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The potent and selective RIPK2 inhibitor BI 706039 improves intestinal inflammation in the TRUC mouse model of inflammatory bowel disease

Publikováno v: American journal of physiology. Gastrointestinal and liver physiology. 321(5)

Mouse and human data implicate the NOD1 and NOD2 sensors of the intestinal microbiome and the associated signal transduction via the receptor interacting protein kinase 2 (RIPK2) as a potential key signaling node for the development of inflammatory b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::249fa75449d8f623e54320bcf73b527e
https://pubmed.ncbi.nlm.nih.gov/34494462

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No Differences Observed among Multiple Clinical S1P1 Receptor Agonists (Functional Antagonists) in S1P1 Receptor Down-regulation and Degradation

Autor: Lori Patnaude, Anthony J. Slavin, Louise K. Modis, Melissa Hill-Drzewi, Josh Horan, Sokol A. Haxhinasto, Susan Lukas

Publikováno v: SLAS Discovery. 19:407-416

Sphingosine-1-phosphate (S1P) is a bioactive metabolite with pleiotropic effects on multiple cellular processes in health and disease. Responses elicited by S1P are a result of binding to five specific G-protein–coupled receptors. We have developed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b583d75d74f31f9782fc6b7958455925
https://doi.org/10.1177/1087057113502234

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Assessment of Biomarkers of Cardiovascular Risk Among HIV Type 1-Infected Adolescents: Role of Soluble Vascular Cell Adhesion Molecule As an Early Indicator of Endothelial Inflammation

Autor: Bill G. Kapogiannis, John W. Sleasman, William A. Meyer, Salma S. Syed, Rula S. Balluz, Edmond K. Kabagambe, Sharon Nachman, Susan Lukas, Craig M. Wilson

Publikováno v: AIDS Research and Human Retroviruses. 29:493-500

Cardiovascular disease (CVD) biomarkers were examined in a cohort of HIV-infected and HIV-uninfected adolescents who participated in Adolescent Trials Network study 083 utilizing samples from the Reaching for Excellence in Adolescent Care cohort, a l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e32f079fa293048256f43ba9d802f397
https://doi.org/10.1089/aid.2012.0086

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Discovery and Characterization of a Substrate Selective p38α Inhibitor

Autor: Walter Davidson, Scott Jakes, Susan Lukas, Gregory W. Peet, Christopher Pargellis, Roger J. Snow, Rachel R. Kroe, Lee Frego, Mark E. Labadia, Brian Werneburg, Christine A. Grygon

Publikováno v: Biochemistry. 43:11658-11671

A novel inhibitor of p38 mitogen-activated protein kinase (p38), CMPD1, identified by high-throughput screening, is characterized herein. Unlike the p38 inhibitors described previously, this inhibitor is substrate selective and noncompetitive with AT

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d621e78115b26c6a3eff01628a61a09
https://doi.org/10.1021/bi0495073

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Catalysis and Function of the p38α·MK2a Signaling Complex

Autor: Jessi Wildeson, Richard H. Ingraham, Rachel R. Kroe, Christopher Pargellis, Walter Davidson, Lee Frego, Susan Lukas, Mark E. Labadia, Brian Werneburg, Gregory W. Peet

Publikováno v: Biochemistry. 43:9950-9960

The p38 mitogen-activated protein kinase (p38) pathway is required for the production of proinflammatory cytokines (TNFalpha and IL-1) that mediate the chronic inflammatory phases of several autoimmune diseases. Potent p38 inhibitors, such as the slo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40596742c49fc9e629da71fb197ae131
https://doi.org/10.1021/bi049508v

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Discovery of 2-Phenylamino-imidazo[4,5-h]isoquinolin-9-ones: A New Class of Inhibitors of Lck Kinase

Autor: Maret Panzenbeck, Mario G. Cardozo, Robert M. Tolbert, Jeffrey D. Peterson, Susan Lukas, Stephen Jacober, Robert J. Eckner, Gregory W. Peet, Anthony S. Prokopowicz, Carl A. Busacca, Suresh R. Kapadia, Scott Jakes, Tina Morwick, Roger J. Snow, Rosemarie Sellati, Yong Dong, Matt Aaron Tschantz, Neil Moss

Publikováno v: Journal of Medicinal Chemistry. 45:3394-3405

An imidazo[4,5-h]isoquinolin-7,9-dione (1) was identified as an adenosine 5'-triphosphate competitive inhibitor of lck by high throughput screening. Initial structure-activity relationship studies identified the dichlorophenyl ring and the imide NH a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcb66ed0ff6ce36eb079aaec851fb78a
https://doi.org/10.1021/jm020113o

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Carboxymethyl-phenylalanine as a Replacement for Phosphotyrosine in SH2 Domain Binding

Autor: Raj Betageri, John R. Proudfoot, Thomas C. Warren, Susan Lukas, Josephine Schembri-King, Liang Tong, Scott Jakes

Publikováno v: Journal of Biological Chemistry. 273:20238-20242

The crystal structure of human p56lck SH2 domain in complex with an inhibitor containing the singly chargedp-(carboxymethyl)phenylalanine residue (cmF) as a phosphotyrosine (Tyr(P) or pY) replacement has been determined at 1.8 A resolution. The bindi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6fc5b6112295c5916d495df6479ad36
https://doi.org/10.1074/jbc.273.32.20238

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Interaction between the SH2 Domains of ZAP-70 and the Tyrosine-Based Activation Motif 1 Sequence of the ζ Subunit of the T-Cell Receptor

Autor: Daniel J. Greenwood, Thomas C. Warren, Richard H. Ingraham, Mark E. Labadia, Scott Jakes, Susan Lukas, Josephine Schembri-King, Christine A. Grygon

Publikováno v: Archives of Biochemistry and Biophysics. 342:117-125

One of the key steps involved in T-cell activation is binding of the tyrosine kinase ZAP-70 via its two SH2 domains to peptide segments termed tyrosine-based activation motifs (ITAM) which are present in three of the T-cell receptor (TCR) subunits. T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::caacc39690823cac5286ac0d0eaeba6f
https://doi.org/10.1006/abbi.1997.0118

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