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 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
Somatic mutation detection and KRAS amplification in testicular germ cell tumors.
Frontiers In Oncology
Cabral, Eduardo R M ERM; Pacanhella, Marilia F MF; Lengert, Andre V H AVH; Dos Reis, Mariana B MB; Leal, Leticia F LF; de Lima, Marcos A MA; da Silva, Aline L V ALV; Pinto, Icaro A IA; Reis, Rui M RM; Pinto, Mariana T MT; Cárcano, Flavio M FM
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
Pugh, Trevor J TJ; Bell, Jonathan L JL; Bruce, Jeff P JP; Doherty, Gary J GJ; Galvin, Matthew M; Green, Michelle F MF; Hunter-Zinck, Haley H; Kumari, Priti P; Lenoue-Newton, Michele L ML; Li, Marilyn M MM; Lindsay, James J; Mazor, Tali T; Ovalle, Andrea A; Sammut, Stephen-John SJ; Schultz, Nikolaus N; Yu, Thomas V TV; Sweeney, Shawn M SM; Bernard, Brady B; ,
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
Clinical genomic profiling in the management of patients with soft tissue and bone sarcoma.
Nature Communications
Gounder, Mrinal M MM; Agaram, Narasimhan P NP; Trabucco, Sally E SE; Robinson, Victoria V; Ferraro, Richard A RA; Millis, Sherri Z SZ; Krishnan, Anita A; Lee, Jessica J; Attia, Steven S; Abida, Wassim W; Drilon, Alexander A; Chi, Ping P; Angelo, Sandra P D' SP; Dickson, Mark A MA; Keohan, Mary Lou ML; Kelly, Ciara M CM; Agulnik, Mark M; Chawla, Sant P SP; Choy, Edwin E; Chugh, Rashmi R; Meyer, Christian F CF; Myer, Parvathi A PA; Moore, Jessica L JL; Okimoto, Ross A RA; Pollock, Raphael E RE; Ravi, Vinod V; Singh, Arun S AS; Somaiah, Neeta N; Wagner, Andrew J AJ; Healey, John H JH; Frampton, Garrett M GM; Venstrom, Jeffrey M JM; Ross, Jeffrey S JS; Ladanyi, Marc M; Singer, Samuel S; Brennan, Murray F MF; Schwartz, Gary K GK; Lazar, Alexander J AJ; Thomas, David M DM; Maki, Robert G RG; Tap, William D WD; Ali, Siraj M SM; Jin, Dexter X DX
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
Pyronaridine Protects against SARS-CoV-2 Infection in Mouse.
Acs Infectious Diseases
Puhl, Ana C AC; Gomes, Giovanni F GF; Damasceno, Samara S; Godoy, Andre S AS; Noske, Gabriela D GD; Nakamura, Aline M AM; Gawriljuk, Victor O VO; Fernandes, Rafaela S RS; Monakhova, Natalia N; Riabova, Olga O; Lane, Thomas R TR; Makarov, Vadim V; Veras, Flavio P FP; Batah, Sabrina S SS; Fabro, Alexandre T AT; Oliva, Glaucius G; Cunha, Fernando Q FQ; Alves-Filho, José C JC; Cunha, Thiago M TM; Ekins, Sean S
Circulating Tumor DNA Mutations in Progressive Gastrointestinal Stromal Tumors Identify Biomarkers of Treatment Resistance and Uncover Potential Therapeutic Strategies.
Frontiers In Oncology
Ko, Tun Kiat TK; Lee, Elizabeth E; Ng, Cedric Chuan-Young CC; Yang, Valerie Shiwen VS; Farid, Mohamad M; Teh, Bin Tean BT; Chan, Jason Yongsheng JY; Somasundaram, Nagavalli N
Anorectal and Genital Mucosal Melanoma: Diagnostic Challenges, Current Knowledge and Therapeutic Opportunities of Rare Melanomas.
Biomedicines
Ottaviano, Margaret M; Giunta, Emilio Francesco EF; Marandino, Laura L; Tortora, Marianna M; Attademo, Laura L; Bosso, Davide D; Cardalesi, Cinzia C; Fabbrocini, Antonietta A; Rosanova, Mario M; Silvestri, Antonia A; Montella, Liliana L; Tammaro, Pasquale P; Marra, Ester E; Trojaniello, Claudia C; Vitale, Maria Grazia MG; Simeone, Ester E; Troiani, Teresa T; Daniele, Bruno B; Ascierto, Paolo Antonio PA
Anorectal and Genital Mucosal Melanoma: Diagnostic Challenges, Current Knowledge and Therapeutic Opportunities of Rare Melanomas.
Biomedicines
Ottaviano, Margaret M; Giunta, Emilio Francesco EF; Marandino, Laura L; Tortora, Marianna M; Attademo, Laura L; Bosso, Davide D; Cardalesi, Cinzia C; Fabbrocini, Antonietta A; Rosanova, Mario M; Silvestri, Antonia A; Montella, Liliana L; Tammaro, Pasquale P; Marra, Ester E; Trojaniello, Claudia C; Vitale, Maria Grazia MG; Simeone, Ester E; Troiani, Teresa T; Daniele, Bruno B; Ascierto, Paolo Antonio PA
Targeted Therapy of Papillary Thyroid Cancer: A Comprehensive Genomic Analysis.
Frontiers In Endocrinology
Hescheler, Daniel A DA; Riemann, Burkhard B; Hartmann, Milan J M MJM; Michel, Maximilian M; Faust, Michael M; Bruns, Christiane J CJ; Alakus, Hakan H; Chiapponi, Costanza C
Combined Inhibition of AKT and KIT Restores Expression of Programmed Cell Death 4 (PDCD4) in Gastrointestinal Stromal Tumor.
Cancers
Kozinova, Marya M; Joshi, Shalina S; Ye, Shuai S; Belinsky, Martin G MG; Sharipova, Dinara D; Farma, Jeffrey M JM; Reddy, Sanjay S SS; Litwin, Samuel S; Devarajan, Karthik K; Campos, Alex Rosa AR; Yu, Yi Y; Schwartz, Brian B; von Mehren, Margaret M; Rink, Lori L
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
Phosphorylated WNK kinase networks in recoded bacteria recapitulate physiological function.
Cell Reports
Schiapparelli, Paula P; Pirman, Natasha L NL; Mohler, Kyle K; Miranda-Herrera, Pierre A PA; Zarco, Natanael N; Kilic, Onur O; Miller, Chad C; Shah, Sagar R SR; Rogulina, Svetlana S; Hungerford, William W; Abriola, Laura L; Hoyer, Denton D; Turk, Benjamin E BE; Guerrero-Cázares, Hugo H; Isaacs, Farren J FJ; Quiñones-Hinojosa, Alfredo A; Levchenko, Andre A; Rinehart, Jesse J
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
Inhibition of Retinal Ganglion Cell Loss By a Novel ROCK Inhibitor (E212) in Ischemic Optic Nerve Injury Via Antioxidative and Anti-Inflammatory Actions.
Spatially interacting phosphorylation sites and mutations in cancer.
Nature Communications
Huang, Kuan-Lin KL; Scott, Adam D AD; Zhou, Daniel Cui DC; Wang, Liang-Bo LB; Weerasinghe, Amila A; Elmas, Abdulkadir A; Liu, Ruiyang R; Wu, Yige Y; Wendl, Michael C MC; Wyczalkowski, Matthew A MA; Baral, Jessika J; Sengupta, Sohini S; Lai, Chin-Wen CW; Ruggles, Kelly K; Payne, Samuel H SH; Raphael, Benjamin B; Fenyö, David D; Chen, Ken K; Mills, Gordon G; Ding, Li L
Assessment of Clinical Benefit of Integrative Genomic Profiling in Advanced Solid Tumors.
Jama Oncology
Cobain, Erin F EF; Wu, Yi-Mi YM; Vats, Pankaj P; Chugh, Rashmi R; Worden, Francis F; Smith, David C DC; Schuetze, Scott M SM; Zalupski, Mark M MM; Sahai, Vaibhav V; Alva, Ajjai A; Schott, Anne F AF; Caram, Megan E V MEV; Hayes, Daniel F DF; Stoffel, Elena M EM; Jacobs, Michelle F MF; Kumar-Sinha, Chandan C; Cao, Xuhong X; Wang, Rui R; Lucas, David D; Ning, Yu Y; Rabban, Erica E; Bell, Janice J; Camelo-Piragua, Sandra S; Udager, Aaron M AM; Cieslik, Marcin M; Lonigro, Robert J RJ; Kunju, Lakshmi P LP; Robinson, Dan R DR; Talpaz, Moshe M; Chinnaiyan, Arul M AM
Sunitinib-Containing Carborane Pharmacophore with the Ability to Inhibit Tyrosine Kinases Receptors FLT3, KIT and PDGFR-β, Exhibits Powerful In Vivo Anti-Glioblastoma Activity.
Cancers
Alamón, Catalina C; Dávila, Belén B; García, María Fernanda MF; Sánchez, Carina C; Kovacs, Mariángeles M; Trias, Emiliano E; Barbeito, Luis L; Gabay, Martín M; Zeineh, Nidal N; Gavish, Moshe M; Teixidor, Francesc F; Viñas, Clara C; Couto, Marcos M; Cerecetto, Hugo H