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Items: 20

1.

Improved Total Synthesis of Tubulysins and Design, Synthesis, and Biological Evaluation of New Tubulysins with Highly Potent Cytotoxicities against Cancer Cells as Potential Payloads for Antibody-Drug Conjugates.

Nicolaou KC, Erande RD, Yin J, Vourloumis D, Aujay M, Sandoval J, Munneke S, Gavrilyuk J.

J Am Chem Soc. 2018 Mar 14;140(10):3690-3711. doi: 10.1021/jacs.7b12692. Epub 2018 Jan 30.

PMID:
29381062
2.

Streamlined Total Synthesis of Trioxacarcins and Its Application to the Design, Synthesis, and Biological Evaluation of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin Analogues.

Nicolaou KC, Chen P, Zhu S, Cai Q, Erande RD, Li R, Sun H, Pulukuri KK, Rigol S, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2017 Nov 1;139(43):15467-15478. doi: 10.1021/jacs.7b08820. Epub 2017 Oct 20.

PMID:
29052423
3.

12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents.

Nicolaou KC, Rhoades D, Wang Y, Bai R, Hamel E, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2017 May 31;139(21):7318-7334. doi: 10.1021/jacs.7b02655. Epub 2017 May 17.

PMID:
28513142
4.

A PTK7-targeted antibody-drug conjugate reduces tumor-initiating cells and induces sustained tumor regressions.

Damelin M, Bankovich A, Bernstein J, Lucas J, Chen L, Williams S, Park A, Aguilar J, Ernstoff E, Charati M, Dushin R, Aujay M, Lee C, Ramoth H, Milton M, Hampl J, Lazetic S, Pulito V, Rosfjord E, Sun Y, King L, Barletta F, Betts A, Guffroy M, Falahatpisheh H, O'Donnell CJ, Stull R, Pysz M, Escarpe P, Liu D, Foord O, Gerber HP, Sapra P, Dylla SJ.

Sci Transl Med. 2017 Jan 11;9(372). pii: eaag2611. doi: 10.1126/scitranslmed.aag2611.

PMID:
28077676
5.

Synthesis and Biological Investigation of Δ(12)-Prostaglandin J3 (Δ(12)-PGJ3) Analogues and Related Compounds.

Nicolaou KC, Pulukuri KK, Rigol S, Heretsch P, Yu R, Grove CI, Hale CR, ElMarrouni A, Fetz V, Brönstrup M, Aujay M, Sandoval J, Gavrilyuk J.

J Am Chem Soc. 2016 May 25;138(20):6550-60. doi: 10.1021/jacs.6b02075. Epub 2016 May 12.

PMID:
27171618
6.

Total Synthesis and Biological Evaluation of Natural and Designed Tubulysins.

Nicolaou KC, Yin J, Mandal D, Erande RD, Klahn P, Jin M, Aujay M, Sandoval J, Gavrilyuk J, Vourloumis D.

J Am Chem Soc. 2016 Feb 10;138(5):1698-708. doi: 10.1021/jacs.5b12557. Epub 2016 Feb 1.

PMID:
26829208
7.

A DLL3-targeted antibody-drug conjugate eradicates high-grade pulmonary neuroendocrine tumor-initiating cells in vivo.

Saunders LR, Bankovich AJ, Anderson WC, Aujay MA, Bheddah S, Black K, Desai R, Escarpe PA, Hampl J, Laysang A, Liu D, Lopez-Molina J, Milton M, Park A, Pysz MA, Shao H, Slingerland B, Torgov M, Williams SA, Foord O, Howard P, Jassem J, Badzio A, Czapiewski P, Harpole DH, Dowlati A, Massion PP, Travis WD, Pietanza MC, Poirier JT, Rudin CM, Stull RA, Dylla SJ.

Sci Transl Med. 2015 Aug 26;7(302):302ra136. doi: 10.1126/scitranslmed.aac9459.

8.

Anti-EFNA4 Calicheamicin Conjugates Effectively Target Triple-Negative Breast and Ovarian Tumor-Initiating Cells to Result in Sustained Tumor Regressions.

Damelin M, Bankovich A, Park A, Aguilar J, Anderson W, Santaguida M, Aujay M, Fong S, Khandke K, Pulito V, Ernstoff E, Escarpe P, Bernstein J, Pysz M, Zhong W, Upeslacis E, Lucas J, Lucas J, Nichols T, Loving K, Foord O, Hampl J, Stull R, Barletta F, Falahatpisheh H, Sapra P, Gerber HP, Dylla SJ.

Clin Cancer Res. 2015 Sep 15;21(18):4165-73. doi: 10.1158/1078-0432.CCR-15-0695. Epub 2015 May 26.

9.

Synergistic effects of proteasome inhibitor carfilzomib in combination with tyrosine kinase inhibitors in imatinib-sensitive and -resistant chronic myeloid leukemia models.

Crawford LJ, Chan ET, Aujay M, Holyoake TL, Melo JV, Jorgensen HG, Suresh S, Walker B, Irvine AE.

Oncogenesis. 2014 Mar 3;3:e90. doi: 10.1038/oncsis.2014.3.

10.

Alkaline phosphatase variation during carfilzomib treatment is associated with best response in multiple myeloma patients.

Zangari M, Aujay M, Zhan F, Hetherington KL, Berno T, Vij R, Jagannath S, Siegel D, Keith Stewart A, Wang L, Orlowski RZ, Belch A, Jakubowiak A, Somlo G, Trudel S, Bahlis N, Lonial S, Singhal S, Kukreti V, Tricot G.

Eur J Haematol. 2011 Jun;86(6):484-7. doi: 10.1111/j.1600-0609.2011.01602.x.

11.

Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia.

Sacco A, Aujay M, Morgan B, Azab AK, Maiso P, Liu Y, Zhang Y, Azab F, Ngo HT, Issa GC, Quang P, Roccaro AM, Ghobrial IM.

Clin Cancer Res. 2011 Apr 1;17(7):1753-64. doi: 10.1158/1078-0432.CCR-10-2130. Epub 2011 Feb 25.

12.

PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo.

Singh AV, Bandi M, Aujay MA, Kirk CJ, Hark DE, Raje N, Chauhan D, Anderson KC.

Br J Haematol. 2011 Jan;152(2):155-63. doi: 10.1111/j.1365-2141.2010.08491.x. Epub 2010 Nov 29.

13.

A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma.

Chauhan D, Singh AV, Aujay M, Kirk CJ, Bandi M, Ciccarelli B, Raje N, Richardson P, Anderson KC.

Blood. 2010 Dec 2;116(23):4906-15. doi: 10.1182/blood-2010-04-276626. Epub 2010 Aug 30.

14.

Selective inhibition of chymotrypsin-like activity of the immunoproteasome and constitutive proteasome in Waldenstrom macroglobulinemia.

Roccaro AM, Sacco A, Aujay M, Ngo HT, Azab AK, Azab F, Quang P, Maiso P, Runnels J, Anderson KC, Demo S, Ghobrial IM.

Blood. 2010 May 20;115(20):4051-60. doi: 10.1182/blood-2009-09-243402. Epub 2010 Jan 28.

15.

Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome.

Parlati F, Lee SJ, Aujay M, Suzuki E, Levitsky K, Lorens JB, Micklem DR, Ruurs P, Sylvain C, Lu Y, Shenk KD, Bennett MK.

Blood. 2009 Oct 15;114(16):3439-47. doi: 10.1182/blood-2009-05-223677. Epub 2009 Aug 11.

16.

A selective inhibitor of the immunoproteasome subunit LMP7 blocks cytokine production and attenuates progression of experimental arthritis.

Muchamuel T, Basler M, Aujay MA, Suzuki E, Kalim KW, Lauer C, Sylvain C, Ring ER, Shields J, Jiang J, Shwonek P, Parlati F, Demo SD, Bennett MK, Kirk CJ, Groettrup M.

Nat Med. 2009 Jul;15(7):781-7. doi: 10.1038/nm.1978. Epub 2009 Jun 14. Erratum in: Nat Med. 2009 Nov;15(11):1333.

PMID:
19525961
17.

Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).

Zhou HJ, Aujay MA, Bennett MK, Dajee M, Demo SD, Fang Y, Ho MN, Jiang J, Kirk CJ, Laidig GJ, Lewis ER, Lu Y, Muchamuel T, Parlati F, Ring E, Shenk KD, Shields J, Shwonek PJ, Stanton T, Sun CM, Sylvain C, Woo TM, Yang J.

J Med Chem. 2009 May 14;52(9):3028-38. doi: 10.1021/jm801329v.

PMID:
19348473
18.

Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome.

Demo SD, Kirk CJ, Aujay MA, Buchholz TJ, Dajee M, Ho MN, Jiang J, Laidig GJ, Lewis ER, Parlati F, Shenk KD, Smyth MS, Sun CM, Vallone MK, Woo TM, Molineaux CJ, Bennett MK.

Cancer Res. 2007 Jul 1;67(13):6383-91.

19.

Human immunodeficiency virus type 1 mutations selected in patients failing efavirenz combination therapy.

Bacheler LT, Anton ED, Kudish P, Baker D, Bunville J, Krakowski K, Bolling L, Aujay M, Wang XV, Ellis D, Becker MF, Lasut AL, George HJ, Spalding DR, Hollis G, Abremski K.

Antimicrob Agents Chemother. 2000 Sep;44(9):2475-84.

20.

The complete genome of the hyperthermophilic bacterium Aquifex aeolicus.

Deckert G, Warren PV, Gaasterland T, Young WG, Lenox AL, Graham DE, Overbeek R, Snead MA, Keller M, Aujay M, Huber R, Feldman RA, Short JM, Olsen GJ, Swanson RV.

Nature. 1998 Mar 26;392(6674):353-8.

PMID:
9537320

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