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Items: 34

1.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility.

Guan J, Zhou W, Hafner M, Blake RA, Chalouni C, Chen IP, De Bruyn T, Giltnane JM, Hartman SJ, Heidersbach A, Houtman R, Ingalla E, Kategaya L, Kleinheinz T, Li J, Martin SE, Modrusan Z, Nannini M, Oeh J, Ubhayakar S, Wang X, Wertz IE, Young A, Yu M, Sampath D, Hager JH, Friedman LS, Daemen A, Metcalfe C.

Cell. 2019 Aug 8;178(4):949-963.e18. doi: 10.1016/j.cell.2019.06.026. Epub 2019 Jul 25.

PMID:
31353221
2.

Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.

Labadie SS, Li J, Blake RA, Chang JH, Goodacre S, Hartman SJ, Liang W, Kiefer JR, Kleinheinz T, Lai T, Liao J, Ortwine DF, Mody V, Ray NC, Roussel F, Vinogradova M, Yeap SK, Zhang B, Zheng X, Zbieg JR, Liang J, Wang X.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2090-2093. doi: 10.1016/j.bmcl.2019.07.013. Epub 2019 Jul 6.

PMID:
31311734
3.

Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.

Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J.

Bioorg Med Chem Lett. 2019 Apr 1;29(7):905-911. doi: 10.1016/j.bmcl.2019.01.036. Epub 2019 Feb 1.

PMID:
30732944
4.

Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.

Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH.

Elife. 2019 Jan 7;8. pii: e44851. doi: 10.7554/eLife.44851.

5.

Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.

Dragovich PS, Blake RA, Chen C, Chen J, Chuh J, den Besten W, Fan F, Fourie A, Hartman SJ, He C, He J, Ingalla ER, Kozak KR, Leong SR, Lu J, Ma Y, Meng L, Nannini M, Oeh J, Ohri R, Lewis Phillips G, Pillow TH, Rowntree RK, Sampath D, Vandlen R, Vollmar B, Wai J, Wertz IE, Xu K, Xu Z, Zhang D.

Chemistry. 2018 Apr 3;24(19):4830-4834. doi: 10.1002/chem.201800859. Epub 2018 Mar 25.

PMID:
29493023
6.

Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.

Di Lello P, Pastor R, Murray JM, Blake RA, Cohen F, Crawford TD, Drobnick J, Drummond J, Kategaya L, Kleinheinz T, Maurer T, Rougé L, Zhao X, Wertz I, Ndubaku C, Tsui V.

J Med Chem. 2017 Dec 28;60(24):10056-10070. doi: 10.1021/acs.jmedchem.7b01293. Epub 2017 Dec 8.

PMID:
29166018
7.

USP7 small-molecule inhibitors interfere with ubiquitin binding.

Kategaya L, Di Lello P, Rougé L, Pastor R, Clark KR, Drummond J, Kleinheinz T, Lin E, Upton JP, Prakash S, Heideker J, McCleland M, Ritorto MS, Alessi DR, Trost M, Bainbridge TW, Kwok MCM, Ma TP, Stiffler Z, Brasher B, Tang Y, Jaishankar P, Hearn BR, Renslo AR, Arkin MR, Cohen F, Yu K, Peale F, Gnad F, Chang MT, Klijn C, Blackwood E, Martin SE, Forrest WF, Ernst JA, Ndubaku C, Wang X, Beresini MH, Tsui V, Schwerdtfeger C, Blake RA, Murray J, Maurer T, Wertz IE.

Nature. 2017 Oct 26;550(7677):534-538. doi: 10.1038/nature24006. Epub 2017 Oct 18.

PMID:
29045385
8.

LBW and SGA Impact Longitudinal Growth and Nutritional Status of Filipino Infants.

Blake RA, Park S, Baltazar P, Ayaso EB, Monterde DB, Acosta LP, Olveda RM, Tallo V, Friedman JF.

PLoS One. 2016 Jul 21;11(7):e0159461. doi: 10.1371/journal.pone.0159461. eCollection 2016.

9.

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.

Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH.

Elife. 2016 Jul 13;5. pii: e15828. doi: 10.7554/eLife.15828. Erratum in: Elife. 2019 Jan 07;8:.

10.

Gender Differences in Scholarly Productivity Within Academic Gynecologic Oncology Departments.

Hill EK, Blake RA, Emerson JB, Svider P, Eloy JA, Raker C, Robison K, Stuckey A.

Obstet Gynecol. 2015 Dec;126(6):1279-84. doi: 10.1097/AOG.0000000000001133.

11.

The mediatory role of maladaptive schema modes between parental care and non-suicidal self-injury.

Saldias A, Power K, Gillanders DT, Campbell CW, Blake RA.

Cogn Behav Ther. 2013;42(3):244-57. doi: 10.1080/16506073.2013.781671. Epub 2013 Jun 4.

PMID:
23734870
12.

A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth.

Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M.

Cancer Res. 2013 May 15;73(10):3132-44. doi: 10.1158/0008-5472.CAN-12-4562. Epub 2013 Mar 28.

13.

High-content, high-throughput analysis of cell cycle perturbations induced by the HSP90 inhibitor XL888.

Lyman SK, Crawley SC, Gong R, Adamkewicz JI, McGrath G, Chew JY, Choi J, Holst CR, Goon LH, Detmer SA, Vaclavikova J, Gerritsen ME, Blake RA.

PLoS One. 2011 Mar 7;6(3):e17692. doi: 10.1371/journal.pone.0017692. Erratum in: PLoS One. 2011;6(3). doi: 10.1371/annotation/73d83e95-8f14-48ed-bb67-2310a33e4ecc.

14.

The genome of deep-sea vent chemolithoautotroph Thiomicrospira crunogena XCL-2.

Scott KM, Sievert SM, Abril FN, Ball LA, Barrett CJ, Blake RA, Boller AJ, Chain PS, Clark JA, Davis CR, Detter C, Do KF, Dobrinski KP, Faza BI, Fitzpatrick KA, Freyermuth SK, Harmer TL, Hauser LJ, Hügler M, Kerfeld CA, Klotz MG, Kong WW, Land M, Lapidus A, Larimer FW, Longo DL, Lucas S, Malfatti SA, Massey SE, Martin DD, McCuddin Z, Meyer F, Moore JL, Ocampo LH Jr, Paul JH, Paulsen IT, Reep DK, Ren Q, Ross RL, Sato PY, Thomas P, Tinkham LE, Zeruth GT.

PLoS Biol. 2006 Nov;4(12):e383.

15.

Target validation in drug discovery.

Blake RA.

Methods Mol Biol. 2007;356:367-77.

PMID:
16988416
16.

The management of inappropriate vocalisation in dementia: a hierarchical approach.

Barton S, Findlay D, Blake RA.

Int J Geriatr Psychiatry. 2005 Dec;20(12):1180-6. Review.

PMID:
16315148
17.

An automated image capture and quantitation approach to identify proteins affecting tumor cell proliferation.

Bhawe KM, Blake RA, Clary DO, Flanagan PM.

J Biomol Screen. 2004 Apr;9(3):216-22.

PMID:
15140383
18.

Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.

Guan H, Laird AD, Blake RA, Tang C, Liang C.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):187-90.

PMID:
14684325
19.

Potent and selective inhibitors of the Met [hepatocyte growth factor/scatter factor (HGF/SF) receptor] tyrosine kinase block HGF/SF-induced tumor cell growth and invasion.

Wang X, Le P, Liang C, Chan J, Kiewlich D, Miller T, Harris D, Sun L, Rice A, Vasile S, Blake RA, Howlett AR, Patel N, McMahon G, Lipson KE.

Mol Cancer Ther. 2003 Nov;2(11):1085-92.

20.

A widely applicable, high-throughput TR-FRET assay for the measurement of kinase autophosphorylation: VEGFR-2 as a prototype.

Moshinsky DJ, Ruslim L, Blake RA, Tang F.

J Biomol Screen. 2003 Aug;8(4):447-52.

PMID:
14567797
22.

In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship.

Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM.

Clin Cancer Res. 2003 Jan;9(1):327-37.

23.

Cellular screening assays using fluorescence microscopy.

Blake RA.

Curr Opin Pharmacol. 2001 Oct;1(5):533-9. Review.

PMID:
11764781
24.

SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling.

Blake RA, Broome MA, Liu X, Wu J, Gishizky M, Sun L, Courtneidge SA.

Mol Cell Biol. 2000 Dec;20(23):9018-27.

25.

SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

Laird AD, Vajkoczy P, Shawver LK, Thurnher A, Liang C, Mohammadi M, Schlessinger J, Ullrich A, Hubbard SR, Blake RA, Fong TA, Strawn LM, Sun L, Tang C, Hawtin R, Tang F, Shenoy N, Hirth KP, McMahon G, Cherrington.

Cancer Res. 2000 Aug 1;60(15):4152-60.

26.

Development of SU5416, a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity, as an anti-angiogenesis agent.

Mendel DB, Laird AD, Smolich BD, Blake RA, Liang C, Hannah AL, Shaheen RM, Ellis LM, Weitman S, Shawver LK, Cherrington JM.

Anticancer Drug Des. 2000 Feb;15(1):29-41. Review.

PMID:
10888034
27.

Src promotes PKCdelta degradation.

Blake RA, Garcia-Paramio P, Parker PJ, Courtneidge SA.

Cell Growth Differ. 1999 Apr;10(4):231-41.

28.

Synthetic scanner arrays in tomographic reconstructionsfrom fan- and cone-beam projections.

Müller M, Arce GR, Blake RA.

Appl Opt. 1994 Dec 10;33(35):8255-69. doi: 10.1364/AO.33.008255.

PMID:
20963059
29.
32.

The use of inhibitors of protein kinases and protein phosphatases to investigate the role of protein phosphorylation in platelet activation.

Watson SP, Blake RA, Lane T, Walker TR.

Adv Exp Med Biol. 1993;344:105-18. Review. No abstract available.

PMID:
8209780
33.

Visualization of a recanalized umbilical vein on hepatobiliary imaging with CT correlation.

Alexander MS, Blake RA, Gelman R.

Clin Nucl Med. 1991 Jul;16(7):517-9. No abstract available.

PMID:
1934798
34.

A method of integrating family nursing in an undergraduate curriculum.

Blake RA, Druck A, Harsanyi B, Hutchinson S, Russell P.

J Nurs Educ. 1976 Nov;15(6):22-5.

PMID:
62040

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