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Items: 1 to 50 of 178

1.

1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.

Asquith CRM, Godoi PH, Couñago RM, Laitinen T, Scott JW, Langendorf CG, Oakhill JS, Drewry DH, Zuercher WJ, Koutentis PA, Willson TM, Kalogirou AS.

Molecules. 2018 May 19;23(5). pii: E1221. doi: 10.3390/molecules23051221.

2.

Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth.

Krulikas LJ, McDonald IM, Lee B, Okumu DO, East MP, Gilbert TSK, Herring LE, Golitz BT, Wells CI, Axtman AD, Zuercher WJ, Willson TM, Kireev D, Yeh JJ, Johnson GL, Baines AT, Graves LM.

SLAS Discov. 2018 May 1:2472555218773045. doi: 10.1177/2472555218773045. [Epub ahead of print]

PMID:
29742358
3.

Donated chemical probes for open science.

Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A.

Elife. 2018 Apr 20;7. pii: e34311. doi: 10.7554/eLife.34311.

4.

Circadian clock component REV-ERBα controls homeostatic regulation of pulmonary inflammation.

Pariollaud M, Gibbs JE, Hopwood TW, Brown S, Begley N, Vonslow R, Poolman T, Guo B, Saer B, Jones DH, Tellam JP, Bresciani S, Tomkinson NC, Wojno-Picon J, Cooper AW, Daniels DA, Trump RP, Grant D, Zuercher W, Willson TM, MacDonald AS, Bolognese B, Podolin PL, Sanchez Y, Loudon AS, Ray DW.

J Clin Invest. 2018 Jun 1;128(6):2281-2296. doi: 10.1172/JCI93910. Epub 2018 Apr 30.

5.

Development and validation of a claims-based approach to proxy ECOG performance status across ten tumor groups.

Sheffield KM, Bowman L, Smith DM, Li L, Hess LM, Montejano LB, Willson TM, Davidoff AJ.

J Comp Eff Res. 2018 Mar;7(3):193-208. doi: 10.2217/cer-2017-0040. Epub 2018 Mar 13.

PMID:
29533694
6.

Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.

Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB.

Cell Chem Biol. 2018 Feb 15;25(2):206-214.e11. doi: 10.1016/j.chembiol.2017.10.010. Epub 2017 Nov 22.

7.

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Asquith CRM, Laitinen T, Bennett JM, Godoi PH, East MP, Tizzard GJ, Graves LM, Johnson GL, Dornsife RE, Wells CI, Elkins JM, Willson TM, Zuercher WJ.

ChemMedChem. 2018 Jan 8;13(1):48-66. doi: 10.1002/cmdc.201700663. Epub 2017 Nov 27.

PMID:
29072804
8.

Characteristics and treatment patterns of US commercially insured and Medicaid patients with opioid dependence or abuse.

Wollschlaeger BA, Willson TM, Montejano LB, Ronquest NA, Nadipelli VR.

J Opioid Manag. 2017 Jul/Aug;13(4):207-220. doi: 10.5055/jom.2017.0389.

PMID:
28953313
9.

Progress towards a public chemogenomic set for protein kinases and a call for contributions.

Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM.

PLoS One. 2017 Aug 2;12(8):e0181585. doi: 10.1371/journal.pone.0181585. eCollection 2017.

10.

Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans.

Smith SH, Jayawickreme C, Rickard DJ, Nicodeme E, Bui T, Simmons C, Coquery CM, Neil J, Pryor WM, Mayhew D, Rajpal DK, Creech K, Furst S, Lee J, Wu D, Rastinejad F, Willson TM, Viviani F, Morris DC, Moore JT, Cote-Sierra J.

J Invest Dermatol. 2017 Oct;137(10):2110-2119. doi: 10.1016/j.jid.2017.05.004. Epub 2017 Jun 6.

11.

Comprehensive characterization of the Published Kinase Inhibitor Set.

Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ.

Nat Biotechnol. 2016 Jan;34(1):95-103. doi: 10.1038/nbt.3374. Epub 2015 Oct 26.

PMID:
26501955
12.

Corrigendum: The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Ross R, Roth B, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Nov;11(11):887. doi: 10.1038/nchembio1115-887c. No abstract available.

PMID:
26485080
13.

The promise and peril of chemical probes.

Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frederiksen M, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ.

Nat Chem Biol. 2015 Aug;11(8):536-41. doi: 10.1038/nchembio.1867. No abstract available. Erratum in: Nat Chem Biol. 2015 Nov;11(11):887. Nat Chem Biol. 2015 Aug;11(8):541. Roth, Brian [Corrected to Roth, Bryan] and Frederiksen, Mathias [Added].

14.

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH.

J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6.

15.

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS).

Drewry DH, Willson TM, Zuercher WJ.

Curr Top Med Chem. 2014;14(3):340-2. Review.

16.

Optimized chemical probes for REV-ERBα.

Trump RP, Bresciani S, Cooper AW, Tellam JP, Wojno J, Blaikley J, Orband-Miller LA, Kashatus JA, Boudjelal M, Dawson HC, Loudon A, Ray D, Grant D, Farrow SN, Willson TM, Tomkinson NC.

J Med Chem. 2013 Jun 13;56(11):4729-37. doi: 10.1021/jm400458q. Epub 2013 May 23.

17.

A public-private partnership to unlock the untargeted kinome.

Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ.

Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. No abstract available.

PMID:
23238671
18.

The importance of chronobiology to drug discovery.

Farrow SN, Solari R, Willson TM.

Expert Opin Drug Discov. 2012 Jul;7(7):535-41. doi: 10.1517/17460441.2012.689283. Epub 2012 Jun 2.

PMID:
22657273
19.

Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist.

Sime M, Allan AC, Chapman P, Fieldhouse C, Giblin GM, Healy MP, Lambert MH, Leesnitzer LM, Lewis A, Merrihew RV, Rutter RA, Sasse R, Shearer BG, Willson TM, Xu RX, Virley DJ.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5568-72. doi: 10.1016/j.bmcl.2011.06.088. Epub 2011 Jun 29. Erratum in: Bioorg Med Chem Lett. 2013 Feb 15;23(4):1143. Wilson, Timothy M [corrected to Willson, Timothy M].

PMID:
21798739
20.

Ligand-dependent regulation of the activity of the orphan nuclear receptor, small heterodimer partner (SHP), in the repression of bile acid biosynthetic CYP7A1 and CYP8B1 genes.

Miao J, Choi SE, Seok SM, Yang L, Zuercher WJ, Xu Y, Willson TM, Xu HE, Kemper JK.

Mol Endocrinol. 2011 Jul;25(7):1159-69. doi: 10.1210/me.2011-0033. Epub 2011 May 12.

21.

Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2).

Whitby RJ, Stec J, Blind RD, Dixon S, Leesnitzer LM, Orband-Miller LA, Williams SP, Willson TM, Xu R, Zuercher WJ, Cai F, Ingraham HA.

J Med Chem. 2011 Apr 14;54(7):2266-81. doi: 10.1021/jm1014296. Epub 2011 Mar 10.

22.

Too many roads not taken.

Edwards AM, Isserlin R, Bader GD, Frye SV, Willson TM, Yu FH.

Nature. 2011 Feb 10;470(7333):163-5. doi: 10.1038/470163a. No abstract available.

PMID:
21307913
23.

A new, highly selective murine peroxisome proliferator-activated receptor δ agonist increases responsiveness to thermogenic stimuli and glucose uptake in skeletal muscle in obese mice.

Ngala RA, Stocker CJ, Roy AG, Hislop D, Wargent E, Bell R, Hassall DG, Harling JD, Billin AN, Willson TM, Arch JR, Cawthorne MA.

Diabetes Obes Metab. 2011 May;13(5):455-64. doi: 10.1111/j.1463-1326.2011.01371.x. Epub 2011 Jan 27.

PMID:
21272187
24.

GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

Grant D, Yin L, Collins JL, Parks DJ, Orband-Miller LA, Wisely GB, Joshi S, Lazar MA, Willson TM, Zuercher WJ.

ACS Chem Biol. 2010 Oct 15;5(10):925-32. doi: 10.1021/cb100141y.

PMID:
20677822
25.

Discovery of tertiary sulfonamides as potent liver X receptor antagonists.

Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM.

J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p.

PMID:
20345102
26.

Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.

Shearer BG, Wiethe RW, Ashe A, Billin AN, Way JM, Stanley TB, Wagner CD, Xu RX, Leesnitzer LM, Merrihew RV, Shearer TW, Jeune MR, Ulrich JC, Willson TM.

J Med Chem. 2010 Feb 25;53(4):1857-61. doi: 10.1021/jm900464j.

PMID:
20128594
27.

Identification of novel pathways that control farnesoid X receptor-mediated hypocholesterolemia.

Zhang Y, Yin L, Anderson J, Ma H, Gonzalez FJ, Willson TM, Edwards PA.

J Biol Chem. 2010 Jan 29;285(5):3035-43. doi: 10.1074/jbc.M109.083899. Epub 2009 Dec 7.

28.

Chemical approaches to nuclear receptors in metabolism.

Margolis RN, Moore DD, Willson TM, Guy RK.

Sci Signal. 2009 Aug 4;2(82):mr5. doi: 10.1126/scisignal.282mr5.

29.

Open access chemical and clinical probes to support drug discovery.

Edwards AM, Bountra C, Kerr DJ, Willson TM.

Nat Chem Biol. 2009 Jul;5(7):436-40. doi: 10.1038/nchembio0709-436.

PMID:
19536100
30.

Differential presentation of protein interaction surfaces on the androgen receptor defines the pharmacological actions of bound ligands.

Norris JD, Joseph JD, Sherk AB, Juzumiene D, Turnbull PS, Rafferty SW, Cui H, Anderson E, Fan D, Dye DA, Deng X, Kazmin D, Chang CY, Willson TM, McDonnell DP.

Chem Biol. 2009 Apr 24;16(4):452-60. doi: 10.1016/j.chembiol.2009.01.016.

31.

The p300 acetylase is critical for ligand-activated farnesoid X receptor (FXR) induction of SHP.

Fang S, Tsang S, Jones R, Ponugoti B, Yoon H, Wu SY, Chiang CM, Willson TM, Kemper JK.

J Biol Chem. 2008 Dec 12;283(50):35086-95. doi: 10.1074/jbc.M803531200. Epub 2008 Oct 8.

32.

Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.

Chao EY, Caravella JA, Watson MA, Campobasso N, Ghisletti S, Billin AN, Galardi C, Wang P, Laffitte BA, Iannone MA, Goodwin BJ, Nichols JA, Parks DJ, Stewart E, Wiethe RW, Williams SP, Smallwood A, Pearce KH, Glass CK, Willson TM, Zuercher WJ, Collins JL.

J Med Chem. 2008 Sep 25;51(18):5758-65. doi: 10.1021/jm800612u.

PMID:
18800767
33.

Liver X receptor agonists increase airway reactivity in a model of asthma via increasing airway smooth muscle growth.

Birrell MA, De Alba J, Catley MC, Hardaker E, Wong S, Collins M, Clarke DL, Farrow SN, Willson TM, Collins JL, Belvisi MG.

J Immunol. 2008 Sep 15;181(6):4265-71.

34.

Discovery of a novel class of PPARdelta partial agonists.

Shearer BG, Patel HS, Billin AN, Way JM, Winegar DA, Lambert MH, Xu RX, Leesnitzer LM, Merrihew RV, Huet S, Willson TM.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5018-22. doi: 10.1016/j.bmcl.2008.08.011. Epub 2008 Aug 9.

PMID:
18722772
35.

Selective partial agonism of liver X receptor alpha is related to differential corepressor recruitment.

Phelan CA, Weaver JM, Steger DJ, Joshi S, Maslany JT, Collins JL, Zuercher WJ, Willson TM, Walker M, Jaye M, Lazar MA.

Mol Endocrinol. 2008 Oct;22(10):2241-9. doi: 10.1210/me.2008-0041. Epub 2008 Jul 31.

36.

ApoE promotes the proteolytic degradation of Abeta.

Jiang Q, Lee CY, Mandrekar S, Wilkinson B, Cramer P, Zelcer N, Mann K, Lamb B, Willson TM, Collins JL, Richardson JC, Smith JD, Comery TA, Riddell D, Holtzman DM, Tontonoz P, Landreth GE.

Neuron. 2008 Jun 12;58(5):681-93. doi: 10.1016/j.neuron.2008.04.010.

37.

The phytoestrogen coumestrol is a naturally occurring antagonist of the human pregnane X receptor.

Wang H, Li H, Moore LB, Johnson MD, Maglich JM, Goodwin B, Ittoop OR, Wisely B, Creech K, Parks DJ, Collins JL, Willson TM, Kalpana GV, Venkatesh M, Xie W, Cho SY, Roboz J, Redinbo M, Moore JT, Mani S.

Mol Endocrinol. 2008 Apr;22(4):838-57. Epub 2007 Dec 20.

38.

Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines.

Girroir EE, Hollingshead HE, Billin AN, Willson TM, Robertson GP, Sharma AK, Amin S, Gonzalez FJ, Peters JM.

Toxicology. 2008 Jan 14;243(1-2):236-43. Epub 2007 Nov 4.

39.

On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.

Hyatt SM, Lockamy EL, Stein RA, McDonnell DP, Miller AB, Orband-Miller LA, Willson TM, Zuercher WJ.

J Med Chem. 2007 Dec 27;50(26):6722-4. Epub 2007 Dec 4.

40.

Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist.

Shearer BG, Steger DJ, Way JM, Stanley TB, Lobe DC, Grillot DA, Iannone MA, Lazar MA, Willson TM, Billin AN.

Mol Endocrinol. 2008 Feb;22(2):523-9. Epub 2007 Nov 1.

41.
42.

Novel role for the liver X nuclear receptor in the suppression of lung inflammatory responses.

Birrell MA, Catley MC, Hardaker E, Wong S, Willson TM, McCluskie K, Leonard T, Farrow SN, Collins JL, Haj-Yahia S, Belvisi MG.

J Biol Chem. 2007 Nov 2;282(44):31882-90. Epub 2007 Aug 31.

43.

Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) ligands do not potentiate growth of human cancer cell lines.

Hollingshead HE, Killins RL, Borland MG, Girroir EE, Billin AN, Willson TM, Sharma AK, Amin S, Gonzalez FJ, Peters JM.

Carcinogenesis. 2007 Dec;28(12):2641-9. Epub 2007 Aug 11.

PMID:
17693664
44.

Co-crystal structure guided array synthesis of PPARgamma inverse agonists.

Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. Epub 2007 May 18.

PMID:
17533125
45.

PPARbeta/delta protects against experimental colitis through a ligand-independent mechanism.

Hollingshead HE, Morimura K, Adachi M, Kennett MJ, Billin AN, Willson TM, Gonzalez FJ, Peters JM.

Dig Dis Sci. 2007 Nov;52(11):2912-9. Epub 2007 Apr 3.

PMID:
17404849
46.

Sweet dreams for LXR.

Lazar MA, Willson TM.

Cell Metab. 2007 Mar;5(3):159-61.

47.

Ligand activation of peroxisome proliferator-activated receptor-beta/delta(PPARbeta/delta) inhibits cell growth of human N/TERT-1 keratinocytes.

Burdick AD, Bility MT, Girroir EE, Billin AN, Willson TM, Gonzalez FJ, Peters JM.

Cell Signal. 2007 Jun;19(6):1163-71. Epub 2007 Jan 3.

48.

Parallel SUMOylation-dependent pathways mediate gene- and signal-specific transrepression by LXRs and PPARgamma.

Ghisletti S, Huang W, Ogawa S, Pascual G, Lin ME, Willson TM, Rosenfeld MG, Glass CK.

Mol Cell. 2007 Jan 12;25(1):57-70.

49.

Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.

Xue Y, Chao E, Zuercher WJ, Willson TM, Collins JL, Redinbo MR.

Bioorg Med Chem. 2007 Mar 1;15(5):2156-66. Epub 2006 Dec 20.

50.

Design and synthesis of an array of selective androgen receptor modulators.

Trump RP, Blanc JB, Stewart EL, Brown PJ, Caivano M, Gray DW, Hoekstra WJ, Willson TM, Han B, Turnbull P.

J Comb Chem. 2007 Jan-Feb;9(1):107-14.

PMID:
17206838

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