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Discovery of a Novel Cabazitaxel Nanoparticle-Drug Conjugate (CRLX522) with Improved Pharmacokinetic Properties and Anticancer Effects Using a β-Cyclodextrin-PEG Copolymer Based Delivery Platform.
Metcalf CA 3rd, Svenson S, Hwang J, Tripathi S, Gangal G, Kabir S, Lazarus D, Cole R, Sweryda-Krawiec B, Shum P, Brown D, Case RI, van der Poll D, Rohde E, Harlfinger S, Teng CH, Eliasof S. Metcalf CA 3rd, et al. J Med Chem. 2019 Nov 14;62(21):9541-9559. doi: 10.1021/acs.jmedchem.9b00892. Epub 2019 Oct 24. J Med Chem. 2019. PMID: 31593466
Structure-based discovery of LpxC inhibitors.
Zhang J, Chan A, Lippa B, Cross JB, Liu C, Yin N, Romero JA, Lawrence J, Heney R, Herradura P, Goss J, Clark C, Abel C, Zhang Y, Poutsiaka KM, Epie F, Conrad M, Mahamoon A, Nguyen K, Chavan A, Clark E, Li TC, Cheng RK, Wood M, Andersen OA, Brooks M, Kwong J, Barker J, Parr IB, Gu Y, Ryan MD, Coleman S, Metcalf CA 3rd. Zhang J, et al. Among authors: metcalf ca 3rd. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1670-1680. doi: 10.1016/j.bmcl.2017.03.006. Epub 2017 Mar 6. Bioorg Med Chem Lett. 2017. PMID: 28302397
Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.
Cross JB, Zhang J, Yang Q, Mesleh MF, Romero JA, Wang B, Bevan D, Poutsiaka KM, Epie F, Moy T, Daniel A, Shotwell J, Chamberlain B, Carter N, Andersen O, Barker J, Ryan MD, Metcalf CA 3rd, Silverman J, Nguyen K, Lippa B, Dolle RE. Cross JB, et al. Among authors: metcalf ca 3rd. ACS Med Chem Lett. 2016 Feb 16;7(4):374-8. doi: 10.1021/acsmedchemlett.5b00368. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096044 Free PMC article.
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
Zhang J, Yang Q, Romero JA, Cross J, Wang B, Poutsiaka KM, Epie F, Bevan D, Wu Y, Moy T, Daniel A, Chamberlain B, Carter N, Shotwell J, Arya A, Kumar V, Silverman J, Nguyen K, Metcalf CA 3rd, Ryan D, Lippa B, Dolle RE. Zhang J, et al. Among authors: metcalf ca 3rd. ACS Med Chem Lett. 2015 Sep 8;6(10):1080-5. doi: 10.1021/acsmedchemlett.5b00266. eCollection 2015 Oct 8. ACS Med Chem Lett. 2015. PMID: 26487916 Free PMC article.
Discovery of Azaindole Ureas as a Novel Class of Bacterial Gyrase B Inhibitors.
Zhang J, Yang Q, Cross JB, Romero JA, Poutsiaka KM, Epie F, Bevan D, Wang B, Zhang Y, Chavan A, Zhang X, Moy T, Daniel A, Nguyen K, Chamberlain B, Carter N, Shotwell J, Silverman J, Metcalf CA 3rd, Ryan D, Lippa B, Dolle RE. Zhang J, et al. Among authors: metcalf ca 3rd. J Med Chem. 2015 Nov 12;58(21):8503-12. doi: 10.1021/acs.jmedchem.5b00961. Epub 2015 Oct 22. J Med Chem. 2015. PMID: 26460684
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.
O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T. O'Hare T, et al. Among authors: metcalf ca 3rd. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Cancer Cell. 2009. PMID: 19878872 Free PMC article.
SRC inhibitors in metastatic bone disease.
Boyce BF, Xing L, Yao Z, Yamashita T, Shakespeare WC, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Dalgarno DC, Iuliucci JD, Sawyer TK. Boyce BF, et al. Among authors: metcalf ca 3rd. Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6291s-6295s. doi: 10.1158/1078-0432.CCR-06-0991. Clin Cancer Res. 2006. PMID: 17062716 Review.
Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.
Han LY, Landen CN, Trevino JG, Halder J, Lin YG, Kamat AA, Kim TJ, Merritt WM, Coleman RL, Gershenson DM, Shakespeare WC, Wang Y, Sundaramoorth R, Metcalf CA 3rd, Dalgarno DC, Sawyer TK, Gallick GE, Sood AK. Han LY, et al. Among authors: metcalf ca 3rd. Cancer Res. 2006 Sep 1;66(17):8633-9. doi: 10.1158/0008-5472.CAN-06-1410. Cancer Res. 2006. PMID: 16951177 Free PMC article.
Future anti-catabolic therapeutic targets in bone disease.
Boyce BF, Xing L, Yao Z, Shakespeare WC, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Dalgarno DC, Iuliucci JD, Sawyer TK. Boyce BF, et al. Among authors: metcalf ca 3rd. Ann N Y Acad Sci. 2006 Apr;1068:447-57. doi: 10.1196/annals.1346.042. Ann N Y Acad Sci. 2006. PMID: 16831942 Review.
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