Cyclin A/B RxL Macrocyclic Inhibitors to Treat Cancers with High E2F Activity
Singh S, Gleason CE, Fang M, Laimon YN, Khivansara V, Xie S, Durmaz YT, Sarkar A, Ngo K, Savla V, Li Y, Abu-Remaileh M, Li X, Tuladhar B, Odeh R, Hamkins-Indik F, He D, Membreno MW, Nosrati M, Gushwa NN, Leung SSF, Fraga-Walton B, Hernandez L, Baldomero MP, Lent BM, Spellmeyer D, Luna JF, Hoang D, Gritsenko Y, Chand M, DeMart MK, Metobo S, Bhatt C, Shapiro JA, Yang K, Dupper NJ, Bockus AT, Doench JG, Aggen JB, Liu LF, Levin B, Wang EW, Vendrell I, Fischer R, Kessler B, Gokhale PC, Signoretti S, Spektor A, Kreatsoulas C, Singh R, Earp DJ, Garcia PD, Nijhawan D, Oser MG. bioRxiv [Preprint] 2024.
Thiophenyl Derivatives of Nicotinamide Are Metabolized by the NAD Salvage Pathway into Unnatural NAD Derivatives That Inhibit IMPDH and Are Toxic to Peripheral Nerve Cancers
Theodoropoulos PC, Guo HH, Wang W, Crossley E, Rivera Cancel G, Fang M, Nguyen T, Baniasadi H, Williams NS, Ready JM, De Brabander JK, Nijhawan D. ACS Chem Biol 2024.
Discovery and Optimization of N-Arylated Tetracyclic Dicarboximides That Target Primary Glioma Stem-like Cells
Wang HY, Nguyen TP, Sternisha AC, Carroll CL, Cross B, Morlock L, Williams NS, McBrayer S, Nijhawan D, De Brabander JK. J Med Chem 2024.
Anticancer benzoxaboroles block pre-mRNA processing by directly inhibiting CPSF3
Tao Y, Budhipramono A, Huang J, Fang M, Xie S, Kim J, Khivansara V, Dominski Z, Tong L, De Brabander JK, Nijhawan D. Cell Chem Biol 2024.
Inducible mismatch repair streamlines forward genetic approaches to target identification of cytotoxic small molecules
Nguyen TP, Fang M, Kim J, Wang B, Lin E, Khivansara V, Barrows N, Rivera-Cancel G, Goralski M, Cervantes CL, Xie S, Peterson JM, Povedano JM, Antczak MI, Posner BA, Harvey CJB, Naughton BT, McFadden DG, Ready JM, De Brabander JK,
Nijhawan D. Cell Chem Biol 2023.
Targeting neddylation sensitizes colorectal cancer to topoisomerase I inhibitors by inactivating the DCAF13-CRL4 ubiquitin ligase complex
Sun Y, Baechler SA, Zhang X, Kumar S, Factor VM, Arakawa Y, Chau CH, Okamoto K, Parikh A, Walker B, Su YP, Chen J, Ting T, Huang SN, Beck E, Itkin Z, McKnight C, Xie C, Roper N, Nijhawan D, Figg WD, Meltzer PS, Yang JC, Thomas CJ, Pommier Y. Nat Commun 2023.
Selective and brain-penetrant lanosterol synthase inhibitors target glioma stem-like cells by inducing 24(S),25-epoxycholesterol production
Nguyen TP, Wang W, Sternisha AC, Corley CD, Wang HL, Wang X, Ortiz F, Lim SK, Abdullah KG, Parada LF, Williams NS, McBrayer SK, McDonald JG, De Brabander JK, Nijhawan D. Cell Chem Biol 2023.
An oncogenic JMJD6-DGAT1 axis tunes the epigenetic regulation of lipid droplet formation in clear cell renal cell carcinoma
Zhou J, Simon JM, Liao C, Zhang C, Hu L, Zurlo G, Liu X, Fan C, Hepperla A, Jia L, Tcheuyap VT, Zhong H, Elias R, Ye J, Henne WM, Kapur P, Nijhawan D, Brugarolas J, Zhang Q. Mol Cell 2022.
Targeting the spliceosome through RBM39 degradation results in exceptional responses in high-risk neuroblastoma models
Singh S, Quarni W, Goralski M, Wan S, Jin H, Van de Velde LA, Fang J, Wu Q, Abu-Zaid A, Wang T, Singh R, Craft D, Fan Y, Confer T, Johnson M, Akers WJ, Wang R, Murray PJ, Thomas PG, Nijhawan D, Davidoff AM, Yang J. Sci Adv 2021.
MIF is a 3' flap nuclease that facilitates DNA replication and promotes tumor growth
Wang Y, Chen Y, Wang C, Yang M, Wang Y, Bao L, Wang JE, Kim B, Chan KY, Xu W, Capota E, Ortega J, Nijhawan D, Li GM, Luo W, Wang Y. Nat Commun 2021.
Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase
Williams NS, Gonzales S, Naidoo J, Rivera-Cancel G, Voruganti S, Mallipeddi P, Theodoropoulos PC, Geboers S, Chen H, Ortiz F, Posner B, Nijhawan D, Ready JM. J Med Chem 2020.
A Medicinal Chemistry-Driven Approach Identified the Sterol Isomerase EBP as the Molecular Target of TASIN Colorectal Cancer Toxins
Theodoropoulos PC, Wang W, Budhipramono A, Thompson BM, Madhusudhan N, Mitsche MA, McDonald JG, De Brabander JK, Nijhawan D. J Am Chem Soc 2020.
Biomarkers for RBM39 degradation in acute myeloid leukemia
Hsiehchen D, Goralski M, Kim J, Xie Y, Nijhawan D. Leukemia 2020.
Target Discovery of Selective Non-Small-Cell Lung Cancer Toxins Reveals Inhibitors of Mitochondrial Complex I
Madhusudhan N, Hu B, Mishra P, Calva-Moreno JF, Patel K, Boriack R, Ready JM, Nijhawan D. ACS Chem Biol 2020.
Structural Basis and Kinetic Pathway of RBM39 Recruitment to DCAF15 by a Sulfonamide Molecular Glue E7820
Du X, Volkov OA, Czerwinski RM, Tan H, Huerta C, Morton ER, Rizzi JP, Wehn PM, Xu R, Nijhawan D, Wallace EM. Structure 2019.
Aryl Sulfonamides Degrade RBM39 and RBM23 by Recruitment to CRL4-DCAF15
Ting TC, Goralski M, Klein K, Wang B, Kim J, Xie Y, Nijhawan D. Cell Rep 2019.
Engineering Forward Genetics into Cultured Cancer Cells for Chemical Target Identification
Povedano JM, Liou J, Wei D, Srivatsav A, Kim J, Xie Y, Nijhawan D, McFadden DG. Cell Chem Biol 2019.
Exome Sequencing of Drug-Resistant Clones for Target Identification
Han T, Nijhawan D. Methods Mol Biol 2019.
Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase
Winterton SE, Capota E, Wang X, Chen H, Mallipeddi PL, Williams NS, Posner BA, Nijhawan D, Ready JM. J Med Chem 2018.
Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15.
Han T, Goralski M, Gaskill N, Capota E, Kim J, Ting TC, Xie Y, Williams NS, Nijhawan D. Science 2017.
Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer
Zhang L, Theodoropoulos PC, Eskiocak U, Wang W, Moon YA, Posner B, Williams NS, Wright WE, Kim SB, Nijhawan D, De Brabander JK, Shay JW. Sci Transl Med 2016.
Synthesis and Biological Evaluation of Kibdelone C and Its Simplified Derivatives
Rujirawanich J, Kim S, Ma AJ, Butler JR, Wang Y, Wang C, Rosen M, Posner B, Nijhawan D, Ready JM. J Am Chem Soc 2016.
The antitumor toxin CD437 is a direct inhibitor of DNA polymerase α.
Han T, Goralski M, Capota E, Padrick SB, Kim J, Xie Y, Nijhawan D. Nat Chem Biol 2016.
Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase.
Theodoropoulos PC, Gonzales SS, Winterton SE, Rodriguez-Navas C, McKnight JS, Morlock LK, Hanson JM, Cross B, Owen AE, Duan Y, Moreno JR, Lemoff A, Mirzaei H, Posner BA, Williams NS, Ready JM, Nijhawan D. Nat Chem Biol 2016.
P7C3 neuroprotective chemicals function by activating the rate-limiting enzyme in NAD salvage
Wang G, Han T, Nijhawan D, Theodoropoulos P, Naidoo J, Yadavalli S, Mirzaei H, Pieper AA, Ready JM, McKnight SL. Cell 2014.
β-Catenin-driven cancers require a YAP1 transcriptional complex for survival and tumorigenesis
Rosenbluh J, Nijhawan D, Cox AG, Li X, Neal JT, Schafer EJ, Zack TI, Wang X, Tsherniak A, Schinzel AC, Shao DD, Schumacher SE, Weir BA, Vazquez F, Cowley GS, Root DE, Mesirov JP, Beroukhim R, Kuo CJ, Goessling W, Hahn WC. Cell 2012.
Cancer vulnerabilities unveiled by genomic loss
Nijhawan D, Zack TI, Ren Y, Strickland MR, Lamothe R, Schumacher SE, Tsherniak A, Besche HC, Rosenbluh J, Shehata S, Cowley GS, Weir BA, Goldberg AL, Mesirov JP, Root DE, Bhatia SN, Beroukhim R, Hahn WC. Cell 2012.
RMRP is a non-coding RNA essential for early murine development
Rosenbluh J, Nijhawan D, Chen Z, Wong KK, Masutomi K, Hahn WC. PLoS One 2011.
Regulating TERT: location, location, location
Rosenbluh J, Nijhawan D, Hahn WC. Cell Cycle 2009.
Mitochondrial activation of apoptosis
Li P, Nijhawan D, Wang X. Cell 2004.
Elimination of Mcl-1 is required for the initiation of apoptosis following ultraviolet irradiation
Nijhawan D, Fang M, Traer E, Zhong Q, Gao W, Du F, Wang X. Genes Dev 2003.
Apoptosis in neural development and disease
Nijhawan D, Honarpour N, Wang X. Annu Rev Neurosci 2000.
Linkage of a commoner form of recessive amyotrophic lateral sclerosis to chromosome 15q15-q22 markers
Hentati A, Ouahchi K, Pericak-Vance MA, Nijhawan D, Ahmad A, Yang Y, Rimmler J, Hung W, Schlotter B, Ahmed A, Ben Hamida M, Hentati F, Siddique T. Neurogenetics 1998
Complementation cloning of S2P, a gene encoding a putative metalloprotease required for intramembrane cleavage of SREBPs
Rawson RB, Zelenski NG, Nijhawan D, Ye J, Sakai J, Hasan MT, Chang TY, Brown MS, Goldstein JL. Mol Cell 1997.
Cytochrome c and dATP-dependent formation of Apaf-1/caspase-9 complex initiates an apoptotic protease cascade
Li P, Nijhawan D, Budihardjo I, Srinivasula SM, Ahmad M, Alnemri ES, Wang X. Cell 1997.
Familial amyotrophic lateral sclerosis
Siddique T, Nijhawan D, Hentati A. J Neural Transm Suppl 1997.
Molecular genetic basis of familial ALS
Siddique T, Nijhawan D, Hentati A. Neurology 1996.