Results 121 to 130 of about 23,676 (191)

Molecular Basis for Activation to Inhibition Switching in Kv7.2 Channel Modulators

Angewandte Chemie, Volume 138, Issue 42, 12 October 2026.
The paper describes the serendipitous discovery of chemical manipulation allowing the activator‐to‐inhibitor switching in Kv7.2 channel modulators. The molecular determinants driving this switch have been rationalized by multidisciplinary investigation encompassing synthetic and analytical chemistry, in silico methods, cryo‐EM analysis ...
Tania Ciaglia, Giusy Carleo, Zhenni Yang, Francesca Di Matteo, Federica De Rosa, Gerardina Smaldone, Zhao‐Bing Gao, Marco D'Alì, Rita Turcio, Demin Ma, Veronica Di Sarno, Nannan Su, Salvatore Vincenzo Giofrè, Giacomo Pepe, Pietro Campiglia, Alessia Bertamino, Francesco Miceli, Jiangtao Guo, Nunzio Iraci, Carmine Ostacolo, Maurizio Taglialatela   +20 more
wiley   +2 more sources

Translating cardiovascular ion channel and Ca2+ signalling mechanisms into therapeutic insights

The Journal of Physiology, EarlyView.
Abstract figure legend This white paper integrates mechanistic discoveries across ion channel biology, Ca2+ signalling and multiscale cardiovascular physiology to highlight new opportunities for accelerating research and guiding next‐generation therapies. Printed with permission from ®Anita Impagliazzo Medical Illustration. [Correction added on 2 March
Silvia Marchianò, Miguel Martín‐Aragón Baudel, Charlotte E. R. Smith, Gonzalo Hernandez Hernandez, Donald M. Bers, Patrick M. Boyle, Dobromir Dobrev, Shanna Hamilton, Osama F. Harraz, Na Li, Thomas A. Longden, William E. Louch, Madeline Nieves‐Cintron, Matthew A. Nystoriak, Walter Lee Murfee, Przemysław B. Radwański, Swapnil K. Sonkusare, Manuel F. Navedo, Eleonora Grandi   +18 more
wiley   +1 more source

RET receptor tyrosine kinase promotes breast cancer metastasis to the brain and RET inhibitors pralsetinib and selpercatinib suppress breast cancer brain metastases. [PDF]

Cell Death Dis
Regua AT, Bindal S, Najjar MK, Tran PL, Cha J, Shams SS, Lo HW.   +6 more
europepmc   +1 more source

Identification of Crucial Drug Targets and Pathways to Reprogram Drug Resistance Through Epigenetic Modulation in Advanced Lung Cancer Using Integrated Bioinformatics Approach

Computational and Systems Oncology, Volume 6, Issue 1, December 2026.
ABSTRACT Resistance to chemotherapy, which is demonstrated in almost every patient with advanced‐stage lung cancer (ALC), underscores an urgent need to unravel the underlying molecular mechanisms and identify novel strategies to overcome drug resistance. In the present study, an attempt was made to identify epigenetic targets and modulators that can be
Okibur Rahman, Mossammat Rima Akter, Nur Alam   +2 more
wiley   +1 more source

Unraveling A4GALT Mechanism and Its Modulation With Adamantyl‐Galactosylceramide Analogues: Advancing Fabry Disease Therapeutic Strategies

Angewandte Chemie, Volume 138, Issue 41, 5 October 2026.
A 310‐helix‐mediated conformational switch promotes a front‐face SNi‐like catalysis by human A4GALT. Mechanism‐guided design identifies AdaGalCer as a selective modulator of globotriaosylceramide (Gb3) biosynthesis, opening a clear route toward new Fabry disease therapeutics.
Nicky de Koster, Òscar Vidal‐Gironès, Rowan de Graaf, Ken Kok, Lindsey T. Lelieveld, Jackelien Hoogervorst, Maria J. Ferraz, José Pablo Rivas‐Fernández, Rob F. Lammers, Herman S. Overkleeft, Johannes M. F. G. Aerts, Rolf G. Boot, Carme Rovira, Marta Artola   +13 more
wiley   +2 more sources

Landscape of Genomic Mechanisms of Resistance to Selective RET Inhibitors in RET-Altered Solid Tumors: Analysis of the RETgistry Global Consortium. [PDF]

Clin Cancer Res
Waliany S, Cooper AJ, Liu SV, Gautschi O, Rotow JK, Smith KER, Weber UM, Lee DH, Loong HHF, Patel JD, Pennell NA, Nagasaka M, Patel SA, Tan DSW, Solomon BJ, Kim TM, Pall G, Riess JW, Sun L, Früh M, Uy NF, Gadgeel S, Feng J, Do A, Falcon C, Leighl NB, Baik CS, Lai GGY, Ou SI, Cheung KSY, Patil T, Mansfield AS, Weiler D, Yeap BY, Wirth LJ, Gainor JF, Drilon A, Lin JJ.   +37 more
europepmc   +1 more source

Clinical Implementation and Oncological Relevance of Molecular Profiling in Brain Metastases Patients—A Multicenter Retrospective Cohort Study

International Journal of Cancer, Volume 159, Issue 10, Page 2562-2574, 15 November 2026.
While current guidelines recommend the analysis of established cancer driver genes in brain metastases, little is known about its real‐life implementation. This multicenter study revealed an upward trend in the profiling rates of surgically treated brain metastases over the past decade, with up to 60% of brain metastases samples undergoing analysis ...
Maria Nikolaeva, Jacopo Bellomo, Meltem Gönel, Vittorio Stumpo, Victor Egon Staartjes, Flavio Vasella, Kevin Akeret, André Sagerer, Anna Maria Zeitlberger, David Wasilewski, Christopher Krämer, Sven König, Julia Onken, Tareq Juratli, Alexander Köpp, Regina Reimann, Marcus Czabanka, Peter Vajkoczy, Ilker Y. Eyüpoglu, Oliver Bozinov, Michael Weller, Emilie Le Rhun, Luca Regli, Carlo Serra, Marian C. Neidert, Stefanos Voglis   +25 more
wiley   +1 more source

RET Inhibitors in RET Fusion-Positive Lung Cancers: Past, Present, and Future. [PDF]

Drugs
Chen MF, Repetto M, Wilhelm C, Drilon A.
europepmc   +1 more source

ALK and RET Inhibitors Promote HLA Class I Antigen Presentation and Unmask New Antigens within the Tumor Immunopeptidome. [PDF]

Cancer Immunol Res, 2019
Oh CY, Klatt MG, Bourne C, Dao T, Dacek MM, Brea EJ, Mun SS, Chang AY, Korontsvit T, Scheinberg DA.   +9 more
europepmc   +1 more source

Utility of Fine Needle Aspiration Supernatant for Real‐Time PCR–Based Mutation Analysis in Non–Small Cell Lung Cancer

Diagnostic Cytopathology, Volume 54, Issue 11, Page 805-811, November 2026.
ABSTRACT Background The emergence of personalized therapy and molecular sequencing has significantly transformed the management of advanced non–small cell lung carcinoma (NSCLC). Supernatants obtained from fine needle aspiration (FNA) have been shown to be a reliable source of high‐quality nucleic acid for molecular testing.
Adeyinka Akinsanya, Riley Gorden, Madison Rector, Hamna Muhammad, Melissa Randolph, Matt Sperling, Kemin Xu, Sheila Segura, Omer Saeed, Tieying Hou   +9 more
wiley   +1 more source