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Article ; Online: Multicellular Complex Tumor Spheroid Response to DNA Repair Inhibitors in Combination with DNA-damaging Drugs.

Dexheimer, Thomas S / Coussens, Nathan P / Silvers, Thomas / Wright, John / Morris, Joel / Doroshow, James H / Teicher, Beverly A

Cancer research communications

2023 Volume 3, Issue 8, Page(s) 1648–1661

Abstract: Multicellular spheroids comprised of malignant cells, endothelial cells, and mesenchymal stem cells served as an : Significance: Clinical efficacy of DNA-damaging anticancer drugs can be influenced by the DNA damage response in tumor cells. The ... ...

Abstract	Multicellular spheroids comprised of malignant cells, endothelial cells, and mesenchymal stem cells served as an Significance: Clinical efficacy of DNA-damaging anticancer drugs can be influenced by the DNA damage response in tumor cells. The potentiation of DNA-damaging drugs by pharmacologic modulation of DNA repair pathways was assessed in multicellular tumor spheroids. Although most combinations demonstrated additive cytotoxicity, synergistic cytotoxicity was observed for several drug combinations.
MeSH term(s)	Humans ; Temozolomide/pharmacology ; Trabectedin ; Ataxia Telangiectasia ; Endothelial Cells ; Spheroids, Cellular ; Topotecan/pharmacology ; Neoplasms/drug therapy ; DNA Repair ; DNA ; DNA-Activated Protein Kinase
Chemical Substances	Temozolomide (YF1K15M17Y) ; Trabectedin (ID0YZQ2TCP) ; Topotecan (7M7YKX2N15) ; DNA (9007-49-2) ; DNA-Activated Protein Kinase (EC 2.7.11.1)
Language	English
Publishing date	2023-08-25
Publishing country	United States
Document type	Journal Article ; Research Support, N.I.H., Extramural
ISSN	2767-9764
ISSN (online)	2767-9764
DOI	10.1158/2767-9764.CRC-23-0193
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Development of a Cell-Based AlphaLISA Assay for High-Throughput Screening for Small Molecule Proteasome Modulators.

Staerz, Sophia D / Lisabeth, Erika M / Njomen, Evert / Dexheimer, Thomas S / Neubig, Richard R / Tepe, Jetze J

ACS omega

2023 Volume 8, Issue 17, Page(s) 15650–15659

Abstract: 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 takes place ... ...

Abstract	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 takes place through either a ubiquitin-dependent or a ubiquitin-independent proteasomal pathway. The ubiquitin-independent pathway selectively targets unfolded proteins, including intrinsically disordered proteins (IDPs). Dysregulation of proteolysis can lead to the accumulation of IDPs, seen in the pathogenesis of various diseases, including cancer and neurodegeneration. Therefore, the enhancement of the proteolytic activity of the 20S proteasome using small molecules has been identified as a promising pathway to combat IDP accumulation. Currently, there are a limited number of known small molecules that enhance the activity of the 20S proteasome, and few are observed to exhibit enhanced proteasome activity in cell culture. Herein, we describe the development of a high-throughput screening assay to identify cell-permeable proteasome enhancers by utilizing an AlphaLISA platform that measures the degradation of a GFP conjugated intrinsically disordered protein, ornithine decarboxylase (ODC). Through the screening of the Prestwick and NIH Clinical Libraries, a kinase inhibitor, erlotinib, was identified as a new 20S proteasome enhancer, which enhances the degradation of ODC in cells and α-synuclein
Language	English
Publishing date	2023-04-21
Publishing country	United States
Document type	Journal Article
ISSN	2470-1343
ISSN (online)	2470-1343
DOI	10.1021/acsomega.3c01158
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Article: BRAF Inhibitor Resistance Confers Increased Sensitivity to Mitotic Inhibitors.

Misek, Sean A / Foda, Bardees M / Dexheimer, Thomas S / Akram, Maisah / Conrad, Susan E / Schmidt, Jens C / Neubig, Richard R / Gallo, Kathleen A

Frontiers in oncology

2022 Volume 12, Page(s) 766794

Abstract: Single agent and combination therapy with ... ...

Abstract	Single agent and combination therapy with BRAF
Language	English
Publishing date	2022-04-04
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2649216-7
ISSN	2234-943X
ISSN	2234-943X
DOI	10.3389/fonc.2022.766794
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Article ; Online: Two highly related odorant receptors specifically detect α-bile acid pheromones in sea lamprey (

Zhang, Zhe / Zhang, Qinghua / Dexheimer, Thomas S / Ren, Jianfeng / Neubig, Richard R / Li, Weiming

The Journal of biological chemistry

2020 Volume 295, Issue 34, Page(s) 12153–12166

Abstract: Pheromones play critical roles in habitat identification and reproductive behavior synchronization in the sea lamprey ( ...

Abstract	Pheromones play critical roles in habitat identification and reproductive behavior synchronization in the sea lamprey (
MeSH term(s)	Animals ; Cholic Acids/chemistry ; Cholic Acids/pharmacology ; Fish Proteins/biosynthesis ; Fish Proteins/chemistry ; Fish Proteins/genetics ; Lampreys/genetics ; Lampreys/metabolism ; Pheromones/chemistry ; Pheromones/pharmacology ; Receptors, Odorant/biosynthesis ; Receptors, Odorant/chemistry ; Receptors, Odorant/genetics
Chemical Substances	Cholic Acids ; Fish Proteins ; Pheromones ; Receptors, Odorant ; petromyzonol sulfate (3N46RR2Q4E)
Language	English
Publishing date	2020-07-07
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2997-x
ISSN	1083-351X ; 0021-9258
ISSN (online)	1083-351X
ISSN	0021-9258
DOI	10.1074/jbc.RA119.011532
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Article: Inhibition of the Myocardin-Related Transcription Factor Pathway Increases Efficacy of Trametinib in

Appleton, Kathryn M / Palsuledesai, Charuta C / Misek, Sean A / Blake, Maja / Zagorski, Joseph / Gallo, Kathleen A / Dexheimer, Thomas S / Neubig, Richard R

Cancers

2021 Volume 13, Issue 9

Abstract: The Ras/MEK/ERK pathway has been the primary focus of targeted therapies in melanoma; it is aberrantly activated in almost 80% of human cutaneous melanomas (≈50% ...

Abstract	The Ras/MEK/ERK pathway has been the primary focus of targeted therapies in melanoma; it is aberrantly activated in almost 80% of human cutaneous melanomas (≈50%
Language	English
Publishing date	2021-04-22
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527080-1
ISSN	2072-6694
ISSN	2072-6694
DOI	10.3390/cancers13092012
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Article ; Online: Probing the evolutionary conserved residues Y204, F259, S400 and W590 that shape the catalytic groove of human TDP1 for 3'- and 5'-phosphodiester-DNA bond cleavage.

Kiselev, Evgeny / Dexheimer, Thomas S / Marchand, Christophe / Huang, Shar-Yin Naomi / Pommier, Yves

DNA repair

2018 Volume 66-67, Page(s) 64–71

Abstract: Tyrosyl-DNA phosphodiesterase 1 (TDP1) is an ubiquitous DNA repair enzyme present in yeast, plants and animals. It removes a broad range of blocking lesions at the ends of DNA breaks. The catalytic core of TDP1 consists in a pair of conserved histidine- ... ...

Abstract	Tyrosyl-DNA phosphodiesterase 1 (TDP1) is an ubiquitous DNA repair enzyme present in yeast, plants and animals. It removes a broad range of blocking lesions at the ends of DNA breaks. The catalytic core of TDP1 consists in a pair of conserved histidine-lysine-asparagine (HKN) motifs. Analysis of the human TDP1 (hTDP1) crystal structure reveals potential involvement of additional residues that shape the substrate binding site. In this biochemical study, we analyzed four such conserved residues, tyrosine 204 (Y204), phenylalanine 259 (F259), serine 400 (S400) and tryptophan 590 (W590). We show that the F259 residue of hTDP1 is critical for both 3'- and 5'-phosphodiesterase catalysis. We propose that the double π-π interactions of the F259 residue with the -2 and -3 nucleobases serve to position the nucleopeptide substrate in phase with the active site histidines of hTDP1. Mutating Y204 of hTDP1 to phenylalanine (Y204F), as in fly and yeast TDP1 enzymes, had minor impact on TDP1 activity. In constrast, we find that S400 enhances 3'-processing activity while it suppresses 5'-processing activity, thereby promoting specificity for 3'-substrates. W590 is selectively important for 5'-processing. These results reveal the impact of conserved amino acid residues that participate in defining the DNA binding groove around the dual HKN catalytic core motif of TDP1, and their differential roles in facilitating the 3'- vs 5'-end processing activities of hTDP1.
MeSH term(s)	Amino Acid Sequence ; Catalytic Domain ; Conserved Sequence ; DNA/metabolism ; DNA Cleavage ; DNA Damage ; DNA Repair ; Humans ; Phosphoric Diester Hydrolases/chemistry ; Phosphoric Diester Hydrolases/metabolism ; Sequence Alignment
Chemical Substances	DNA (9007-49-2) ; Phosphoric Diester Hydrolases (EC 3.1.4.-) ; TDP1 protein, human (EC 3.1.4.-)
Language	English
Publishing date	2018-05-02
Publishing country	Netherlands
Document type	Journal Article ; Research Support, N.I.H., Intramural
ZDB-ID	2071608-4
ISSN	1568-7856 ; 1568-7864
ISSN (online)	1568-7856
ISSN	1568-7864
DOI	10.1016/j.dnarep.2018.05.001
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Zs.A 5555: Show issues

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Article ; Online: Targeted Investigational Oncology Agents in the NCI-60: A Phenotypic Systems-based Resource.

Molecular cancer therapeutics

2023 Volume 22, Issue 11, Page(s) 1270–1279

Abstract: The NCI-60 human tumor cell line panel has proved to be a useful tool for the global cancer research community in the search for novel chemotherapeutics. The publicly available cell line characterization and compound screening data from the NCI-60 assay ... ...

Abstract	The NCI-60 human tumor cell line panel has proved to be a useful tool for the global cancer research community in the search for novel chemotherapeutics. The publicly available cell line characterization and compound screening data from the NCI-60 assay have significantly contributed to the understanding of cellular mechanisms targeted by new oncology agents. Signature sensitivity/resistance patterns generated for a given chemotherapeutic agent against the NCI-60 panel have long served as fingerprint presentations that encompass target information and the mechanism of action associated with the tested agent. We report the establishment of a new public NCI-60 resource based on the cell line screening of a large and growing set of 175 FDA-approved oncology drugs (AOD) plus >825 clinical and investigational oncology agents (IOA), representing a diverse set (>250) of therapeutic targets and mechanisms. This data resource is available to the public (https://ioa.cancer.gov) and includes the raw data from the screening of the IOA and AOD collection along with an extensive set of visualization and analysis tools to allow for comparative study of individual test compounds and multiple compound sets.
MeSH term(s)	Humans ; Cell Line, Tumor ; Neoplasms/drug therapy ; Neoplasms/pathology ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use
Chemical Substances	Antineoplastic Agents
Language	English
Publishing date	2023-08-07
Publishing country	United States
Document type	Journal Article
ZDB-ID	2063563-1
ISSN	1538-8514 ; 1535-7163
ISSN (online)	1538-8514
ISSN	1535-7163
DOI	10.1158/1535-7163.MCT-23-0267
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Zs.A 5750: Show issues

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Article ; Online: Convergent olfactory trace amine-associated receptors detect biogenic polyamines with distinct motifs via a conserved binding site.

Jia, Liang / Li, Shengju / Dai, Wenxuan / Guo, Lingna / Xu, Zhengrong / Scott, Anne M / Zhang, Zhe / Ren, Jianfeng / Zhang, Qinghua / Dexheimer, Thomas S / Chung-Davidson, Yu-Wen / Neubig, Richard R / Li, Qian / Li, Weiming

The Journal of biological chemistry

2021 Volume 297, Issue 5, Page(s) 101268

Abstract: Biogenic amines activate G-protein-coupled receptors (GPCRs) in the central nervous system in vertebrate animals. Several biogenic amines, when excreted, stimulate trace amine-associated receptors (TAARs), a group of GPCRs in the main olfactory ... ...

Abstract	Biogenic amines activate G-protein-coupled receptors (GPCRs) in the central nervous system in vertebrate animals. Several biogenic amines, when excreted, stimulate trace amine-associated receptors (TAARs), a group of GPCRs in the main olfactory epithelium, and elicit innate behaviors. How TAARs recognize amines with varying numbers of amino groups is largely unknown. We reasoned that a comparison between lamprey and mammalian olfactory TAARs, which are thought to have evolved independently but show convergent responses to polyamines, may reveal structural determinants of amine recognition. Here, we demonstrate that sea lamprey TAAR365 (sTAAR365) responds strongly to biogenic polyamines cadaverine, putrescine, and spermine, and shares a similar response profile as a mammalian TAAR (mTAAR9). Docking and site-directed mutagenesis analyses show that both sTAAR365 and mTAAR9 recognize the two amino groups of cadaverine with the conserved Asp
MeSH term(s)	Amino Acid Motifs ; Animals ; Binding Sites ; Biogenic Polyamines/chemistry ; Fish Proteins/chemistry ; Fish Proteins/genetics ; Fish Proteins/metabolism ; HEK293 Cells ; Humans ; Lampreys ; Mice ; Molecular Docking Simulation ; Mutagenesis, Site-Directed ; Receptors, Odorant/chemistry ; Receptors, Odorant/genetics ; Receptors, Odorant/metabolism
Chemical Substances	Biogenic Polyamines ; Fish Proteins ; Receptors, Odorant
Language	English
Publishing date	2021-09-30
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2997-x
ISSN	1083-351X ; 0021-9258
ISSN (online)	1083-351X
ISSN	0021-9258
DOI	10.1016/j.jbc.2021.101268
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Article ; Online: Feedback at the Point of Care to Decrease Medication Alert Rates in an Electronic Health Record.

van Camp, P J / Kirkendall, Eric S / Hagedorn, Philip A / Minich, Thomas / Kouril, Michal / Spooner, S Andrew / Gecili, Emrah / Dexheimer, Judith W

Pediatric emergency care

2019 Volume 36, Issue 7, Page(s) e417–e422

Abstract: Frequently overridden alerts in the electronic health record can highlight alerts that may need revision. This method is a way of fine-tuning clinical decision support. We evaluated the feasibility of a complementary, yet different method that directly ... ...

Abstract	Frequently overridden alerts in the electronic health record can highlight alerts that may need revision. This method is a way of fine-tuning clinical decision support. We evaluated the feasibility of a complementary, yet different method that directly involved pediatric emergency department (PED) providers in identifying additional medication alerts that were potentially incorrect or intrusive. We then evaluated the effect subsequent resulting modifications had on alert salience. Methods: We performed a prospective, interventional study over 34 months (March 6, 2014, to December 31, 2016) in the PED. We implemented a passive alert feedback mechanism by enhancing the native electronic health record functionality on alert reviews. End-users flagged potentially incorrect/bothersome alerts for review by the study's team. The alerts were updated when clinically appropriate and trends of the impact were evaluated. Results: More than 200 alerts were reported from both inside and outside the PED, suggesting an intuitive approach. On average, we processed 4 reviews per week from the PED, with attending physicians as major contributors. The general trend of the impact of these changes seems favorable. Discussion: The implementation of the review mechanism for user-selected alerts was intuitive and sustainable and seems to be able to detect alerts that are bothersome to the end-users. The method should be run in parallel with the traditional data-driven approach to support capturing of inaccurate alerts. Conclusions: User-centered, context-specific alert feedback can be used for selecting suboptimal, interruptive medication alerts.
MeSH term(s)	Child ; Decision Support Systems, Clinical ; Drug-Related Side Effects and Adverse Reactions/prevention & control ; Electronic Health Records ; Emergency Service, Hospital ; Feasibility Studies ; Feedback ; Humans ; Medical Order Entry Systems ; Medication Errors/prevention & control ; Point-of-Care Systems ; Prospective Studies ; Reminder Systems
Language	English
Publishing date	2019-05-27
Publishing country	United States
Document type	Journal Article
ZDB-ID	632588-9
ISSN	1535-1815 ; 0749-5161
ISSN (online)	1535-1815
ISSN	0749-5161
DOI	10.1097/PEC.0000000000001847
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Zs.A 2083: Show issues

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Article ; Online: Identifying chemopreventive agents for obesity-associated cancers using an efficient, 3D high-throughput transformation assay.

Benham, Vanessa / Bullard, Blair / Dexheimer, Thomas S / Bernard, Matthew P / Neubig, Richard R / Liby, Karen T / Bernard, Jamie J

Scientific reports

2019 Volume 9, Issue 1, Page(s) 10278

Abstract: Obesity is associated with ~40% of cancer diagnoses but there are currently no effective preventive strategies, illustrating a need for chemoprevention. We previously demonstrated that fibroblast growth factor 2 (FGF2) from adipose tissue stimulates ... ...

Abstract	Obesity is associated with ~40% of cancer diagnoses but there are currently no effective preventive strategies, illustrating a need for chemoprevention. We previously demonstrated that fibroblast growth factor 2 (FGF2) from adipose tissue stimulates malignant transformation, as measured by growth in soft agar, the gold-standard in vitro transformation assay. Because the soft agar assay is unsuitable for high throughput screens (HTS), we developed a novel method using 3D growth in ultra-low attachment conditions as an alternative to growth in agar to discover compounds that inhibit transformation. Treating non-tumorigenic, skin epithelial JB6 P
MeSH term(s)	Animals ; Antineoplastic Agents/pharmacology ; Cell Culture Techniques ; Cell Proliferation/drug effects ; Cell Transformation, Neoplastic/drug effects ; Drug Screening Assays, Antitumor/methods ; Fibroblast Growth Factor 2/pharmacology ; Fibroblasts/cytology ; Fibroblasts/drug effects ; Fluvastatin/pharmacology ; High-Throughput Screening Assays ; Humans ; Mice ; Models, Biological ; Neoplasms/prevention & control ; Obesity/complications ; Obesity/metabolism ; Podophyllotoxin/analogs & derivatives ; Podophyllotoxin/pharmacology ; Skin/cytology ; Skin/drug effects
Chemical Substances	Antineoplastic Agents ; picropodophyllin (0F35AOI227) ; Fibroblast Growth Factor 2 (103107-01-3) ; Fluvastatin (4L066368AS) ; Podophyllotoxin (L36H50F353)
Language	English
Publishing date	2019-07-16
Publishing country	England
Document type	Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
ZDB-ID	2615211-3
ISSN	2045-2322 ; 2045-2322
ISSN (online)	2045-2322
ISSN	2045-2322
DOI	10.1038/s41598-019-46531-y
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