Bioorganic & Medicinal Chemistry: Synthesis and SAR of novel capsazepine analogs with significant anti-cancer effects in multiple cancer types

June 1, 2019

JorgeDe La Chapaa, Matthew Valdezb, Franscisco RuizIIIb, Keith Gonzalesb, Wes Mitchellb, Stanton F.McHardybc, Matthew Hartbc, Srikanth R.Polusanib, Cara B.Gonzalesac Abstract We previously demonstrated that capsazepine (CPZ), a synthetic transient receptor potential Vanilloid subtype 1 (TRPV1) antagonist, has significant anti-cancer effects in vivo. The purpose of this study was to develop more potent analogs based upon CPZ pharmacophore and structure-activity relationships (SAR) across analogs. We […]

Journal of Translational Immunology: IL‐1 receptor antagonist, anakinra, prevents myocardial dysfunction in a mouse model of Kawasaki disease vasculitis and myocarditis

May 17, 2019

M. Gorelik  Y. Lee  M. Abe  T. Andrews L. Davis J. Patterson S. Chen T. R. Crother G. J. Aune M. Noval Rivas M. Arditi Summary Kawasaki disease (KD) vasculitis is an acute febrile illness of childhood characterized by systemic vasculitis of unknown origin and is the most common cause of acquired heart disease among children in the United States. While histological […]

Journal of Immunology: Progesterone Receptor Attenuates STAT1-Mediated IFN Signaling in Breast Cancer

May 15, 2019

Merit L Goodman 1 2 3, Gloria M Trinca 1 2 3, Katherine R Walter 1 2 3, Evangelia K Papachristou 4, Clive S D’Santos 4, Tianbao Li 5, Qi Liu 5, Zhao Lai 5 6, Prabhakar Chalise 7, Rashna Madan 8, Fang Fan 8, Mary A Markiewicz 9, Victor X Jin 5, Jason S Carroll 4, Christy R Hagan 10 2 3 Abstract Why some tumors remain indolent and others progress to clinical relevance remains a major unanswered question in cancer biology. IFN signaling in nascent tumors, mediated by STAT1, is a […]

Cell: Proteogenomic analysis of human colon cancer reveals new therapeutic opportunities

May 2, 2019

Author links open overlay panelSuhasVasaikar1214ChenHuang1214XiaojingWang121214Vladislav A.Petyuk314Sara R.Savage414BoWen12YongchaoDou12YunZhang1ZhiaoShi12Osama A.Arshad3Marina A.Gritsenko3Lisa J.Zimmerman5Jason E.McDermott3Therese R.Clauss3Ronald J.Moore3RuiZhao3Matthew E.Monroe3Yi-TingWang3Matthew C.Chambers5Robbert J.C.Slebos5Ken S.Lau6QianxingMo713LiDing8MatthewEllis17MathangiThiagarajan9Christopher R.Kinsinger10HenryRodriguez10Richard D.Smith3Karin D.Rodland31115Daniel C.Liebler515TaoLiu315BingZhang1271516 We performed the first proteogenomic study on a prospectively collected colon cancer cohort. Comparative proteomic and phosphoproteomic analysis of paired tumor and normal adjacent tissues produced a catalog of colon cancer-associated proteins and phosphosites, […]

Molecular Cancer Therapeutics: Prospective Clinical Sequencing of Adult Glioma

May 1, 2019

Siyuan Zheng, Kristin Alfaro-Munoz, Wei Wei, Xiaojing Wang, Fang Wang, Agda Karina Eterovic, Kenna R Mills Shaw, Funda Meric-Bernstam, Gregory N Fuller, Ken Chen, Roel G Verhaak, Gordon B Mills, WK Alfred Yung, Shiao-Pei Weathers, John F de Groot Malignant gliomas are a group of intracranial cancers associated with disproportionately high mortality and morbidity. Here, […]

Molecular Cancer Therapeutics: Prospective Clinical Sequencing of Adult Glioma

May 1, 2019

Siyuan Zheng 1 2 3, Kristin Alfaro-Munoz 4, Wei Wei 5, Xiaojing Wang 3, Fang Wang 6, Agda Karina Eterovic 7, Kenna R Mills Shaw 7, Funda Meric-Bernstam 7, Gregory N Fuller 8, Ken Chen 6, Roel G Verhaak 4 2 6 9, Gordon B Mills 7, W K Alfred Yung 4, Shiao-Pei Weathers 4, John F de Groot 1   Abstract Malignant gliomas are a group of intracranial cancers associated with disproportionately high mortality and morbidity. Here, we report ultradeep targeted sequencing of a prospective cohort of 237 […]

Clinical Cancer Research: Broad Spectrum Activity of the Checkpoint Kinase 1 Inhibitor Prexasertib as a Single Agent or Chemopotentiator Across a Range of Preclinical Pediatric Tumor Models

April 25, 2019

Caitlin D Lowery 1, Michele Dowless 1, Matthew Renschler 1, Wayne Blosser 1, Alle B VanWye 1, Jennifer R Stephens 1, Philip W Iversen 1, Aimee Bence Lin 1, Richard P Beckmann 1, Kateryna Krytska 2, Kristina A Cole 2, John M Maris 2, Douglas S Hawkins 3, Brian P Rubin 4, Raushan T Kurmasheva 5, Peter J Houghton 5, Richard Gorlick 6, E Anders Kolb 7, Min H Kang 8, C Patrick Reynolds 8, Stephen W Erickson 9, Beverly A Teicher 10, Malcolm A Smith 10, Louis F Stancato 11 Abstract Purpose: Checkpoint kinase 1 (CHK1) inhibitors potentiate the DNA-damaging effects of […]

Pediatric Blood & Cancer: Preclinical activity of the antibody‐drug conjugate denintuzumab mafodotin (SGN‐CD19A) against pediatric acute lymphoblastic leukemia xenografts

April 23, 2019

Luke Jones, Hannah McCalmont, Kathryn Evans, Chelsea Mayoh, Raushan T. Kurmasheva, Catherine A. Billups, Peter J. Houghton, Malcolm A. Smith,  Richard B. Lock Abstract Background Denintuzumab mafodotin (SGN‐CD19A) is a CD19‐targeting antibody‐drug conjugate, comprising a monoclonal antibody conjugated to the potent cytotoxin monomethyl auristatin F. Since denintuzumab mafodotin has previously shown activity against B‐cell malignancies in early‐stage clinical trials, it […]

RNA: Antagonism between the RNA-binding protein Musashi1 and miR-137 and its potential impact on neurogenesis and glioblastoma development

April 19, 2019

Mitzli X Velasco, Adam Kosti, Gabriela DA Guardia, Marcia C Santos, Allison Tegge, Mei Qiao, Bruna RS Correa, Greco Hernández, Erzsebet Kokovay, Pedro AF Galante, Luiz OF Penalva Abstract RNA-binding proteins (RBPs) and miRNAs are critical gene expression regulators that interact with one another in cooperative and antagonistic fashions. We identified Musashi1 (Msi1) and miR-137 […]