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
Assessing variants of uncertain significance implicated in hearing loss using a comprehensive deafness proteome.
Human Genetics
Tollefson, Mallory R MR; Gogal, Rose A RA; Weaver, A Monique AM; Schaefer, Amanda M AM; Marini, Robert J RJ; Azaiez, Hela H; Kolbe, Diana L DL; Wang, Donghong D; Weaver, Amy E AE; Casavant, Thomas L TL; Braun, Terry A TA; Smith, Richard J H RJH; Schnieders, Michael J MJ
Publication Date: 2023-04-22
Variant appearance in text: FGFR3: 2089G>T; Gly697Cys
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
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
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
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
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
Induction of Lysosome Membrane Permeabilization as a Therapeutic Strategy to Target Pancreatic Cancer Stem Cells.
Cancers
Cash, Timothy P TP; Alcalá, Sonia S; Rico-Ferreira, María Del Rosario MDR; Hernández-Encinas, Elena E; García, Jennifer J; Albarrán, María Isabel MI; Valle, Sandra S; Muñoz, Javier J; Martínez-González, Sonia S; Blanco-Aparicio, Carmen C; Pastor, Joaquín J; Serrano, Manuel M; Sainz, Bruno B
Identification of targeted therapy options for gastric adenocarcinoma by comprehensive analysis of genomic data.
Gastric Cancer : Official Journal Of The International Gastric Cancer Association And The Japanese Gastric Cancer Association
Hescheler, Daniel A DA; Plum, Patrick S PS; Zander, Thomas T; Quaas, Alexander A; Korenkov, Michael M; Gassa, Asmae A; Michel, Maximilian M; Bruns, Christiane J CJ; Alakus, Hakan H
Development and validation of a targeted gene sequencing panel for application to disparate cancers.
Scientific Reports
McCabe, Mark J MJ; Gauthier, Marie-Emilie A MA; Chan, Chia-Ling CL; Thompson, Tanya J TJ; De Sousa, Sunita M C SMC; Puttick, Clare C; Grady, John P JP; Gayevskiy, Velimir V; Tao, Jiang J; Ying, Kevin K; Cipponi, Arcadi A; Deng, Niantao N; Swarbrick, Alex A; Thomas, Melissa L ML; Lord, Reginald V RV; Johns, Amber L AL; Kohonen-Corish, Maija M; O'Toole, Sandra A SA; Clark, Jonathan J; Mueller, Simon A SA; Gupta, Ruta R; McCormack, Ann I AI; Dinger, Marcel E ME; Cowley, Mark J MJ; ,
Identification of New Mono/Dihydroxynaphthoquinone as Lead Agents That Inhibit the Growth of Refractive and Triple-Negative Breast Cancer Cell Lines.
Acs Omega
Schroeder, Richard R; Sfondouris, Mary M; Goyal, Navneet N; Komati, Rajesh R; Weerathunga, Achira A; Gettridge, Cory C; Stevens, Cheryl L Klein CLK; Jones, Frank E FE; Sridhar, Jayalakshmi J
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
Targeted mutation detection in breast cancer using MammaSeq™.
Breast Cancer Research : Bcr
Smith, Nicholas G NG; Gyanchandani, Rekha R; Shah, Osama S OS; Gurda, Grzegorz T GT; Lucas, Peter C PC; Hartmaier, Ryan J RJ; Brufsky, Adam M AM; Puhalla, Shannon S; Bahreini, Amir A; Kota, Karthik K; Wald, Abigail I AI; Nikiforov, Yuri E YE; Nikiforova, Marina N MN; Oesterreich, Steffi S; Lee, Adrian V AV
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
Disease Variants of FGFR3 Reveal Molecular Basis for the Recognition and Additional Roles for Cdc37 in Hsp90 Chaperone System.
Structure (London, England : 1993)
Bunney, Tom D TD; Inglis, Alison J AJ; Sanfelice, Domenico D; Farrell, Brendan B; Kerr, Christopher J CJ; Thompson, Gary S GS; Masson, Glenn R GR; Thiyagarajan, Nethaji N; Svergun, Dmitri I DI; Williams, Roger L RL; Breeze, Alexander L AL; Katan, Matilda M
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
Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors.
Oncotarget
Rewcastle, Gordon W GW; Kolekar, Sharada S; Buchanan, Christina M CM; Gamage, Swarna A SA; Giddens, Anna C AC; Tsang, Kit Y KY; Kendall, Jackie D JD; Singh, Ripudaman R; Lee, Woo-Jeong WJ; Smith, Greg C GC; Han, Weiping W; Matthews, David J DJ; Denny, William A WA; Shepherd, Peter R PR; Jamieson, Stephen M F SMF
Genome-wide chemical mutagenesis screens allow unbiased saturation of the cancer genome and identification of drug resistance mutations.
Genome Research
Brammeld, Jonathan S JS; Petljak, Mia M; Martincorena, Inigo I; Williams, Steven P SP; Alonso, Luz Garcia LG; Dalmases, Alba A; Bellosillo, Beatriz B; Robles-Espinoza, Carla Daniela CD; Price, Stacey S; Barthorpe, Syd S; Tarpey, Patrick P; Alifrangis, Constantine C; Bignell, Graham G; Vidal, Joana J; Young, Jamie J; Stebbings, Lucy L; Beal, Kathryn K; Stratton, Michael R MR; Saez-Rodriguez, Julio J; Garnett, Mathew M; Montagut, Clara C; Iorio, Francesco F; McDermott, Ultan U
Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins.
Antiviral Research
Beelontally, Rooksarr R; Wilkie, Gavin S GS; Lau, Betty B; Goodmaker, Charles J CJ; Ho, Catherine M K CMK; Swanson, Chad M CM; Deng, Xianming X; Wang, Jinhua J; Gray, Nathanael S NS; Davison, Andrew J AJ; Strang, Blair L BL
Unprecedently Large-Scale Kinase Inhibitor Set Enabling the Accurate Prediction of Compound-Kinase Activities: A Way toward Selective Promiscuity by Design?
Journal Of Chemical Information And Modeling
Christmann-Franck, Serge S; van Westen, Gerard J P GJ; Papadatos, George G; Beltran Escudie, Fanny F; Roberts, Alexander A; Overington, John P JP; Domine, Daniel D
Integrated digital error suppression for improved detection of circulating tumor DNA.
Nature Biotechnology
Newman, Aaron M AM; Lovejoy, Alexander F AF; Klass, Daniel M DM; Kurtz, David M DM; Chabon, Jacob J JJ; Scherer, Florian F; Stehr, Henning H; Liu, Chih Long CL; Bratman, Scott V SV; Say, Carmen C; Zhou, Li L; Carter, Justin N JN; West, Robert B RB; Sledge, George W GW; Shrager, Joseph B JB; Loo, Billy W BW; Neal, Joel W JW; Wakelee, Heather A HA; Diehn, Maximilian M; Alizadeh, Ash A AA
Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use.
Oncotarget
Patani, Harshnira H; Bunney, Tom D TD; Thiyagarajan, Nethaji N; Norman, Richard A RA; Ogg, Derek D; Breed, Jason J; Ashford, Paul P; Potterton, Andrew A; Edwards, Mina M; Williams, Sarah V SV; Thomson, Gary S GS; Pang, Camilla S M CS; Knowles, Margaret A MA; Breeze, Alexander L AL; Orengo, Christine C; Phillips, Chris C; Katan, Matilda M
Mutational profiling of brain metastasis from breast cancer: matched pair analysis of targeted sequencing between brain metastasis and primary breast cancer.
Oncotarget
Lee, Ji Yun JY; Park, Kyunghee K; Lim, Sung Hee SH; Kim, Hae Su HS; Yoo, Kwai Han KH; Jung, Ki Sun KS; Song, Haa-Na HN; Hong, Mineui M; Do, In-Gu IG; Ahn, TaeJin T; Lee, Se Kyung SK; Bae, Soo Youn SY; Kim, Seok Won SW; Lee, Jeong Eon JE; Nam, Seok Jin SJ; Kim, Duk-Hwan DH; Jung, Hae Hyun HH; Kim, Ji-Yeon JY; Ahn, Jin Seok JS; Im, Young-Hyuck YH; Park, Yeon Hee YH
Patient-derived cell models as preclinical tools for genome-directed targeted therapy.
Oncotarget
Lee, Ji Yun JY; Kim, Sun Young SY; Park, Charny C; Kim, Nayoung K D NK; Jang, Jiryeon J; Park, Kyunghee K; Yi, Jun Ho JH; Hong, Mineui M; Ahn, Taejin T; Rath, Oliver O; Schueler, Julia J; Kim, Seung Tae ST; Do, In-Gu IG; Lee, Sujin S; Park, Se Hoon SH; Ji, Yong Ick YI; Kim, Dukwhan D; Park, Joon Oh JO; Park, Young Suk YS; Kang, Won Ki WK; Kim, Kyoung-Mee KM; Park, Woong-Yang WY; Lim, Ho Yeong HY; Lee, Jeeyun J