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.
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
A High Percentage of NSCLC With Germline CHEK2 Mutation Harbors Actionable Driver Alterations: Survey of a Cancer Genomic Database and Review of Literature.
Jto Clinical And Research Reports
Zhang, Shannon S SS; Lee, Jessica K JK; Tukachinsky, Hanna H; Schrock, Alexa B AB; Nagasaka, Misako M; Ou, Sai-Hong Ignatius SI
Comprehensive characterization of genomic and radiologic features reveals distinct driver patterns of RTK/RAS pathway in ground-glass opacity pulmonary nodules.
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
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
Validation of ctDNA Quality Control Materials Through a Precompetitive Collaboration of the Foundation for the National Institutes of Health.
Jco Precision Oncology
Williams, P Mickey PM; Forbes, Thomas T; P Lund, Steven S; Cole, Kenneth D KD; He, Hua-Jun HJ; Karlovich, Chris C; Paweletz, Cloud P CP; Stetson, Daniel D; Yee, Laura M LM; Connors, Dana E DE; Keating, Susan M SM; Destenaves, Benoit B; Cleveland, Megan H MH; Lau, Christie J CJ; Barrett, J Carl JC; Kelloff, Gary J GJ; McCormack, Robert T RT
Molecular characterization of advanced non-small cell lung cancer patients by cfDNA analysis: experience from routine laboratory practice.
Journal Of Thoracic Disease
González de Aledo-Castillo, José Manuel JM; Arcocha, Ainara A; Victoria, Iván I; Martinez-Puchol, Ana Isabel AI; Sánchez, Cristina C; Jares, Pedro P; Rodríguez, Gabriel Felipe GF; Viñolas, Núria N; Reyes, Roxana R; Reguart, Noemí N; Puig-Butillé, Joan Antón JA
[Different Gene Mutation Spectrum of the Paired CSF and Plasma Samples in Lung Adenocarcinoma with Leptomeningeal Metastases: the Liquid Biopsy Based on Circulating Tumor DNA].
Zhongguo Fei Ai Za Zhi = Chinese Journal Of Lung Cancer
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
Analysis of Predictive Biomarkers in Patients With Lung Adenocarcinoma From Southern Brazil Reveals a Distinct Profile From Other Regions of the Country.
Journal Of Global Oncology
Andreis, Tiago F TF; Correa, Bruno S BS; Vianna, Fernanda S FS; De-Paris, Fernanda F; Siebert, Marina M; Leistner-Segal, Sandra S; Hahn, Eriza C EC; Ulbrich, Jane M JM; Rivero, Luis F R LFR; De Oliveira, Francine H FH; Lorandi, Vinícius V; Ashton-Prolla, Patricia P; Macedo, Gabriel S GS
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.
Acs Medicinal Chemistry Letters
Harris, Philip A PA; Marinis, Jill M JM; Lich, John D JD; Berger, Scott B SB; Chirala, Anirudh A; Cox, Julie A JA; Eidam, Patrick M PM; Finger, Joshua N JN; Gough, Peter J PJ; Jeong, Jae U JU; Kang, James J; Kasparcova, Viera V; Leister, Lara K LK; Mahajan, Mukesh K MK; Miller, George G; Nagilla, Rakesh R; Ouellette, Michael T MT; Reilly, Michael A MA; Rendina, Alan R AR; Rivera, Elizabeth J EJ; Sun, Helen H HH; Thorpe, James H JH; Totoritis, Rachel D RD; Wang, Wei W; Wu, Dongling D; Zhang, Daohua D; Bertin, John J; Marquis, Robert W RW
RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Cell Death And Differentiation
Patel, Snahel S; Webster, Joshua D JD; Varfolomeev, Eugene E; Kwon, Youngsu C YC; Cheng, Jason H JH; Zhang, Juan J; Dugger, Debra L DL; Wickliffe, Kate E KE; Maltzman, Allie A; Sujatha-Bhaskar, Swathi S; Bir Kohli, Pawan P; Ramaswamy, Sreema S; Deshmukh, Gauri G; Liederer, Bianca M BM; Fong, Rina R; Hamilton, Greg G; Lupardus, Patrick P; Caplazi, Patrick P; Lee, Wyne P WP; van Lookeren Campagne, Menno M; Johnson, Adam A; McKenzie, Brent S BS; Junttila, Melissa R MR; Newton, Kim K; Vucic, Domagoj D
On-target Resistance to the Mutant-Selective EGFR Inhibitor Osimertinib Can Develop in an Allele-Specific Manner Dependent on the Original EGFR-Activating Mutation.
Clinical Cancer Research : An Official Journal Of The American Association For Cancer Research
Brown, Benjamin P BP; Zhang, Yun-Kai YK; Westover, David D; Yan, Yingjun Y; Qiao, Huan H; Huang, Vincent V; Du, Zhenfang Z; Smith, Jarrod A JA; Ross, Jeffrey S JS; Miller, Vincent A VA; Ali, Siraj S; Bazhenova, Lyudmila L; Schrock, Alexa B AB; Meiler, Jens J; Lovly, Christine M CM
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Proceedings Of The National Academy Of Sciences Of The United States Of America
Hillig, Roman C RC; Sautier, Brice B; Schroeder, Jens J; Moosmayer, Dieter D; Hilpmann, André A; Stegmann, Christian M CM; Werbeck, Nicolas D ND; Briem, Hans H; Boemer, Ulf U; Weiske, Joerg J; Badock, Volker V; Mastouri, Julia J; Petersen, Kirstin K; Siemeister, Gerhard G; Kahmann, Jan D JD; Wegener, Dennis D; Böhnke, Niels N; Eis, Knut K; Graham, Keith K; Wortmann, Lars L; von Nussbaum, Franz F; Bader, Benjamin B
DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome.
Acs Chemical Biology
Richter, Hans H; Satz, Alexander L AL; Bedoucha, Marc M; Buettelmann, Bernd B; Petersen, Ann C AC; Harmeier, Anja A; Hermosilla, Ricardo R; Hochstrasser, Remo R; Burger, Dominique D; Gsell, Bernard B; Gasser, Rodolfo R; Huber, Sylwia S; Hug, Melanie N MN; Kocer, Buelent B; Kuhn, Bernd B; Ritter, Martin M; Rudolph, Markus G MG; Weibel, Franziska F; Molina-David, Judith J; Kim, Jin-Ju JJ; Santos, Javier Varona JV; Stihle, Martine M; Georges, Guy J GJ; Bonfil, R Daniel RD; Fridman, Rafael R; Uhles, Sabine S; Moll, Solange S; Faul, Christian C; Fornoni, Alessia A; Prunotto, Marco M
The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models.
Oncotarget
Kim, Sunkyu S; Tiedt, Ralph R; Loo, Alice A; Horn, Thomas T; Delach, Scott S; Kovats, Steven S; Haas, Kristy K; Engstler, Barbara Schacher BS; Cao, Alexander A; Pinzon-Ortiz, Maria M; Mulford, Iain I; Acker, Michael G MG; Chopra, Rajiv R; Brain, Christopher C; di Tomaso, Emmanuelle E; Sellers, William R WR; Caponigro, Giordano G
Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors.
Nature Communications
Fassunke, Jana J; Müller, Fabienne F; Keul, Marina M; Michels, Sebastian S; Dammert, Marcel A MA; Schmitt, Anna A; Plenker, Dennis D; Lategahn, Jonas J; Heydt, Carina C; Brägelmann, Johannes J; Tumbrink, Hannah L HL; Alber, Yannic Y; Klein, Sebastian S; Heimsoeth, Alena A; Dahmen, Ilona I; Fischer, Rieke N RN; Scheffler, Matthias M; Ihle, Michaela A MA; Priesner, Vanessa V; Scheel, Andreas H AH; Wagener, Svenja S; Kron, Anna A; Frank, Konrad K; Garbert, Katia K; Persigehl, Thorsten T; Püsken, Michael M; Haneder, Stefan S; Schaaf, Bernhard B; Rodermann, Ernst E; Engel-Riedel, Walburga W; Felip, Enriqueta E; Smit, Egbert F EF; Merkelbach-Bruse, Sabine S; Reinhardt, H Christian HC; Kast, Stefan M SM; Wolf, Jürgen J; Rauh, Daniel D; Büttner, Reinhard R; Sos, Martin L ML
Identification of a novel ATM inhibitor with cancer cell specific radiosensitization activity.
Oncotarget
Dohmen, Amy J C AJC; Qiao, Xiaohang X; Duursma, Anja A; Wijdeven, Ruud H RH; Lieftink, Cor C; Hageman, Floor F; Morris, Ben B; Halonen, Pasi P; Vens, Conchita C; van den Brekel, Michiel W M MWM; Ovaa, Huib H; Neefjes, Jacques J; Zuur, Charlotte L CL
Identification of 4-phenylquinolin-2(1H)-one as a specific allosteric inhibitor of Akt.
Scientific Reports
Huang, Bill X BX; Newcomer, Kenny K; Kevala, Karl K; Barnaeva, Elena E; Zheng, Wei W; Hu, Xin X; Patnaik, Samarjit S; Southall, Noel N; Marugan, Juan J; Ferrer, Marc M; Kim, Hee-Yong HY
A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin.
Cell Reports
Mujahid, Nisma N; Liang, Yanke Y; Murakami, Ryo R; Choi, Hwan Geun HG; Dobry, Allison S AS; Wang, Jinhua J; Suita, Yusuke Y; Weng, Qing Yu QY; Allouche, Jennifer J; Kemeny, Lajos V LV; Hermann, Andrea L AL; Roider, Elisabeth M EM; Gray, Nathanael S NS; Fisher, David E DE