and characterization of rabbit monoclonal antibodies that recognize human spermine oxidase and application to immunohistochemistry of human cancer tissues
Development and characterization of rabbit monoclonal antibodies that recognize human spermine oxidase and application to immunohistochemistry of human cancer tissues Open
The enzyme spermine oxidase (SMOX) is involved in polyamine catabolism and converts spermine to spermidine. The enzymatic reaction generates reactive hydrogen peroxide and aldehydes as by-products that can damage DNA and other biomolecules…
View article: The CoREST Repressor Complex Mediates Phenotype Switching and Therapy Resistance in Melanoma
The CoREST Repressor Complex Mediates Phenotype Switching and Therapy Resistance in Melanoma Open
Virtually all patients with BRAF-mutant melanoma develop resistance to MAPK inhibitors largely through non-mutational events 1,2 . Although the epigenetic landscape has been shown to be altered in therapy-resistant melanomas and other canc…
View article: <i>Schistosoma mansoni</i>lysine specific demethylase 1 (SmLSD1) is a druggable target involved in parasite survival, oviposition and stem cell proliferation
<i>Schistosoma mansoni</i>lysine specific demethylase 1 (SmLSD1) is a druggable target involved in parasite survival, oviposition and stem cell proliferation Open
Schistosomiasis is a chronically-debilitating neglected tropical disease (NTD) that predominantly affects people living in resource-poor communities of tropical and subtropical countries. Schistosoma mansoni , one of three species responsi…
View article: Inhibiting the coregulator CoREST impairs Foxp3+ Treg function and promotes antitumor immunity
Inhibiting the coregulator CoREST impairs Foxp3+ Treg function and promotes antitumor immunity Open
Foxp3+ Tregs are key to immune homeostasis, but the contributions of various large, multiprotein complexes that regulate gene expression remain unexplored. We analyzed the role in Tregs of the evolutionarily conserved CoREST complex, consi…
View article: Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i> -Mutant Colorectal Cancer
Lysine-Specific Demethylase 1 Mediates AKT Activity and Promotes Epithelial-to-Mesenchymal Transition in <i>PIK3CA</i> -Mutant Colorectal Cancer Open
Activation of the epithelial-to-mesenchymal transition (EMT) program is a critical mechanism for initiating cancer progression and migration. Colorectal cancers contain many genetic and epigenetic alterations that can contribute to EMT. Mu…
View article: Investigation into the use of histone deacetylase inhibitor MS-275 as a topical agent for the prevention and treatment of cutaneous squamous cell carcinoma in an SKH-1 hairless mouse model
Investigation into the use of histone deacetylase inhibitor MS-275 as a topical agent for the prevention and treatment of cutaneous squamous cell carcinoma in an SKH-1 hairless mouse model Open
Cutaneous squamous cell carcinomas are a common form of highly mutated keratinocyte skin cancers that are of particular concern in immunocompromised patients. Here we report on the efficacy of topically applied MS-275, a clinically used hi…
View article: GENE-22. RE-PROGRAMING CHROMATIN WITH A BIFUNCTIONAL LSD1/HDAC INHIBITOR INDUCES THERAPEUTIC DIFFERENTIATION IN DIPG
GENE-22. RE-PROGRAMING CHROMATIN WITH A BIFUNCTIONAL LSD1/HDAC INHIBITOR INDUCES THERAPEUTIC DIFFERENTIATION IN DIPG Open
Diffuse intrinsic high grade glioma (DIPG) is an almost universally fatal tumor of childhood characterized by epigenetic dysregulation driven by somatic H3.3/H3.1 K27M mutations observed in >80% of tumors. We conducted a chromatin-focused …
View article: Lysine-14 acetylation of histone H3 in chromatin confers resistance to the deacetylase and demethylase activities of an epigenetic silencing complex
Lysine-14 acetylation of histone H3 in chromatin confers resistance to the deacetylase and demethylase activities of an epigenetic silencing complex Open
The core CoREST complex (LHC) contains histone deacetylase HDAC1 and histone demethylase LSD1 held together by the scaffold protein CoREST. Here, we analyze the purified LHC with modified peptide and reconstituted semisynthetic mononucleos…
View article: Author response: Lysine-14 acetylation of histone H3 in chromatin confers resistance to the deacetylase and demethylase activities of an epigenetic silencing complex
Author response: Lysine-14 acetylation of histone H3 in chromatin confers resistance to the deacetylase and demethylase activities of an epigenetic silencing complex Open
Article Figures and data Abstract Introduction Results Discussion Materials and methods Data availability References Decision letter Author response Article and author information Metrics Abstract The core CoREST complex (LHC) contains his…