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Items: 15


A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment.

Hyer ML, Milhollen MA, Ciavarri J, Fleming P, Traore T, Sappal D, Huck J, Shi J, Gavin J, Brownell J, Yang Y, Stringer B, Griffin R, Bruzzese F, Soucy T, Duffy J, Rabino C, Riceberg J, Hoar K, Lublinsky A, Menon S, Sintchak M, Bump N, Pulukuri SM, Langston S, Tirrell S, Kuranda M, Veiby P, Newcomb J, Li P, Wu JT, Powe J, Dick LR, Greenspan P, Galvin K, Manfredi M, Claiborne C, Amidon BS, Bence NF.

Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15.


Overcoming platinum resistance in preclinical models of ovarian cancer using the neddylation inhibitor MLN4924.

Jazaeri AA, Shibata E, Park J, Bryant JL, Conaway MR, Modesitt SC, Smith PG, Milhollen MA, Berger AJ, Dutta A.

Mol Cancer Ther. 2013 Oct;12(10):1958-67. doi: 10.1158/1535-7163.MCT-12-1028. Epub 2013 Aug 12.


Novel DNA damage checkpoints mediating cell death induced by the NEDD8-activating enzyme inhibitor MLN4924.

Blank JL, Liu XJ, Cosmopoulos K, Bouck DC, Garcia K, Bernard H, Tayber O, Hather G, Liu R, Narayanan U, Milhollen MA, Lightcap ES.

Cancer Res. 2013 Jan 1;73(1):225-34. doi: 10.1158/0008-5472.CAN-12-1729. Epub 2012 Oct 24.


Treatment-emergent mutations in NAEβ confer resistance to the NEDD8-activating enzyme inhibitor MLN4924.

Milhollen MA, Thomas MP, Narayanan U, Traore T, Riceberg J, Amidon BS, Bence NF, Bolen JB, Brownell J, Dick LR, Loke HK, McDonald AA, Ma J, Manfredi MG, Sells TB, Sintchak MD, Yang X, Xu Q, Koenig EM, Gavin JM, Smith PG.

Cancer Cell. 2012 Mar 20;21(3):388-401. doi: 10.1016/j.ccr.2012.02.009.


Identification and application of NEDD8 E1 inhibitors.

Bruzzese FJ, Milhollen MA, Gavin JM, Josephine HR, Brownell JE.

Methods Mol Biol. 2012;832:577-88. doi: 10.1007/978-1-61779-474-2_40.


Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues.

Chen JJ, Tsu CA, Gavin JM, Milhollen MA, Bruzzese FJ, Mallender WD, Sintchak MD, Bump NJ, Yang X, Ma J, Loke HK, Xu Q, Li P, Bence NF, Brownell JE, Dick LR.

J Biol Chem. 2011 Nov 25;286(47):40867-77. doi: 10.1074/jbc.M111.279984. Epub 2011 Oct 3.


The NEDD8 Conjugation Pathway and Its Relevance in Cancer Biology and Therapy.

Soucy TA, Dick LR, Smith PG, Milhollen MA, Brownell JE.

Genes Cancer. 2010 Jul;1(7):708-16. doi: 10.1177/1947601910382898.


Inhibition of NEDD8-activating enzyme induces rereplication and apoptosis in human tumor cells consistent with deregulating CDT1 turnover.

Milhollen MA, Narayanan U, Soucy TA, Veiby PO, Smith PG, Amidon B.

Cancer Res. 2011 Apr 15;71(8):3042-51. doi: 10.1158/0008-5472.CAN-10-2122. Epub 2011 Apr 12.


NEDD8-targeting drug MLN4924 elicits DNA rereplication by stabilizing Cdt1 in S phase, triggering checkpoint activation, apoptosis, and senescence in cancer cells.

Lin JJ, Milhollen MA, Smith PG, Narayanan U, Dutta A.

Cancer Res. 2010 Dec 15;70(24):10310-20. doi: 10.1158/0008-5472.CAN-10-2062.


MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF-{kappa}B-dependent lymphoma.

Milhollen MA, Traore T, Adams-Duffy J, Thomas MP, Berger AJ, Dang L, Dick LR, Garnsey JJ, Koenig E, Langston SP, Manfredi M, Narayanan U, Rolfe M, Staudt LM, Soucy TA, Yu J, Zhang J, Bolen JB, Smith PG.

Blood. 2010 Sep 2;116(9):1515-23. doi: 10.1182/blood-2010-03-272567. Epub 2010 Jun 4.


Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ.

Brownell JE, Sintchak MD, Gavin JM, Liao H, Bruzzese FJ, Bump NJ, Soucy TA, Milhollen MA, Yang X, Burkhardt AL, Ma J, Loke HK, Lingaraj T, Wu D, Hamman KB, Spelman JJ, Cullis CA, Langston SP, Vyskocil S, Sells TB, Mallender WD, Visiers I, Li P, Claiborne CF, Rolfe M, Bolen JB, Dick LR.

Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024.


An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer.

Soucy TA, Smith PG, Milhollen MA, Berger AJ, Gavin JM, Adhikari S, Brownell JE, Burke KE, Cardin DP, Critchley S, Cullis CA, Doucette A, Garnsey JJ, Gaulin JL, Gershman RE, Lublinsky AR, McDonald A, Mizutani H, Narayanan U, Olhava EJ, Peluso S, Rezaei M, Sintchak MD, Talreja T, Thomas MP, Traore T, Vyskocil S, Weatherhead GS, Yu J, Zhang J, Dick LR, Claiborne CF, Rolfe M, Bolen JB, Langston SP.

Nature. 2009 Apr 9;458(7239):732-6. doi: 10.1038/nature07884.


Alpha-lactalbumin forms a compact molten globule in the absence of disulfide bonds.

Redfield C, Schulman BA, Milhollen MA, Kim PS, Dobson CM.

Nat Struct Biol. 1999 Oct;6(10):948-52.


Core structure of the envelope glycoprotein GP2 from Ebola virus at 1.9-A resolution.

Malashkevich VN, Schneider BJ, McNally ML, Milhollen MA, Pang JX, Kim PS.

Proc Natl Acad Sci U S A. 1999 Mar 16;96(6):2662-7.


Identification of D-peptide ligands through mirror-image phage display.

Schumacher TN, Mayr LM, Minor DL Jr, Milhollen MA, Burgess MW, Kim PS.

Science. 1996 Mar 29;271(5257):1854-7.


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