Results 141 to 150 of about 3,678,790 (312)

Experience from an HTS campaign: Investigation of susceptibility and rescue of SARS-CoV-2 nsp3 protease assay from metal contamination

SLAS Technology
Different biochemical assays yield different rates of false positives than others either due to the nature of the enzyme, the technology associated with the bioassay, or properties of the compounds being screened.
Irene Georgiou, Sandra O’Neill, Colin Robinson, Fraser Cunningham, Sean N. O’Byrne, David Gray, Ian H. Gilbert, Duncan E. Scott   +7 more
doaj   +1 more source

Predictive and prognostic biomarkers of Bacillus Calmette‐Guérin therapy failure in bladder cancer patients: A systematic review

Molecular Oncology, EarlyView.
High‐risk bladder cancer is typically treated with Bacillus Calmette‐Guérin (BCG), but 30–40% of patients relapse. No FDA‐ or CE‐approved biomarkers currently predict or prognosticate BCG failure. We systematically reviewed the literature and identified 72 eligible studies, revealing several promising biomarkers associated with BCG treatment response ...
Rui Ribeiro‐Pereira, Ana Teixeira‐Marques, Rui Freitas, João A Carvalho, Sara Monteiro‐Reis, Giorgio I. Russo, Rui Henrique, Carmen Jerónimo   +7 more
wiley   +1 more source

Reversing T cell dysfunction in a novel in vitro model of T cell exhaustion reveals differential roles of RASA2

Frontiers in Immunology
IntroductionT cell exhaustion driven by chronic antigen stimulation limits durable responses to cancer immunotherapy. Using repeated soluble anti-CD3/anti-CD28 stimulation, we established an in vitro system that recapitulates hallmark exhaustion features
Hilal Saraç, Rachael Nicholson, Rebecca N. Graham, Meera Augustus, Raha Taghavi, Dympna J. Connolly, Lindsay Lim, Sofia Lourenco   +7 more
doaj   +1 more source

Structural diversity of G protein-coupled receptors and significance for drug discovery

, 2008
G protein-coupled receptors (GPCRs) are the largest family of membrane-bound receptors and also the targets of many drugs. Understanding of the functional significance of the wide structural diversity of GPCRs has been aided considerably in recent years ...
Helgi B. Schiöth, Schiöth, Helgi B.,, Malin C. Lagerström, Lagerström, Malin C.,   +3 more
core   +1 more source

SPHINX31 acts as a SRPK1 inhibitor targeting the ATR/DNA‐PKcs/CHK1 replicative checkpoint to inhibit cell growth in non‐small cell lung cancer

Molecular Oncology, EarlyView.
The kinase SRPK1 directly interacts with the protein TOPBP1 and regulates the pre‐mRNA splicing of WIZ thereby contributing to the activation of the ATR/CHK1 replicative checkpoint in response to replicative stress. This allows cancer cells' genomic stability and survival.
Amani Shreim, Aurelie Genoux, Nadiia Zubchuk, Haoyang Zheng, Perla Salameh, Theo Ziegelmeyer, Fabien Dalonneau, Margot Rouchette, Christiane Oddou, Simona Miron, Helene Polveche, Adiilah Mamode Cassim, Carmen Garrido, Eleni Nikolakaki, Didier Auboeuf, Tao Jia, Sophie Zinn‐Justin, Beatrice Eymin   +17 more
wiley   +1 more source

TamGen: drug design with target-aware molecule generation through a chemical language model

Nature Communications
Generative drug design facilitates the creation of compounds effective against pathogenic target proteins. This opens up the potential to discover novel compounds within the vast chemical space and fosters the development of innovative therapeutic ...
Kehan Wu, Yingce Xia, Pan Deng, Renhe Liu, Yuan Zhang, Han Guo, Yumeng Cui, Qizhi Pei, Lijun Wu, Shufang Xie, Si Chen, Xi Lu, Song Hu, Jinzhi Wu, Chi-Kin Chan, Shawn Chen, Liangliang Zhou, Nenghai Yu, Enhong Chen, Haiguang Liu, Jinjiang Guo, Tao Qin, Tie-Yan Liu   +22 more
doaj   +1 more source

Mutant p53R273H disrupts PDPK1 homodimerization and contributes to PDPK1 activation

Molecular Oncology, EarlyView.
How mutant p53R273H drives AKT signaling is unclear. We show that p53R273H, but not wild‐type, directly binds PDPK1 via a mutation‐dependent conformational change. This interaction disrupts inhibitory PDPK1 homodimerization and enhances AKT phosphorylation.
Mei Chee Lim, Alvin Kunyao Guo, Yoko Itahana, Srinivasaraghavan Kannan, Valerie Goh, Mingmin Ong, Terina Yan Wen Tay, Weiying Ye, Sabhashina Radha Krishnan, Jun Nishiyama, Chandra S Verma, Koji Itahana   +11 more
wiley   +1 more source

Recent developments in the application of immobilized artificial membrane (IAM) chromatography to drug discovery

IntroductionImmobilized artificial membrane (IAM) chromatography is widely used in many aspects of drug discovery. It employs stationary phases, which contain phospholipids combining simulation of biological membranes with rapid measurements.Areas ...
Tsantili-Kakoulidou, Anna,, Tsopelas, Fotios,, Vallianatou, Theodosia,   +2 more
core   +1 more source

Targeting the EpCAM‐AXL axis to overcome drug resistance in lung cancer

Molecular Oncology, EarlyView.
Lung cancer cells often evade therapy by hijacking signaling pathways. We reveal that cleaved EpCAM (sEpCAM) stabilizes the oncogenic protein AXL, driving NF‐κB and STAT3‐mediated chemoresistance. This EpCAM‐AXL axis identifies a high‐risk patient subset with poor prognosis.
Alexa Guerrero‐Alba, Mark Shacker, Timothy P. Fleming, Michael A. Smith, Ross M. Bremner, Narendra V. Sankpal   +5 more
wiley   +1 more source

Characterization of therapeutic antibodies targeting lymphatic and vascular resistance factor for the treatment of hypervascularized and highly metastatic cancers

Molecular Oncology, EarlyView.
LVRF (lymphatic and vascular resistance factor) is a VEGFA splice variant upregulated in response to anti‐angiogenic therapy that fosters tumor adaptation through enhanced vascularization, lymphangiogenesis, and metastatic dissemination. Targeting LVRF with fully human neutralizing antibodies disrupts these processes and limits resistant tumor growth ...
Marion David, Arthur Karaulic, Audrey Bennetot, Clémence Fournier, Quentin Odet, Arthur Gouraud, Isabelle Bourget, Cédric Gaggioli, Sandy Giuliano, Frédéric Luciano, Olivier Léger, Zaki Sellam, Gilles Pagès   +12 more
wiley   +1 more source