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Items: 29

1.

KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice.

Polson ES, Kuchler VB, Abbosh C, Ross EM, Mathew RK, Beard HA, da Silva B, Holding AN, Ballereau S, Chuntharpursat-Bon E, Williams J, Griffiths HBS, Shao H, Patel A, Davies AJ, Droop A, Chumas P, Short SC, Lorger M, Gestwicki JE, Roberts LD, Bon RS, Allison SJ, Zhu S, Markowetz F, Wurdak H.

Sci Transl Med. 2018 Aug 15;10(454). pii: eaar2718. doi: 10.1126/scitranslmed.aar2718.

2.

Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease.

Minard A, Bauer CC, Wright DJ, Rubaiy HN, Muraki K, Beech DJ, Bon RS.

Cells. 2018 Jun 1;7(6). pii: E52. doi: 10.3390/cells7060052. Review.

3.

Na+ entry through heteromeric TRPC4/C1 channels mediates (-)Englerin A-induced cytotoxicity in synovial sarcoma cells.

Muraki K, Ohnishi K, Takezawa A, Suzuki H, Hatano N, Muraki Y, Hamzah N, Foster R, Waldmann H, Nussbaumer P, Christmann M, Bon RS, Beech DJ.

Sci Rep. 2017 Dec 5;7(1):16988. doi: 10.1038/s41598-017-17303-3.

4.

Affimer proteins are versatile and renewable affinity reagents.

Tiede C, Bedford R, Heseltine SJ, Smith G, Wijetunga I, Ross R, AlQallaf D, Roberts AP, Balls A, Curd A, Hughes RE, Martin H, Needham SR, Zanetti-Domingues LC, Sadigh Y, Peacock TP, Tang AA, Gibson N, Kyle H, Platt GW, Ingram N, Taylor T, Coletta LP, Manfield I, Knowles M, Bell S, Esteves F, Maqbool A, Prasad RK, Drinkhill M, Bon RS, Patel V, Goodchild SA, Martin-Fernandez M, Owens RJ, Nettleship JE, Webb ME, Harrison M, Lippiat JD, Ponnambalam S, Peckham M, Smith A, Ferrigno PK, Johnson M, McPherson MJ, Tomlinson DC.

Elife. 2017 Jun 27;6. pii: e24903. doi: 10.7554/eLife.24903.

5.

Pico145 - powerful new tool for TRPC1/4/5 channels.

Rubaiy HN, Ludlow MJ, Bon RS, Beech DJ.

Channels (Austin). 2017 Sep 3;11(5):362-364. doi: 10.1080/19336950.2017.1317485. Epub 2017 Apr 11. No abstract available.

6.

Picomolar, selective, and subtype-specific small-molecule inhibition of TRPC1/4/5 channels.

Rubaiy HN, Ludlow MJ, Henrot M, Gaunt HJ, Miteva K, Cheung SY, Tanahashi Y, Hamzah N, Musialowski KE, Blythe NM, Appleby HL, Bailey MA, McKeown L, Taylor R, Foster R, Waldmann H, Nussbaumer P, Christmann M, Bon RS, Muraki K, Beech DJ.

J Biol Chem. 2017 May 19;292(20):8158-8173. doi: 10.1074/jbc.M116.773556. Epub 2017 Mar 21.

7.

Antibody Mimetics for the Detection of Small Organic Compounds Using a Quartz Crystal Microbalance.

Koutsoumpeli E, Tiede C, Murray J, Tang A, Bon RS, Tomlinson DC, Johnson S.

Anal Chem. 2017 Mar 7;89(5):3051-3058. doi: 10.1021/acs.analchem.6b04790. Epub 2017 Feb 15.

PMID:
28192970
8.

Economical and scalable synthesis of 6-amino-2-cyanobenzothiazole.

Hauser JR, Beard HA, Bayana ME, Jolley KE, Warriner SL, Bon RS.

Beilstein J Org Chem. 2016 Sep 13;12:2019-2025. eCollection 2016.

9.

Trivalent Gd-DOTA reagents for modification of proteins.

Fisher MJ, Williamson DJ, Burslem GM, Plante JP, Manfield IW, Tiede C, Ault JR, Stockley PG, Plein S, Maqbool A, Tomlinson DC, Foster R, Warriner SL, Bon RS.

RSC Adv. 2015 Dec 9;5(116):96194-96200. Epub 2015 Nov 11.

10.

Natural and synthetic flavonoid modulation of TRPC5 channels.

Naylor J, Minard A, Gaunt HJ, Amer MS, Wilson LA, Migliore M, Cheung SY, Rubaiy HN, Blythe NM, Musialowski KE, Ludlow MJ, Evans WD, Green BL, Yang H, You Y, Li J, Fishwick CW, Muraki K, Beech DJ, Bon RS.

Br J Pharmacol. 2016 Feb;173(3):562-74. doi: 10.1111/bph.13387. Epub 2016 Jan 13.

11.

Solid phase synthesis of functionalised SAM-forming alkanethiol-oligoethyleneglycols.

Murray J, Nowak D, Pukenas L, Azhar R, Guillorit M, Wälti C, Critchley K, Johnson S, Bon RS.

J Mater Chem B. 2014 Jun 28;2(24):3741-3744.

12.

In pursuit of small molecule chemistry for calcium-permeable non-selective TRPC channels -- mirage or pot of gold?

Bon RS, Beech DJ.

Br J Pharmacol. 2013 Oct;170(3):459-74. doi: 10.1111/bph.12274. Review.

13.

Inhibition of endothelial cell Ca²⁺ entry and transient receptor potential channels by Sigma-1 receptor ligands.

Amer MS, McKeown L, Tumova S, Liu R, Seymour VA, Wilson LA, Naylor J, Greenhalgh K, Hou B, Majeed Y, Turner P, Sedo A, O'Regan DJ, Li J, Bon RS, Porter KE, Beech DJ.

Br J Pharmacol. 2013 Mar;168(6):1445-55. doi: 10.1111/bph.12041.

14.

Development of selective, potent RabGGTase inhibitors.

Stigter EA, Guo Z, Bon RS, Wu YW, Choidas A, Wolf A, Menninger S, Waldmann H, Blankenfeldt W, Goody RS.

J Med Chem. 2012 Oct 11;55(19):8330-40. doi: 10.1021/jm300624s. Epub 2012 Oct 3.

PMID:
22963166
15.

Psoromic acid is a selective and covalent Rab-prenylation inhibitor targeting autoinhibited RabGGTase.

Deraeve C, Guo Z, Bon RS, Blankenfeldt W, DiLucrezia R, Wolf A, Menninger S, Stigter EA, Wetzel S, Choidas A, Alexandrov K, Waldmann H, Goody RS, Wu YW.

J Am Chem Soc. 2012 May 2;134(17):7384-91. doi: 10.1021/ja211305j. Epub 2012 Apr 22.

PMID:
22480322
16.

Psoromic acid derivatives: a new family of small-molecule pre-mRNA splicing inhibitors discovered by a stage-specific high-throughput in vitro splicing assay.

Samatov TR, Wolf A, Odenwälder P, Bessonov S, Deraeve C, Bon RS, Waldmann H, Lührmann R.

Chembiochem. 2012 Mar 19;13(5):640-4. doi: 10.1002/cbic.201100790. Epub 2012 Feb 14. No abstract available.

PMID:
22334518
17.

Biology-oriented synthesis.

Wetzel S, Bon RS, Kumar K, Waldmann H.

Angew Chem Int Ed Engl. 2011 Nov 11;50(46):10800-26. doi: 10.1002/anie.201007004. Epub 2011 Oct 28. Review.

PMID:
22038946
18.

Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design.

Hedberg C, Dekker FJ, Rusch M, Renner S, Wetzel S, Vartak N, Gerding-Reimers C, Bon RS, Bastiaens PI, Waldmann H.

Angew Chem Int Ed Engl. 2011 Oct 10;50(42):9832-7. doi: 10.1002/anie.201102965. Epub 2011 Sep 9.

PMID:
21905185
19.

A small-molecule screening strategy to identify suppressors of statin myopathy.

Wagner BK, Gilbert TJ, Hanai J, Imamura S, Bodycombe NE, Bon RS, Waldmann H, Clemons PA, Sukhatme VP, Mootha VK.

ACS Chem Biol. 2011 Sep 16;6(9):900-4. doi: 10.1021/cb200206w. Epub 2011 Jul 15.

20.

Structure-guided development of selective RabGGTase inhibitors.

Bon RS, Guo Z, Stigter EA, Wetzel S, Menninger S, Wolf A, Choidas A, Alexandrov K, Blankenfeldt W, Goody RS, Waldmann H.

Angew Chem Int Ed Engl. 2011 May 16;50(21):4957-61. doi: 10.1002/anie.201101210. Epub 2011 Apr 21. No abstract available.

PMID:
21520375
21.

Bioactivity-guided navigation of chemical space.

Bon RS, Waldmann H.

Acc Chem Res. 2010 Aug 17;43(8):1103-14. doi: 10.1021/ar100014h.

PMID:
20481515
22.

Design, synthesis, and characterization of peptide-based rab geranylgeranyl transferase inhibitors.

Tan KT, Guiu-Rozas E, Bon RS, Guo Z, Delon C, Wetzel S, Arndt S, Alexandrov K, Waldmann H, Goody RS, Wu YW, Blankenfeldt W.

J Med Chem. 2009 Dec 24;52(24):8025-37. doi: 10.1021/jm901117d.

PMID:
19894725
23.

Analysis of the eukaryotic prenylome by isoprenoid affinity tagging.

Nguyen UT, Guo Z, Delon C, Wu Y, Deraeve C, Fränzel B, Bon RS, Blankenfeldt W, Goody RS, Waldmann H, Wolters D, Alexandrov K.

Nat Chem Biol. 2009 Apr;5(4):227-35. doi: 10.1038/nchembio.149. Epub 2009 Feb 15.

PMID:
19219049
24.

Development of selective RabGGTase inhibitors and crystal structure of a RabGGTase-inhibitor complex.

Guo Z, Wu YW, Tan KT, Bon RS, Guiu-Rozas E, Delon C, Nguyen TU, Wetzel S, Arndt S, Goody RS, Blankenfeldt W, Alexandrov K, Waldmann H.

Angew Chem Int Ed Engl. 2008;47(20):3747-50. doi: 10.1002/anie.200705795. No abstract available.

PMID:
18399557
25.

Efficient C2 functionalisation of 2H-2-imidazolines.

Bon RS, Sprenkels NE, Koningstein MM, Schmitz RF, de Kanter FJ, Dömling A, Groen MB, Orru RV.

Org Biomol Chem. 2008 Jan 7;6(1):130-7. Epub 2007 Nov 8.

PMID:
18075657
26.

Diastereoselective multicomponent synthesis of dihydropyridones with an isocyanide functionality.

Paravidino M, Bon RS, Scheffelaar R, Vugts DJ, Znabet A, Schmitz RF, de Kanter FJ, Lutz M, Spek AL, Groen MB, Orru RV.

Org Lett. 2006 Nov 9;8(23):5369-72.

PMID:
17078720
27.

Multicomponent synthesis of 2-imidazolines.

Bon RS, van Vliet B, Sprenkels NE, Schmitz RF, de Kanter FJ, Stevens CV, Swart M, Bickelhaupt FM, Groen MB, Orru RV.

J Org Chem. 2005 Apr 29;70(9):3542-53.

PMID:
15844989
28.

Novel multicomponent reaction for the combinatorial synthesis of 2-imidazolines.

Bon RS, Hong C, Bouma MJ, Schmitz RF, de Kanter FJ, Lutz M, Spek AL, Orru RV.

Org Lett. 2003 Oct 2;5(20):3759-62.

PMID:
14507224
29.

Synthesis of 2,6-bridged piperazine-3-ones by N-acyliminium ion chemistry.

Veerman JJ, Bon RS, Hue BT, Girones D, Rutjes FP, van Maarseveen JH, Hiemstra H.

J Org Chem. 2003 May 30;68(11):4486-94.

PMID:
12762754

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