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Page 1
Discovery of BBO-8520, a first-in-class direct and covalent dual inhibitor of GTP-bound (ON) and GDP-bound (OFF) KRASG12C.
Maciag AE, Stice JP, Wang B, Sharma AK, Chan AH, Lin K, Singh D, Dyba M, Yang Y, Setoodeh S, Smith BP, Ju JH, Jeknic S, Rabara D, Zhang Z, Larsen EK, Esposito D, Denson JP, Ranieri M, Meynardie M, Mehdizadeh S, Alexander PA, Abreu Blanco M, Turner DM, Xu R, Lightstone FC, Wong KK, Stephen AG, Wang K, Simanshu DK, Sinkevicius KW, Nissley DV, Wallace E, McCormick F, Beltran PJ. Maciag AE, et al. Among authors: rabara d. Cancer Discov. 2024 Dec 6. doi: 10.1158/2159-8290.CD-24-0840. Online ahead of print. Cancer Discov. 2024. PMID: 39642212
Comprehensive structure-function analysis reveals gain- and loss-of-function mechanisms impacting oncogenic KRAS activity.
Kwon JJ, Dilly J, Liu S, Kim E, Bian Y, Dharmaiah S, Tran TH, Kapner KS, Ly SH, Yang X, Rabara D, Waybright TJ, Giacomelli AO, Hong AL, Misek S, Wang B, Ravi A, Doench JG, Beroukhim R, Lemke CT, Haigis KM, Esposito D, Root DE, Nissley DV, Stephen AG, McCormick F, Simanshu DK, Hahn WC, Aguirre AJ. Kwon JJ, et al. Among authors: rabara d. bioRxiv [Preprint]. 2024 Oct 25:2024.10.22.618529. doi: 10.1101/2024.10.22.618529. bioRxiv. 2024. PMID: 39484452 Free PMC article. Preprint.
Determining KRAS4B-Targeting Compound Specificity by Top-Down Mass Spectrometry.
D'Ippolito RA, Scheidemantle GM, Rabara D, Abreu Blanco M, Ramakrishnan N, Widmeyer SRT, Messing S, Turner D, Maciag AE, Stephen AG, Esposito D, McCormick F, Nissley DV, DeHart CJ. D'Ippolito RA, et al. Among authors: rabara d. Methods Mol Biol. 2024;2823:291-310. doi: 10.1007/978-1-0716-3922-1_18. Methods Mol Biol. 2024. PMID: 39052227
Measurement of KRAS-GTPase Activity.
Rabara D, Stephen AG. Rabara D, et al. Methods Mol Biol. 2024;2797:91-102. doi: 10.1007/978-1-0716-3822-4_7. Methods Mol Biol. 2024. PMID: 38570454
A Top-Down Proteomic Assay to Evaluate KRAS4B-Compound Engagement.
D'Ippolito RA, Rabara D, Blanco MA, Alberico E, Drew MR, Ramakrishnan N, Sontan D, Widmeyer SRT, Scheidemantle GM, Messing S, Turner D, Arkin M, Maciag AE, Stephen AG, Esposito D, McCormick F, Nissley DV, DeHart CJ. D'Ippolito RA, et al. Among authors: rabara d. Anal Chem. 2024 Apr 2;96(13):5223-5231. doi: 10.1021/acs.analchem.3c05626. Epub 2024 Mar 18. Anal Chem. 2024. PMID: 38498381 Free PMC article.
Revealing the mechanism of action of a first-in-class covalent inhibitor of KRASG12C (ON) and other functional properties of oncogenic KRAS by 31P NMR.
Sharma AK, Pei J, Yang Y, Dyba M, Smith B, Rabara D, Larsen EK, Lightstone FC, Esposito D, Stephen AG, Wang B, Beltran PJ, Wallace E, Nissley DV, McCormick F, Maciag AE. Sharma AK, et al. Among authors: rabara d. J Biol Chem. 2024 Feb;300(2):105650. doi: 10.1016/j.jbc.2024.105650. Epub 2024 Jan 16. J Biol Chem. 2024. PMID: 38237681 Free PMC article.
Biochemical and structural analyses reveal that the tumor suppressor neurofibromin (NF1) forms a high-affinity dimer.
Sherekar M, Han SW, Ghirlando R, Messing S, Drew M, Rabara D, Waybright T, Juneja P, O'Neill H, Stanley CB, Bhowmik D, Ramanathan A, Subramaniam S, Nissley DV, Gillette W, McCormick F, Esposito D. Sherekar M, et al. Among authors: rabara d. J Biol Chem. 2020 Jan 24;295(4):1105-1119. doi: 10.1074/jbc.RA119.010934. Epub 2019 Dec 13. J Biol Chem. 2020. PMID: 31836666 Free PMC article.
KRAS G13D sensitivity to neurofibromin-mediated GTP hydrolysis.
Rabara D, Tran TH, Dharmaiah S, Stephens RM, McCormick F, Simanshu DK, Holderfield M. Rabara D, et al. Proc Natl Acad Sci U S A. 2019 Oct 29;116(44):22122-22131. doi: 10.1073/pnas.1908353116. Epub 2019 Oct 14. Proc Natl Acad Sci U S A. 2019. PMID: 31611389 Free PMC article.