Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers (Englisch)
Freier Zugriff
- Neue Suche nach: Smith, Christopher R.
- Weitere Informationen zu Smith, Christopher R.:
- https://orcid.org/0000-0002-6553-2791
- Neue Suche nach: Aranda, Ruth
- Neue Suche nach: Bobinski, Thomas P.
- Neue Suche nach: Briere, David M.
- Neue Suche nach: Burns, Aaron C.
- Neue Suche nach: Christensen, James G.
- Neue Suche nach: Clarine, Jeffery
- Neue Suche nach: Engstrom, Lars D.
- Neue Suche nach: Gunn, Robin J.
- Neue Suche nach: Ivetac, Anthony
- Neue Suche nach: Jean-Baptiste, Ronald
- Neue Suche nach: Ketcham, John M.
- Neue Suche nach: Kobayashi, Masakazu
- Neue Suche nach: Kuehler, Jon
- Neue Suche nach: Kulyk, Svitlana
- Neue Suche nach: Lawson, J. David
- Neue Suche nach: Moya, Krystal
- Neue Suche nach: Olson, Peter
- Neue Suche nach: Rahbaek, Lisa
- Neue Suche nach: Thomas, Nicole C.
- Neue Suche nach: Wang, Xiaolun
- Neue Suche nach: Waters, Laura M.
- Neue Suche nach: Marx, Matthew A.
- Neue Suche nach: Smith, Christopher R.
- Weitere Informationen zu Smith, Christopher R.:
- https://orcid.org/0000-0002-6553-2791
- Neue Suche nach: Aranda, Ruth
- Neue Suche nach: Bobinski, Thomas P.
- Neue Suche nach: Briere, David M.
- Neue Suche nach: Burns, Aaron C.
- Neue Suche nach: Christensen, James G.
- Neue Suche nach: Clarine, Jeffery
- Neue Suche nach: Engstrom, Lars D.
- Neue Suche nach: Gunn, Robin J.
- Neue Suche nach: Ivetac, Anthony
- Neue Suche nach: Jean-Baptiste, Ronald
- Neue Suche nach: Ketcham, John M.
- Neue Suche nach: Kobayashi, Masakazu
- Neue Suche nach: Kuehler, Jon
- Neue Suche nach: Kulyk, Svitlana
- Neue Suche nach: Lawson, J. David
- Neue Suche nach: Moya, Krystal
- Neue Suche nach: Olson, Peter
- Neue Suche nach: Rahbaek, Lisa
- Neue Suche nach: Thomas, Nicole C.
- Neue Suche nach: Wang, Xiaolun
- Neue Suche nach: Waters, Laura M.
- Neue Suche nach: Marx, Matthew A.
In:
Journal of Medicinal Chemistry
;
65
, 3
;
1749-1766
;
2022
- Aufsatz (Zeitschrift) / Elektronische Ressource
-
Titel:Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers
-
Weitere Titelangaben:J. Med. Chem.
-
Beteiligte:Smith, Christopher R. ( Autor:in ) / Aranda, Ruth ( Autor:in ) / Bobinski, Thomas P. ( Autor:in ) / Briere, David M. ( Autor:in ) / Burns, Aaron C. ( Autor:in ) / Christensen, James G. ( Autor:in ) / Clarine, Jeffery ( Autor:in ) / Engstrom, Lars D. ( Autor:in ) / Gunn, Robin J. ( Autor:in ) / Ivetac, Anthony ( Autor:in )
-
Erschienen in:Journal of Medicinal Chemistry ; 65, 3 ; 1749-1766
-
Verlag:
- Neue Suche nach: American Chemical Society
-
Erscheinungsdatum:10.02.2022
-
ISSN:
-
Coden:
-
DOI:
-
Medientyp:Aufsatz (Zeitschrift)
-
Format:Elektronische Ressource
-
Sprache:Englisch
-
Lizenzbestimmungen:
-
Datenquelle:
Inhaltsverzeichnis – Band 65, Ausgabe 3
Zeige alle Jahrgänge und Ausgaben
Die Inhaltsverzeichnisse werden automatisch erzeugt und basieren auf den im Index des TIB-Portals verfügbaren Einzelnachweisen der enthaltenen Beiträge. Die Anzeige der Inhaltsverzeichnisse kann daher unvollständig oder lückenhaft sein.
- 1609
-
A Call for Diversity Story Guest EditorialsLindsley, Craig W. et al. | 2022
- 1610
-
Journal of Medicinal Chemistry/ACS Medicinal Chemistry Letters/Division of Medicinal Chemistry Joint Portoghese Lectureship Awards: CALL FOR NOMINATIONSLindsley, Craig W. / Liotta, Dennis C. / Bryant-Friedrich, Amanda et al. | 2022
- 1612
-
Analgesic Opioid Ligand Discovery Based on Nonmorphinan Scaffolds Derived from Natural SourcesSmith, Maree T. / Kong, Dehui / Kuo, Andy / Imam, Mohammad Z. / Williams, Craig M. et al. | 2022
- 1662
-
Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside AnaloguesTalukdar, Arindam / Mukherjee, Ayan / Bhattacharya, Debomita et al. | 2022
- 1685
-
Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug DiscoveryWuelfing, W. Peter / El Marrouni, Abdellatif / Lipert, Maya P. / Daublain, Pierre / Kesisoglou, Filippos / Converso, Antonella / Templeton, Allen C. et al. | 2022
- 1695
-
Conjugates of Porphyrinoid-Based Photosensitizers with Cytotoxic Drugs: Current Progress and Future Directions toward Selective Photodynamic TherapyOtvagin, Vasilii F. / Kuzmina, Natalia S. / Kudriashova, Ekaterina S. / Nyuchev, Alexander V. / Gavryushin, Andrei E. / Fedorov, Alexey Yu. et al. | 2022
- 1735
-
Targeting the Non-Catalytic Functions: a New Paradigm for Kinase Drug Discovery?Wang, Zhen / Huang, Weixue / Zhou, Kaijie / Ren, Xiaomei / Ding, Ke et al. | 2022
- 1749
-
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted CancersSmith, Christopher R. / Aranda, Ruth / Bobinski, Thomas P. / Briere, David M. / Burns, Aaron C. / Christensen, James G. / Clarine, Jeffery / Engstrom, Lars D. / Gunn, Robin J. / Ivetac, Anthony et al. | 2022
- 1767
-
Persistence Pays Off: Milvexian Emerges from the Industry’s Longstanding Search for Orally Bioavailable Factor XIa InhibitorsGoodwin, Nicole C. et al. | 2022
- 1770
-
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic TherapyDilger, Andrew K. / Pabbisetty, Kumar B. / Corte, James R. / De Lucca, Indawati / Fang, Tianan / Yang, Wu / Pinto, Donald J. P. / Wang, Yufeng / Zhu, Yeheng / Mathur, Arvind et al. | 2022
- 1786
-
Discovery of 3,4-Dihydrobenzo[f][1,4]oxazepin-5(2H)‑one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer EffectsLi, Yueshan / Zhang, Liting / Yang, Ruicheng / Qiao, Zeen / Wu, Ming / Huang, Chong / Tian, Chenyu / Luo, Xinling / Yang, Wei / Zhang, Yun et al. | 2022
- 1808
-
Circ_ZNF512-Mediated miR-181d-5p Inhibition Limits Cardiomyocyte Autophagy and Promotes Myocardial Ischemia/Reperfusion Injury through an EGR1/mTORC1/TFEB-Based MechanismHuang, Chen / Shu, Liliang / Zhang, Hualu / Zhu, Xiaohua / Huang, Gongcheng / Xu, Jing et al. | 2022
- 1822
-
One- and Two-Photon Uncaging of Carbon Monoxide (CO) with Real-Time Monitoring: On-Demand Carbazole-Based Dual CO-Releasing Platform to Test over Single and Combinatorial Approaches for the Efficient Regression of Orthotopic Murine Melanoma In VivoVenkatesh, Yarra / Vangala, Venugopal / Mengji, Rakesh / Chaudhuri, Amrita / Bhattacharya, Sayantan / Datta, Prasanta Kumar / Banerjee, Rajkumar / Jana, Avijit / Singh, N. D. Pradeep et al. | 2022
- 1835
-
Development of Radiohalogenated Osimertinib Derivatives as Imaging Probes for Companion Diagnostics of OsimertinibMishiro, Kenji / Nishii, Ryuichi / Sawazaki, Izumi / Sofuku, Tomoki / Fuchigami, Takeshi / Sudo, Hitomi / Effendi, Nurmaya / Makino, Akira / Kiyono, Yasushi / Shiba, Kazuhiro et al. | 2022
- 1848
-
Pt(II)-NHC Complex Induces ROS-ERS-Related DAMP Balance to Harness Immunogenic Cell Death in Hepatocellular CarcinomaBian, Mianli / Fan, Rong / Yang, Zhibin / Chen, Yanan / Xu, Zhongren / Lu, Yunlong / Liu, Wukun et al. | 2022
- 1867
-
Multitarget Hybrid Fasudil Derivatives as a New Approach to the Potential Treatment of Amyotrophic Lateral SclerosisMartín-Cámara, Olmo / Arribas, Marina / Wells, Geoffrey / Morales-Tenorio, Marcos / Martín-Requero, Ángeles / Porras, Gracia / Martínez, Ana / Giorgi, Giorgio / López-Alvarado, Pilar / Lastres-Becker, Isabel et al. | 2022
- 1883
-
One-Pot Enzymatic Synthesis and Biological Evaluation of Ganglioside GM3 Derivatives as Potential Cancer ImmunotherapeuticsWang, Juntao / Lu, Dan / Sun, Ran / Lei, Shuwen / Luo, Shuhua / Dang, Xin / Zhang, Yang / Yuan, Chang / Zhang, Yong / Wu, Jinhong et al. | 2022
- 1898
-
Stabilization of the RAS:PDE6D Complex Is a Novel Strategy to Inhibit RAS SignalingYelland, Tamas / Garcia, Esther / Parry, Charles / Kowalczyk, Dominika / Wojnowska, Marta / Gohlke, Andrea / Zalar, Matja / Cameron, Kenneth / Goodwin, Gillian / Yu, Qing et al. | 2022
- 1915
-
Novel Macrocyclic Peptidomimetics Targeting the Polo-Box Domain of Polo-Like Kinase 1Ryu, SeongShick / Park, Jung-Eun / Ham, Young Jin / Lim, Daniel C. / Kwiatkowski, Nicholas P. / Kim, Do-Hee / Bhunia, Debabrata / Kim, Nam Doo / Yaffe, Michael B. / Son, Woolim et al. | 2022
- 1933
-
Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA)S El Salamouni, Nehad / Buckley, Benjamin J. / Jiang, Longguang / Huang, Mingdong / Ranson, Marie / Kelso, Michael J. / Yu, Haibo et al. | 2022
- 1946
-
Discovery of Gut-Restricted Small-Molecule Inhibitors of Intestinal Sodium-Dependent Phosphate Transport Protein 2b (NaPi2b) for the Treatment of HyperphosphatemiaMaemoto, Michihiro / Hirata, Yuuki / Hosoe, Shintaro / Ouchi, Jun / Narushima, Kazuya / Akizawa, Emi / Tsuji, Yoshiro / Takada, Hidenori / Yanagisawa, Arata / Shuto, Satoshi et al. | 2022
- 1961
-
Phenolic Lipids Derived from Cashew Nut Shell Liquid to Treat Metabolic DiseasesSahin, Cigdem / Magomedova, Lilia / Ferreira, Thais A. M. / Liu, Jiabao / Tiefenbach, Jens / Alves, Priscilla S. / Queiroz, Fellipe J. G. / Oliveira, Andressa S. de / Bhattacharyya, Mousumi / Grouleff, Julie et al. | 2022
- 1979
-
N‑Substituted 5‑(1H‑Indol-2-yl)-2-methoxyanilines Are Allosteric Inhibitors of the Linoleate Oxygenase Activity of Selected Mammalian ALOX15 Orthologs: Mechanism of ActionGolovanov, Alexey / Zhuravlev, Alexander / Cruz, Alejandro / Aksenov, Vladislav / Shafiullina, Rania / Kakularam, Kumar R. / Lluch, José M. / Kuhn, Hartmut / González-Lafont, Àngels / Ivanov, Igor et al. | 2022
- 1996
-
In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by AmidinoureasOttavi, Samantha / Scarry, Sarah M. / Mosior, John / Ling, Yan / Roberts, Julia / Singh, Amrita / Zhang, David / Goullieux, Laurent / Roubert, Christine / Bacqué, Eric et al. | 2022
- 2023
-
Development and Characterization of a Fluorescent Ligand for Leukotriene B4 Receptor 2 in Cells and TissuesHeering, Jan / Hernandez-Olmos, Victor / Ildefeld, Niklas / Liu, Ting / Kaiser, Anja / Naeem, Zumer / Frömel, Timo / Fleming, Ingrid / Steinhilber, Dieter / Proschak, Ewgenij et al. | 2022
- 2035
-
Structural Optimization and Structure–Activity Relationship Studies of 6,6-Dimethyl-4-(phenylamino)‑6H‑pyrimido[5,4‑b][1,4]oxazin-7(8H)‑one Derivatives as A New Class of Potent Inhibitors of Pan-Trk and Their Drug-Resistant MutantsPan, Shulei / Zhang, Liting / Luo, Xinling / Nan, Jinshan / Yang, Wei / Bin, Huachao / Li, Yang / Huang, Qiao / Wang, Tianqi / Pan, Zhiling et al. | 2022
- 2059
-
Thieno[2,3‑d]pyrimidine-2,4(1H,3H)‑dione Derivative Inhibits d‑Dopachrome Tautomerase Activity and Suppresses the Proliferation of Non-Small Cell Lung Cancer CellsXiao, Zhangping / Osipyan, Angelina / Song, Shanshan / Chen, Deng / Schut, Reinder A. / van Merkerk, Ronald / van der Wouden, Petra E. / Cool, Robbert H. / Quax, Wim J. / Melgert, Barbro N. et al. | 2022
- 2078
-
Self-assembled NIR-II Fluorophores with Ultralong Blood Circulation for Cancer Imaging and Image-guided SurgeryLi, Yang / Gao, Jianfeng / Wang, Shuping / Du, Mingxia / Hou, Xiaowen / Tian, Tian / Qiao, Xue / Tian, Zhiquan / Stang, Peter J. / Li, Shijun et al. | 2022
- 2091
-
Optimization of 2‑Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A1 AntagonistsVal, Cristina / Rodríguez-García, Carlos / Prieto-Díaz, Rubén / Crespo, Abel / Azuaje, Jhonny / Carbajales, Carlos / Majellaro, Maria / Díaz-Holguín, Alejandro / Brea, José M. / Loza, Maria Isabel et al. | 2022
- 2107
-
Design, Synthesis, and Biological Evaluation of 2‑((4-Bisarylmethyl-piperazin-1-yl)methyl)benzonitrile Derivatives as HCV Entry InhibitorsWang, Yixuan / Li, Jianrui / Tan, Jiali / Yang, Bo / Quan, Yanni / Peng, Zonggen / Li, Yanping / Li, Zhuorong et al. | 2022
- 2122
-
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PKDing, Li / Pannecouque, Christophe / De Clercq, Erik / Zhuang, Chunlin / Chen, Fen-Er et al. | 2022
- 2139
-
Structure–Activity Relationships of Anti-microRNA Oligonucleotides Containing Cationic Guanidine-Modified Nucleic AcidsTakegawa-Araki, Tomo / Kumagai, Shinji / Yasukawa, Kai / Kuroda, Masataka / Sasaki, Takashi / Obika, Satoshi et al. | 2022
- 2149
-
Discovery of Novel Inhibitors of Uridine Diphosphate‑N‑Acetylenolpyruvylglucosamine Reductase (MurB) from Pseudomonas aeruginosa, an Opportunistic Infectious Agent Causing Death in Cystic Fibrosis PatientsAcebrón-García-de-Eulate, Marta / Mayol-Llinàs, Joan / Holland, Matthew T. O. / Kim, So Yeon / Brown, Karen P. / Marchetti, Chiara / Hess, Jeannine / Di Pietro, Ornella / Mendes, Vitor / Abell, Chris et al. | 2022
- 2174
-
Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting‑1 (Pin1)Liu, Liping / Zhu, Rui / Li, Jiacheng / Pei, Yuan / Wang, Shuangshuang / Xu, Pan / Wang, Mingyu / Wen, Yu / Zhang, Hao / Du, Daohai et al. | 2022
- 2191
-
Development of High Brain-Penetrant and Reversible Monoacylglycerol Lipase PET Tracers for NeuroimagingHe, Yingfang / Schild, Matthias / Grether, Uwe / Benz, Jörg / Leibrock, Lea / Heer, Dominik / Topp, Andreas / Collin, Ludovic / Kuhn, Bernd / Wittwer, Matthias et al. | 2022
- 2208
-
N‑Methylpropargylamine-Conjugated Hydroxamic Acids as Dual Inhibitors of Monoamine Oxidase A and Histone Deacetylase for Glioma TreatmentMehndiratta, Samir / Qian, Bin / Chuang, Jian-Ying / Liou, Jing-Ping / Shih, Jean C. et al. | 2022
- 2225
-
A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal TherapyLiu, Yishen / Li, Qianqian / Gu, Meijia / Lu, Disheng / Xiong, Xiaoxing / Zhang, Zhiyun / Pan, Yanna / Liao, Yuqin / Ding, Qihang / Gong, Wanxia et al. | 2022
- 2238
-
Highly Antiproliferative Latonduine and Indolo[2,3‑c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory ProfileWittmann, Christopher / Bacher, Felix / Enyedy, Eva A. / Dömötör, Orsolya / Spengler, Gabriella / Madejski, Christian / Reynisson, Jóhannes / Arion, Vladimir B. et al. | 2022
- 2262
-
Design, Synthesis, and Characterization of I‑BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral CandidateHumphreys, Philip G. / Atkinson, Stephen J. / Bamborough, Paul / Bit, Rino A. / Chung, Chun-wa / Craggs, Peter D. / Cutler, Leanne / Davis, Rob / Ferrie, Alan / Gong, GangLi et al. | 2022
- 2288
-
Design of a Potent TLX Agonist by Rational Fragment FusionFaudone, Giuseppe / Zhubi, Rezart / Celik, Fatih / Knapp, Stefan / Chaikuad, Apirat / Heering, Jan / Merk, Daniel et al. | 2022
- 2297
-
Structural Biology-Guided Design, Synthesis, and Biological Evaluation of Novel Insect Nicotinic Acetylcholine Receptor Orthosteric ModulatorsMontgomery, Mark / Rendine, Stefano / Zimmer, Christoph T. / Elias, Jan / Schaetzer, Jürgen / Pitterna, Thomas / Benfatti, Fides / Skaljac, Marisa / Bigot, Aurélien et al. | 2022
- 2313
-
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC DegradersLu, Jibu / Huang, Yongjun / Huang, Jing / He, Rui / Huang, Minhao / Lu, Xiaoyun / Xu, Yong / Zhou, Fengtao / Zhang, Zhang / Ding, Ke et al. | 2022
- 2329
-
5‑C‑Branched Deoxynojirimycin: Strategy for Designing a 1‑Deoxynojirimycin-Based Pharmacological Chaperone with a Nanomolar Affinity for Pompe DiseaseKato, Atsushi / Nakagome, Izumi / Kanekiyo, Uta / Lu, Tian-Tian / Li, Yi-Xian / Yoshimura, Kosuke / Kishida, Mana / Shinzawa, Kenta / Yoshida, Tomoki / Tanaka, Nobutada et al. | 2022
- 2342
-
A Structure-based Design Approach for Generating High Affinity BRD4 D1-Selective Chemical ProbesCui, Huarui / Divakaran, Anand / Hoell, Zachariah J. / Ellingson, Mikael O. / Scholtz, Cole R. / Zahid, Huda / Johnson, Jorden A. / Griffith, Elizabeth C. / Gee, Clifford T. / Lee, Amani L. et al. | 2022
- 2361
-
Fluconazole-COX Inhibitor Hybrids: A Dual-Acting Class of Antifungal AzolesElias, Rebecca / Basu, Pallabita / Fridman, Micha et al. | 2022
- 2374
-
Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid‑1 (CB1R) Receptor with Reduced LipophilicityIyer, Malliga R. / Cinar, Resat / Wood, Casey M. / Zawatsky, Charles N. / Coffey, Nathan J. / Kim, Kyu Ah / Liu, Ziyi / Katz, Alexis / Abdalla, Jasmina / Hassan, Sergio A. et al. | 2022
- 2388
-
Discovery, X‑ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding SiteLiu, Zhiqing / Li, Yi / Chen, Haiying / Lai, Hsien-Tsung / Wang, Pingyuan / Wu, Shwu-Yuan / Wold, Eric A. / Leonard, Paul G. / Joseph, Sarah / Hu, Haitao et al. | 2022
- 2409
-
Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 InhibitorsScortichini, Mirko / Idris, Riham Mohammed / Moschütz, Susanne / Keim, Antje / Salmaso, Veronica / Dobelmann, Clemens / Oliva, Paola / Losenkova, Karolina / Irjala, Heikki / Vaittinen, Samuli et al. | 2022
- 2434
-
Discovery of Novel Histone Deacetylase 6 (HDAC6) Inhibitors with Enhanced Antitumor Immunity of Anti-PD-L1 Immunotherapy in MelanomaPeng, Xiaopeng / Li, Ling / Chen, Jingxuan / Ren, Yichang / Liu, Jin / Yu, Ziwen / Cao, Hao / Chen, Jianjun et al. | 2022
- 2458
-
Development of Novel Dihydrofuro[3,4‑d]pyrimidine Derivatives as HIV‑1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181CKang, Dongwei / Sun, Yanying / Feng, Da / Gao, Shenghua / Wang, Zhao / Jing, Lanlan / Zhang, Tao / Jiang, Xiangyi / Lin, Hao / De Clercq, Erik et al. | 2022
- 2471
-
Synthesis and Evaluation of Structurally Diverse C‑2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate SynthaseLee, Hiu-Fung / Lacbay, Cyrus M. / Boutin, Rebecca / Matralis, Alexios N. / Park, Jaeok / Waller, Daniel D. / Guan, Tian Lai / Sebag, Michael / Tsantrizos, Youla S. et al. | 2022
- 2497
-
Activation of E6AP/UBE3A-Mediated Protein Ubiquitination and Degradation Pathways by a Cyclic γ‑AA PeptideHuang, Bo / Zhou, Li / Liu, Ruochuan / Wang, Lei / Xue, Songyi / Shi, Yan / Jeong, Geon Ho / Jeong, In Ho / Li, Sihao / Yin, Jun et al. | 2022
- 2507
-
Discovery of N‑(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2Chai, Xin / Sun, Huiyong / Zhou, Wenfang / Chen, Changwei / Shan, Luhu / Yang, Yuhui / He, Junzhao / Pang, Jinping / Yang, Liu / Wang, Xinyue et al. | 2022
- 2522
-
A Vaccine against Benzimidazole-Derived New Psychoactive Substances That Are More Potent Than FentanylLee, Jinny Claire / Park, Hyeri / Eubanks, Lisa M. / Ellis, Beverly / Zhou, Bin / Janda, Kim D. et al. | 2022
- 2532
-
Synthesis of Hemiprotonic Phenanthroline–Phenanthroline+ Compounds with both Antitumor and Antimicrobial ActivityZhao, Zizhen / Li, Xiaorong / Cui, Zhihong / Tong, Tingting / Zhang, Yingying / Zhang, Yuping / Yang, Xiaoxi / Keerthiga, Rajendiran / Fu, Chen / Fu, Ailing et al. | 2022
- 2548
-
Repositioning Food and Drug Administration-Approved Drugs for Inhibiting Biliverdin IXβ Reductase B as a Novel Thrombocytopenia Therapeutic TargetKim, Myeongkyu / Ha, Jung-Hye / Choi, Joonhyeok / Kim, Bo-Ram / Gapsys, Vytautas / Lee, Ko On / Jee, Jun-Goo / Chakrabarti, Kalyan S. / de Groot, Bert L. / Griesinger, Christian et al. | 2022
- 2558
-
Self-Adjuvanting Lipoprotein Conjugate αGalCer-RBD Induces Potent Immunity against SARS-CoV‑2 and its Variants of ConcernWang, Jian / Wen, Yu / Zhou, Shi-Hao / Zhang, Hai-Wei / Peng, Xiao-Qian / Zhang, Ru-Yan / Yin, Xu-Guang / Qiu, Hong / Gong, Rui / Yang, Guang-Fu et al. | 2022
- 2571
-
Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic SteatohepatitisFeng, Zhiqi / Xiang, Jiehao / Liu, Hui / Li, Jiaxin / Xu, Xiangrui / Sun, Gang / Zheng, Runan / Zhang, Shangran / Liu, Junlong / Yang, Shanlin et al. | 2022
- 2593
-
Synthesis and Characterization of 5‑(2-Fluoro-4‑[11C]methoxyphenyl)-2,2-dimethyl-3,4-dihydro‑2H‑pyrano[2,3‑b]pyridine-7-carboxamide as a PET Imaging Ligand for Metabotropic Glutamate Receptor 2Yuan, Gengyang / Dhaynaut, Maeva / Lan, Yu / Guehl, Nicolas J. / Huynh, Dalena / Iyengar, Suhasini M. / Afshar, Sepideh / Jain, Manish Kumar / Pickett, Julie E. / Kang, Hye Jin et al. | 2022
- 2610
-
Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P‑Glycoprotein Inhibitory PharmacophoreDewa, Amila Agampodi / Elbanna, Ahmed H. / Khalil, Zeinab G. / Capon, Robert J. et al. | 2022
- 2623
-
Aggregation Time Machine: A Platform for the Prediction and Optimization of Long-Term Antibody Stability Using Short-Term Kinetic AnalysisBunc, Marko / Hadži, San / Graf, Christian / Bončina, Matjaž / Lah, Jurij et al. | 2022
- 2633
-
Molecular Engineering of Efficacious Mono-Valent Ultra-Long Acting Two-Chain Insulin-Fc ConjugatesTagmose, Tina M. / Pedersen, Karen-Margrethe / Pridal, Lone / Stidsen, Carsten E. / Pedersen, Marie Ø. / Lin, Zhaosheng / Zhang, Yuanyuan / Wan, Zhe / Ferreras, Mercedes / Naver, Helle et al. | 2022
- 2646
-
Systematic Variation of Both the Aromatic Cage and Dialkyllysine via GCE-SAR Reveal Mechanistic Insights in CBX5 Reader Protein BindingKean, Kelsey M. / Baril, Stefanie A. / Lamb, Kelsey N. / Dishman, Sarah N. / Treacy, Joseph W. / Houk, Kendall N. / Brustad, Eric M. / James, Lindsey I. / Waters, Marcey L. et al. | 2022
- 2656
-
Structure-Guided Discovery of the Novel Covalent Allosteric Site and Covalent Inhibitors of Fructose-1,6-Bisphosphate Aldolase to Overcome the Azole Resistance of CandidiasisWen, Wuqiang / Cao, Hongxuan / Huang, Yunyuan / Tu, Jie / Wan, Chen / Wan, Jian / Han, Xinya / Chen, Han / Liu, Jiaqi / Rao, Li et al. | 2022
- 2675
-
Structure-Based Design and Synthesis of N‑Substituted 3‑Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation AgentsLi, Yong / Liu, Yan / Zhu, Zejiang / Yan, Wei / Zhang, Chufeng / Yang, Zhuang / Bai, Peng / Tang, Minghai / Shi, Mingsong / He, Wen et al. | 2022
- 2694
-
Discovery of Pteridine-7(8H)‑one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK)Dou, Dou / Diao, Yanyan / Sha, Wenjie / Su, Rongrong / Tong, Linjiang / Li, Wenjie / Leng, Limin / Xie, Lijuan / Yu, Zhixiao / Song, Haoming et al. | 2022
- 2710
-
Correction to “Multifunctional Antibiotic–Host Defense Peptide Conjugate Kills Bacteria, Eradicates Biofilms, and Modulates the Innate Immune Response”Etayash, Hashem / Alford, Morgan / Akhoundsadegh, Noushin / Drayton, Matthew / Straus, Suzana K. / Hancock, Robert E. W. et al. | 2022