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Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.

Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW.

J Med Chem. 2019 Apr 25;62(8):3971-3988. doi: 10.1021/acs.jmedchem.8b01991. Epub 2019 Apr 16.


Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses.

Akan DT, Howes JE, Sai J, Arnold AL, Beesetty Y, Phan J, Olejniczak ET, Waterson AG, Fesik SW.

ACS Chem Biol. 2019 Mar 15;14(3):325-331. doi: 10.1021/acschembio.8b00869. Epub 2019 Feb 18.


Fragment-based screening of programmed death ligand 1 (PD-L1).

Perry E, Mills JJ, Zhao B, Wang F, Sun Q, Christov PP, Tarr JC, Rietz TA, Olejniczak ET, Lee T, Fesik S.

Bioorg Med Chem Lett. 2019 Mar 15;29(6):786-790. doi: 10.1016/j.bmcl.2019.01.028. Epub 2019 Jan 24.


A Novel MCL1 Inhibitor Combined with Venetoclax Rescues Venetoclax-Resistant Acute Myelogenous Leukemia.

Ramsey HE, Fischer MA, Lee T, Gorska AE, Arrate MP, Fuller L, Boyd KL, Strickland SA, Sensintaffar J, Hogdal LJ, Ayers GD, Olejniczak ET, Fesik SW, Savona MR.

Cancer Discov. 2018 Dec;8(12):1566-1581. doi: 10.1158/2159-8290.CD-18-0140. Epub 2018 Sep 5.


Understanding the Species Selectivity of Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors.

Zhao B, Arnold AL, Coronel MA, Lee JH, Lee T, Olejniczak ET, Fesik SW.

Biochemistry. 2018 Aug 14;57(32):4952-4958. doi: 10.1021/acs.biochem.8b00626. Epub 2018 Jul 31.


Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design.

Wang F, Jeon KO, Salovich JM, Macdonald JD, Alvarado J, Gogliotti RD, Phan J, Olejniczak ET, Sun Q, Wang S, Camper D, Yuh JP, Shaw JG, Sai J, Rossanese OW, Tansey WP, Stauffer SR, Fesik SW.

J Med Chem. 2018 Jul 12;61(13):5623-5642. doi: 10.1021/acs.jmedchem.8b00375. Epub 2018 Jun 29.


Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.

Shaw S, Bian Z, Zhao B, Tarr JC, Veerasamy N, Jeon KO, Belmar J, Arnold AL, Fogarty SA, Perry E, Sensintaffar JL, Camper DV, Rossanese OW, Lee T, Olejniczak ET, Fesik SW.

J Med Chem. 2018 Mar 22;61(6):2410-2421. doi: 10.1021/acs.jmedchem.7b01155. Epub 2018 Mar 9.


Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.

Zhao B, Sensintaffar J, Bian Z, Belmar J, Lee T, Olejniczak ET, Fesik SW.

Bioorg Med Chem. 2017 Jun 15;25(12):3087-3092. doi: 10.1016/j.bmc.2017.03.060. Epub 2017 Mar 29.


Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors.

Lee T, Bian Z, Zhao B, Hogdal LJ, Sensintaffar JL, Goodwin CM, Belmar J, Shaw S, Tarr JC, Veerasamy N, Matulis SM, Koss B, Fischer MA, Arnold AL, Camper DV, Browning CF, Rossanese OW, Budhraja A, Opferman J, Boise LH, Savona MR, Letai A, Olejniczak ET, Fesik SW.

FEBS Lett. 2017 Jan;591(1):240-251. doi: 10.1002/1873-3468.12497. Epub 2016 Dec 19.


Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.

Pelz NF, Bian Z, Zhao B, Shaw S, Tarr JC, Belmar J, Gregg C, Camper DV, Goodwin CM, Arnold AL, Sensintaffar JL, Friberg A, Rossanese OW, Lee T, Olejniczak ET, Fesik SW.

J Med Chem. 2016 Mar 10;59(5):2054-66. doi: 10.1021/acs.jmedchem.5b01660. Epub 2016 Feb 24.


Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A.

Patrone JD, Pelz NF, Bates BS, Souza-Fagundes EM, Vangamudi B, Camper DV, Kuznetsov AG, Browning CF, Feldkamp MD, Frank AO, Gilston BA, Olejniczak ET, Rossanese OW, Waterson AG, Chazin WJ, Fesik SW.

ChemMedChem. 2016 Apr 19;11(8):893-9. doi: 10.1002/cmdc.201500479. Epub 2016 Jan 8.


Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer.

Goodwin CM, Rossanese OW, Olejniczak ET, Fesik SW.

Cell Death Differ. 2015 Dec;22(12):2098-106. doi: 10.1038/cdd.2015.73. Epub 2015 Jun 5.


Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.

Burke JP, Bian Z, Shaw S, Zhao B, Goodwin CM, Belmar J, Browning CF, Vigil D, Friberg A, Camper DV, Rossanese OW, Lee T, Olejniczak ET, Fesik SW.

J Med Chem. 2015 May 14;58(9):3794-805. doi: 10.1021/jm501984f. Epub 2015 Apr 17.


Interaction with WDR5 promotes target gene recognition and tumorigenesis by MYC.

Thomas LR, Wang Q, Grieb BC, Phan J, Foshage AM, Sun Q, Olejniczak ET, Clark T, Dey S, Lorey S, Alicie B, Howard GC, Cawthon B, Ess KC, Eischen CM, Zhao Z, Fesik SW, Tansey WP.

Mol Cell. 2015 May 7;58(3):440-52. doi: 10.1016/j.molcel.2015.02.028. Epub 2015 Mar 26.


A method for the second-site screening of K-Ras in the presence of a covalently attached first-site ligand.

Sun Q, Phan J, Friberg AR, Camper DV, Olejniczak ET, Fesik SW.

J Biomol NMR. 2014 Sep;60(1):11-4. doi: 10.1007/s10858-014-9849-8. Epub 2014 Aug 3.


Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange.

Burns MC, Sun Q, Daniels RN, Camper D, Kennedy JP, Phan J, Olejniczak ET, Lee T, Waterson AG, Rossanese OW, Fesik SW.

Proc Natl Acad Sci U S A. 2014 Mar 4;111(9):3401-6. doi: 10.1073/pnas.1315798111. Epub 2014 Feb 18.


Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A.

Frank AO, Vangamudi B, Feldkamp MD, Souza-Fagundes EM, Luzwick JW, Cortez D, Olejniczak ET, Waterson AG, Rossanese OW, Chazin WJ, Fesik SW.

J Med Chem. 2014 Mar 27;57(6):2455-61. doi: 10.1021/jm401730y. Epub 2014 Feb 19.


Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.

Friberg A, Vigil D, Zhao B, Daniels RN, Burke JP, Garcia-Barrantes PM, Camper D, Chauder BA, Lee T, Olejniczak ET, Fesik SW.

J Med Chem. 2013 Jan 10;56(1):15-30. doi: 10.1021/jm301448p. Epub 2012 Dec 17.


Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.

Sun Q, Burke JP, Phan J, Burns MC, Olejniczak ET, Waterson AG, Lee T, Rossanese OW, Fesik SW.

Angew Chem Int Ed Engl. 2012 Jun 18;51(25):6140-3. doi: 10.1002/anie.201201358. Epub 2012 May 8. No abstract available.


A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A.

Souza-Fagundes EM, Frank AO, Feldkamp MD, Dorset DC, Chazin WJ, Rossanese OW, Olejniczak ET, Fesik SW.

Anal Biochem. 2012 Feb 15;421(2):742-9. doi: 10.1016/j.ab.2011.11.025. Epub 2011 Dec 1.


Rapid determination of antigenic epitopes in human NGAL using NMR.

Olejniczak ET, Ruan Q, Ziemann RN, Birkenmeyer LG, Saldana SC, Tetin SY.

Biopolymers. 2010 Jul;93(7):657-67. doi: 10.1002/bip.21417.


Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket.

Stewart KD, Huth JR, Ng TI, McDaniel K, Hutchinson RN, Stoll VS, Mendoza RR, Matayoshi ED, Carrick R, Mo H, Severin J, Walter K, Richardson PL, Barrett LW, Meadows R, Anderson S, Kohlbrenner W, Maring C, Kempf DJ, Molla A, Olejniczak ET.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):612-7. doi: 10.1016/j.bmcl.2009.11.076. Epub 2009 Nov 20.


Structural characterization of a soluble amyloid beta-peptide oligomer.

Yu L, Edalji R, Harlan JE, Holzman TF, Lopez AP, Labkovsky B, Hillen H, Barghorn S, Ebert U, Richardson PL, Miesbauer L, Solomon L, Bartley D, Walter K, Johnson RW, Hajduk PJ, Olejniczak ET.

Biochemistry. 2009 Mar 10;48(9):1870-7. doi: 10.1021/bi802046n.


Solution structure and calcium-binding properties of EF-hands 3 and 4 of calsenilin.

Yu L, Sun C, Mendoza R, Wang J, Matayoshi ED, Hebert E, Pereda-Lopez A, Hajduk PJ, Olejniczak ET.

Protein Sci. 2007 Nov;16(11):2502-9.


Solution structure and mutational analysis of pituitary adenylate cyclase-activating polypeptide binding to the extracellular domain of PAC1-RS.

Sun C, Song D, Davis-Taber RA, Barrett LW, Scott VE, Richardson PL, Pereda-Lopez A, Uchic ME, Solomon LR, Lake MR, Walter KA, Hajduk PJ, Olejniczak ET.

Proc Natl Acad Sci U S A. 2007 May 8;104(19):7875-80. Epub 2007 Apr 30.


Integrative genomic analysis of small-cell lung carcinoma reveals correlates of sensitivity to bcl-2 antagonists and uncovers novel chromosomal gains.

Olejniczak ET, Van Sant C, Anderson MG, Wang G, Tahir SK, Sauter G, Lesniewski R, Semizarov D.

Mol Cancer Res. 2007 Apr;5(4):331-9.


Discovery of a novel small molecule binding site of human survivin.

Wendt MD, Sun C, Kunzer A, Sauer D, Sarris K, Hoff E, Yu L, Nettesheim DG, Chen J, Jin S, Comess KM, Fan Y, Anderson SN, Isaac B, Olejniczak ET, Hajduk PJ, Rosenberg SH, Elmore SW.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3122-9. Epub 2007 Mar 16.


Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.

Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM.

J Med Chem. 2006 Jun 15;49(12):3563-80.


Structural studies of Bcl-xL/ligand complexes using 19F NMR.

Yu L, Hajduk PJ, Mack J, Olejniczak ET.

J Biomol NMR. 2006 Apr;34(4):221-7.


Nuclear magnetic resonance structural studies of a potassium channel-charybdotoxin complex.

Yu L, Sun C, Song D, Shen J, Xu N, Gunasekera A, Hajduk PJ, Olejniczak ET.

Biochemistry. 2005 Dec 6;44(48):15834-41.


A surface groove essential for viral Bcl-2 function during chronic infection in vivo.

Loh J, Huang Q, Petros AM, Nettesheim D, van Dyk LF, Labrada L, Speck SH, Levine B, Olejniczak ET, Virgin HW 4th.

PLoS Pathog. 2005 Sep;1(1):e10. Epub 2005 Sep 30.


1H, 13C and 15N resonance assignments of a Bcl-xL/Bad peptide complex.

Petros AM, Fesik SW, Olejniczak ET.

J Biomol NMR. 2005 Jul;32(3):260. No abstract available.


Non-peptidic small molecule inhibitors of XIAP.

Park CM, Sun C, Olejniczak ET, Wilson AE, Meadows RP, Betz SF, Elmore SW, Fesik SW.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):771-5.


ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screens.

Huth JR, Mendoza R, Olejniczak ET, Johnson RW, Cothron DA, Liu Y, Lerner CG, Chen J, Hajduk PJ.

J Am Chem Soc. 2005 Jan 12;127(1):217-24.


Solution structure of human survivin and its binding interface with Smac/Diablo.

Sun C, Nettesheim D, Liu Z, Olejniczak ET.

Biochemistry. 2005 Jan 11;44(1):11-7.


Over-expression of the human MDM2 p53 binding domain by fusion to a p53 transactivation peptide.

Liu Z, Olejniczak ET, Fesik SW.

Protein Expr Purif. 2004 Oct;37(2):493-8.


Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.

Oost TK, Sun C, Armstrong RC, Al-Assaad AS, Betz SF, Deckwerth TL, Ding H, Elmore SW, Meadows RP, Olejniczak ET, Oleksijew A, Oltersdorf T, Rosenberg SH, Shoemaker AR, Tomaselli KJ, Zou H, Fesik SW.

J Med Chem. 2004 Aug 26;47(18):4417-26.


Structure of the N-terminal RNA-binding domain of the SARS CoV nucleocapsid protein.

Huang Q, Yu L, Petros AM, Gunasekera A, Liu Z, Xu N, Hajduk P, Mack J, Fesik SW, Olejniczak ET.

Biochemistry. 2004 May 25;43(20):6059-63.


Structural biology of the Bcl-2 family of proteins.

Petros AM, Olejniczak ET, Fesik SW.

Biochim Biophys Acta. 2004 Mar 1;1644(2-3):83-94. Review.


SOS-NMR: a saturation transfer NMR-based method for determining the structures of protein-ligand complexes.

Hajduk PJ, Mack JC, Olejniczak ET, Park C, Dandliker PJ, Beutel BA.

J Am Chem Soc. 2004 Mar 3;126(8):2390-8.


Defining the p53 DNA-binding domain/Bcl-x(L)-binding interface using NMR.

Petros AM, Gunasekera A, Xu N, Olejniczak ET, Fesik SW.

FEBS Lett. 2004 Feb 13;559(1-3):171-4.


Solution structure and function of an essential CMP kinase of Streptococcus pneumoniae.

Yu L, Mack J, Hajduk PJ, Kakavas SJ, Saiki AY, Lerner CG, Olejniczak ET.

Protein Sci. 2003 Nov;12(11):2613-21.


Solution structure of the BHRF1 protein from Epstein-Barr virus, a homolog of human Bcl-2.

Huang Q, Petros AM, Virgin HW, Fesik SW, Olejniczak ET.

J Mol Biol. 2003 Oct 3;332(5):1123-30.


Structural analysis of UBL5, a novel ubiquitin-like modifier.

McNally T, Huang Q, Janis RS, Liu Z, Olejniczak ET, Reilly RM.

Protein Sci. 2003 Jul;12(7):1562-6.


Solution structure of a Bcl-2 homolog from Kaposi sarcoma virus.

Huang Q, Petros AM, Virgin HW, Fesik SW, Olejniczak ET.

Proc Natl Acad Sci U S A. 2002 Mar 19;99(6):3428-33.


Solution structure and function of a conserved protein SP14.3 encoded by an essential Streptococcus pneumoniae gene.

Yu L, Gunasekera AH, Mack J, Olejniczak ET, Chovan LE, Ruan X, Towne DL, Lerner CG, Fesik SW.

J Mol Biol. 2001 Aug 17;311(3):593-604.


Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.

Liu G, Huth JR, Olejniczak ET, Mendoza R, DeVries P, Leitza S, Reilly EB, Okasinski GF, Fesik SW, von Geldern TW.

J Med Chem. 2001 Apr 12;44(8):1202-10.


Rationale for Bcl-xL/Bad peptide complex formation from structure, mutagenesis, and biophysical studies.

Petros AM, Nettesheim DG, Wang Y, Olejniczak ET, Meadows RP, Mack J, Swift K, Matayoshi ED, Zhang H, Thompson CB, Fesik SW.

Protein Sci. 2000 Dec;9(12):2528-34.


An approach for high-throughput structure determination of proteins by NMR spectroscopy.

Medek A, Olejniczak ET, Meadows RP, Fesik SW.

J Biomol NMR. 2000 Nov;18(3):229-38.


Structural basis for binding of Smac/DIABLO to the XIAP BIR3 domain.

Liu Z, Sun C, Olejniczak ET, Meadows RP, Betz SF, Oost T, Herrmann J, Wu JC, Fesik SW.

Nature. 2000 Dec 21-28;408(6815):1004-8.


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