Characterization of p38α autophosphorylation inhibitors that target the non-canonical activation pathway.
Nature Communications
González, Lorena L; Díaz, Lucía L; Pous, Joan J; Baginski, Blazej B; Duran-Corbera, Anna A; Scarpa, Margherita M; Brun-Heath, Isabelle I; Igea, Ana A; Martin-Malpartida, Pau P; Ruiz, Lidia L; Pallara, Chiara C; Esguerra, Mauricio M; Colizzi, Francesco F; Mayor-Ruiz, Cristina C; Biondi, Ricardo M RM; Soliva, Robert R; Macias, Maria J MJ; Orozco, Modesto M; Nebreda, Angel R AR
Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective.
Acs Chemical Neuroscience
Ong, Han Wee HW; Liang, Yi Y; Richardson, William W; Lowry, Emily R ER; Wells, Carrow I CI; Chen, Xiangrong X; Silvestre, Margaux M; Dempster, Kelvin K; Silvaroli, Josie A JA; Smith, Jeffery L JL; Wichterle, Hynek H; Pabla, Navjot S NS; Ultanir, Sila K SK; Bullock, Alex N AN; Drewry, David H DH; Axtman, Alison D AD
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones.
Journal Of Medicinal Chemistry
Harnden, Alice C AC; Davis, Owen A OA; Box, Gary M GM; Hayes, Angela A; Johnson, Louise D LD; Henley, Alan T AT; de Haven Brandon, Alexis K AK; Valenti, Melanie M; Cheung, Kwai-Ming J KJ; Brennan, Alfie A; Huckvale, Rosemary R; Pierrat, Olivier A OA; Talbot, Rachel R; Bright, Michael D MD; Akpinar, Hafize Aysin HA; Miller, Daniel S J DSJ; Tarantino, Dalia D; Gowan, Sharon S; de Klerk, Selby S; McAndrew, Peter Craig PC; Le Bihan, Yann-Vaï YV; Meniconi, Mirco M; Burke, Rosemary R; Kirkin, Vladimir V; van Montfort, Rob L M RLM; Raynaud, Florence I FI; Rossanese, Olivia W OW; Bellenie, Benjamin R BR; Hoelder, Swen S
Investigation of the anti-tumor mechanism of tirabrutinib, a highly selective Bruton's tyrosine kinase inhibitor, by phosphoproteomics and transcriptomics.
Clinical outcome of Brazilian patients with non-small cell lung cancer in early stage harboring rare mutations in epidermal growth factor receptor.
Brazilian Journal Of Medical And Biological Research = Revista Brasileira De Pesquisas Medicas E Biologicas
Machado-Rugolo, J J; Baldavira, C M CM; Prieto, T G TG; Olivieri, E H R EHR; Fabro, A T AT; Rainho, C A CA; Castelli, E C EC; Ribolla, P E M PEM; Ab'Saber, A M AM; Takagaki, T T; Nagai, M A MA; Capelozzi, V L VL
VIP152 is a selective CDK9 inhibitor with pre-clinical in vitro and in vivo efficacy in chronic lymphocytic leukemia.
Leukemia
Sher, Steven S; Whipp, Ethan E; Walker, Janek J; Zhang, Pu P; Beaver, Larry L; Williams, Katie K; Orwick, Shelley S; Ravikrishnan, Janani J; Walker, Brandi B; Perry, Elizabeth E; Gregory, Charles C; Purcell, Matthew M; Pan, Alexander A; Yan, Pearlly P; Alinari, Lapo L; Johnson, Amy J AJ; Frigault, Melanie M MM; Greer, Joy M JM; Hamdy, Ahmed A; Izumi, Raquel R; Mo, Xiaokui X; Sampath, Deepa D; Woyach, Jennifer J; Blachly, James J; Byrd, John C JC; Lapalombella, Rosa R
Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
Acs Medicinal Chemistry Letters
Hall, Adrian A; Abendroth, Jan J; Bolejack, Madison J MJ; Ceska, Tom T; Dell'Aiera, Sylvie S; Ellis, Victoria V; Fox, David D; François, Cyril C; Muruthi, Muigai M MM; Prével, Camille C; Poullennec, Karine K; Romanov, Sergei S; Valade, Anne A; Vanbellinghen, Alain A; Yano, Jason J; Geraerts, Martine M
Reengineering Ponatinib to Minimize Cardiovascular Toxicity.
Cancer Research
Hnatiuk, Anna P AP; Bruyneel, Arne A N AAN; Tailor, Dhanir D; Pandrala, Mallesh M; Dheeraj, Arpit A; Li, Wenqi W; Serrano, Ricardo R; Feyen, Dries A M DAM; Vu, Michelle M MM; Amatya, Prashila P; Gupta, Saloni S; Nakauchi, Yusuke Y; Morgado, Isabel I; Wiebking, Volker V; Liao, Ronglih R; Porteus, Matthew H MH; Majeti, Ravindra R; Malhotra, Sanjay V SV; Mercola, Mark M
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo.
Journal Of Medicinal Chemistry
Huckvale, Rosemary R; Harnden, Alice C AC; Cheung, Kwai-Ming J KJ; Pierrat, Olivier A OA; Talbot, Rachel R; Box, Gary M GM; Henley, Alan T AT; de Haven Brandon, Alexis K AK; Hallsworth, Albert E AE; Bright, Michael D MD; Akpinar, Hafize Aysin HA; Miller, Daniel S J DSJ; Tarantino, Dalia D; Gowan, Sharon S; Hayes, Angela A; Gunnell, Emma A EA; Brennan, Alfie A; Davis, Owen A OA; Johnson, Louise D LD; de Klerk, Selby S; McAndrew, Craig C; Le Bihan, Yann-Vaï YV; Meniconi, Mirco M; Burke, Rosemary R; Kirkin, Vladimir V; van Montfort, Rob L M RLM; Raynaud, Florence I FI; Rossanese, Olivia W OW; Bellenie, Benjamin R BR; Hoelder, Swen S
Clinical Utility of Plasma-Based Comprehensive Molecular Profiling in Advanced Non-Small-Cell Lung Cancer.
Jco Precision Oncology
Schouten, Robert D RD; Vessies, Daan C L DCL; Bosch, Linda J W LJW; Barlo, Nicole P NP; van Lindert, Anne S R ASR; Cillessen, Saskia A G M SAGM; van den Broek, Daan D; van den Heuvel, Michel M MM; Monkhorst, Kim K
Clinical Utility of Plasma-Based Comprehensive Molecular Profiling in Advanced Non-Small-Cell Lung Cancer.
Jco Precision Oncology
Schouten, Robert D RD; Vessies, Daan C L DCL; Bosch, Linda J W LJW; Barlo, Nicole P NP; van Lindert, Anne S R ASR; Cillessen, Saskia A G M SAGM; van den Broek, Daan D; van den Heuvel, Michel M MM; Monkhorst, Kim K
Structure-based classification predicts drug response in EGFR-mutant NSCLC.
Nature
Robichaux, Jacqulyne P JP; Le, Xiuning X; Vijayan, R S K RSK; Hicks, J Kevin JK; Heeke, Simon S; Elamin, Yasir Y YY; Lin, Heather Y HY; Udagawa, Hibiki H; Skoulidis, Ferdinandos F; Tran, Hai H; Varghese, Susan S; He, Junqin J; Zhang, Fahao F; Nilsson, Monique B MB; Hu, Lemei L; Poteete, Alissa A; Rinsurongkawong, Waree W; Zhang, Xiaoshan X; Ren, Chenghui C; Liu, Xiaoke X; Hong, Lingzhi L; Zhang, Jianjun J; Diao, Lixia L; Madison, Russell R; Schrock, Alexa B AB; Saam, Jennifer J; Raymond, Victoria V; Fang, Bingliang B; Wang, Jing J; Ha, Min Jin MJ; Cross, Jason B JB; Gray, Jhanelle E JE; Heymach, John V JV
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.
Journal Of Medicinal Chemistry
Henderson, Scott H SH; Sorrell, Fiona F; Bennett, James J; Fedorov, Oleg O; Hanley, Marcus T MT; Godoi, Paulo H PH; Ruela de Sousa, Roberta R; Robinson, Sean S; Ashall-Kelly, Alexander A; Hopkins Navratilova, Iva I; Walter, Daryl S DS; Elkins, Jonathan M JM; Ward, Simon E SE
A Nationwide Study on the Impact of Routine Testing for EGFR Mutations in Advanced NSCLC Reveals Distinct Survival Patterns Based on EGFR Mutation Subclasses.
Cancers
Koopman, Bart B; Cajiao Garcia, Betzabel N BN; Kuijpers, Chantal C H J CCHJ; Damhuis, Ronald A M RAM; van der Wekken, Anthonie J AJ; Groen, Harry J M HJM; Schuuring, Ed E; Willems, Stefan M SM; van Kempen, Léon C LC
Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes.
Journal Of Medicinal Chemistry
Eduful, Benjamin J BJ; O'Byrne, Sean N SN; Temme, Louisa L; Asquith, Christopher R M CRM; Liang, Yi Y; Picado, Alfredo A; Pilotte, Joseph R JR; Hossain, Mohammad Anwar MA; Wells, Carrow I CI; Zuercher, William J WJ; Catta-Preta, Carolina M C CMC; Zonzini Ramos, Priscila P; Santiago, André de S AS; Couñago, Rafael M RM; Langendorf, Christopher G CG; Nay, Kévin K; Oakhill, Jonathan S JS; Pulliam, Thomas L TL; Lin, Chenchu C; Awad, Dominik D; Willson, Timothy M TM; Frigo, Daniel E DE; Scott, John W JW; Drewry, David H DH
Longitudinal multi-gene panel assessment of circulating tumor DNA revealed tumor burden and molecular characteristics along treatment course of non-small cell lung cancer.
Translational Lung Cancer Research
Ho, Gloria Y F GYF; Wang, Tao T; Kwok, Hoi-Hin HH; Rasul, Rehana R; Peila, Rita R; Guzman, Maria M; Ip, Mary S M MSM; Lam, David C L DCL
Efficacy of afatinib for pulmonary adenocarcinoma with leptomeningeal metastases harboring an epidermal growth factor receptor complex mutation (exon 19del+K754E): A case report.
Medicine
Ma, Chunhua C; Liu, Mei M; Mu, Ning N; Li, Jinduo J; Li, Lin L; Jiang, Rong R
Mutation and drug-specific intracellular accumulation of EGFR predict clinical responses to tyrosine kinase inhibitors.
Ebiomedicine
de Wit, Maurice M; Gao, Ya Y; Mercieca, Darlene D; de Heer, Iris I; Valkenburg, Bart B; van Royen, Martin E ME; Aerts, Joachim J; Sillevis Smitt, Peter P; French, Pim P
Identifying a wide range of actionable variants using capture-based ultra-deep targeted sequencing in treatment-naive patients with primary lung adenocarcinoma.
International Journal Of Clinical And Experimental Pathology
Chen, Lingfeng L; Chen, Minyan M; Lin, Jie J; Chen, Xiaoyan X; Yu, Xunbin X; Chen, Zhizhong Z; Jin, Long L
Rapid EGFR mutation testing in lung cancer tissue samples using a fully automated system and single-use cartridge.
Practical Laboratory Medicine
Al-Turkmani, M Rabie MR; Suriawinata, Michael A MA; Deharvengt, Sophie J SJ; Green, Donald C DC; Black, Candice C CC; Shirai, Keisuke K; Dragnev, Konstantin H KH; Tsongalis, Gregory J GJ
Results of Liquid Biopsy Studies by Next Generation Sequencing in Patients with Advanced Stage Non-small Cell Lung Cancer: Single Center Experience from Turkey.
Balkan Journal Of Medical Genetics : Bjmg
Buyuksimsek, M M; Togun, M M; Oguz, Kara I KI; Bisgin, A A; Boga, I I; Tohumcuoglu, M M; Ogul, A A; Evren, Yetisir A YA; Sahin, B B; Erdem, Sumbul H SH; Mirili, C C
High concordance of EGFR mutation status between sputum and corresponding tissue specimens of late-stage lung cancers using amplification refractory mutation system-PCR.
International Journal Of Clinical And Experimental Pathology
Su, Fei F; Fu, Yiyun Y; Wu, Qian Q; Zheng, Ke K; Tang, Yuan Y; Su, Xueying X; Wang, Ye Y; Jiang, Lili L
Potential mechanism of primary resistance to icotinib in patients with advanced non-small cell lung cancer harboring uncommon mutant epidermal growth factor receptor: A multi-center study.
Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK).
Molecules (Basel, Switzerland)
Asquith, Christopher R M CRM; Bennett, James M JM; Su, Lianyong L; Laitinen, Tuomo T; Elkins, Jonathan M JM; Pickett, Julie E JE; Wells, Carrow I CI; Li, Zengbiao Z; Willson, Timothy M TM; Zuercher, William J WJ