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Items: 41

1.

Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics.

Tyagi R, Elfawal MA, Wildman SA, Helander J, Bulman CA, Sakanari J, Rosa BA, Brindley PJ, Janetka JW, Aroian RV, Mitreva M.

Sci Rep. 2019 Jun 24;9(1):9085. doi: 10.1038/s41598-019-45548-7.

2.

Recent progress on inhibitors of the type II transmembrane serine proteases, hepsin, matriptase and matriptase-2.

Damalanka VC, Janetka JW.

Future Med Chem. 2019 Apr;11(7):743-769. doi: 10.4155/fmc-2018-0446. Epub 2019 Apr 4.

PMID:
30945556
3.

Hepatocyte growth factor activator inhibitor-2 stabilizes Epcam and maintains epithelial organization in the mouse intestine.

Kawaguchi M, Yamamoto K, Takeda N, Fukushima T, Yamashita F, Sato K, Kitamura K, Hippo Y, Janetka JW, Kataoka H.

Commun Biol. 2019 Jan 4;2:11. doi: 10.1038/s42003-018-0255-8. eCollection 2019.

4.

Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology.

Damalanka VC, Han Z, Karmakar P, O'Donoghue AJ, La Greca F, Kim T, Pant SM, Helander J, Klefström J, Craik CS, Janetka JW.

J Med Chem. 2019 Jan 24;62(2):480-490. doi: 10.1021/acs.jmedchem.8b01536. Epub 2019 Jan 4.

PMID:
30571119
5.

Biphenyl Gal and GalNAc FmlH Lectin Antagonists of Uropathogenic E. coli (UPEC): Optimization through Iterative Rational Drug Design.

Maddirala AR, Klein R, Pinkner JS, Kalas V, Hultgren SJ, Janetka JW.

J Med Chem. 2019 Jan 24;62(2):467-479. doi: 10.1021/acs.jmedchem.8b01561. Epub 2019 Jan 2.

PMID:
30540910
6.

Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics.

Tyagi R, Maddirala AR, Elfawal M, Fischer C, Bulman CA, Rosa BA, Gao X, Chugani R, Zhou M, Helander J, Brindley PJ, Tseng CC, Greig IR, Sakanari J, Wildman SA, Aroian R, Janetka JW, Mitreva M.

ACS Infect Dis. 2018 Jul 13;4(7):1130-1145. doi: 10.1021/acsinfecdis.8b00090. Epub 2018 May 14.

7.

MFN2 agonists reverse mitochondrial defects in preclinical models of Charcot-Marie-Tooth disease type 2A.

Rocha AG, Franco A, Krezel AM, Rumsey JM, Alberti JM, Knight WC, Biris N, Zacharioudakis E, Janetka JW, Baloh RH, Kitsis RN, Mochly-Rosen D, Townsend RR, Gavathiotis E, Dorn GW 2nd.

Science. 2018 Apr 20;360(6386):336-341. doi: 10.1126/science.aao1785.

8.

Precision antimicrobial therapeutics: the path of least resistance?

Spaulding CN, Klein RD, Schreiber HL 4th, Janetka JW, Hultgren SJ.

NPJ Biofilms Microbiomes. 2018 Feb 27;4:4. doi: 10.1038/s41522-018-0048-3. eCollection 2018. Review.

9.

Structure-based discovery of glycomimetic FmlH ligands as inhibitors of bacterial adhesion during urinary tract infection.

Kalas V, Hibbing ME, Maddirala AR, Chugani R, Pinkner JS, Mydock-McGrane LK, Conover MS, Janetka JW, Hultgren SJ.

Proc Natl Acad Sci U S A. 2018 Mar 20;115(12):E2819-E2828. doi: 10.1073/pnas.1720140115. Epub 2018 Mar 5.

10.

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Yang B, Vasbinder MM, Hird AW, Su Q, Wang H, Yu Y, Toader D, Lyne PD, Read JA, Breed J, Ioannidis S, Deng C, Grondine M, DeGrace N, Whitston D, Brassil P, Janetka JW.

J Med Chem. 2018 Feb 8;61(3):1061-1073. doi: 10.1021/acs.jmedchem.7b01490. Epub 2018 Jan 19.

PMID:
29301085
11.

Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation.

Owusu BY, Thomas S, Venukadasula P, Han Z, Janetka JW, Galemmo RA Jr, Klampfer L.

Oncotarget. 2017 May 29;8(38):63014-63025. doi: 10.18632/oncotarget.18260. eCollection 2017 Sep 8.

12.

Inhibition of Calcium Dependent Protein Kinase 1 (CDPK1) by Pyrazolopyrimidine Analogs Decreases Establishment and Reoccurrence of Central Nervous System Disease by Toxoplasma gondii.

Rutaganira FU, Barks J, Dhason MS, Wang Q, Lopez MS, Long S, Radke JB, Jones NG, Maddirala AR, Janetka JW, El Bakkouri M, Hui R, Shokat KM, Sibley LD.

J Med Chem. 2017 Dec 28;60(24):9976-9989. doi: 10.1021/acs.jmedchem.7b01192. Epub 2017 Oct 9.

13.

Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist.

Spaulding CN, Klein RD, Ruer S, Kau AL, Schreiber HL, Cusumano ZT, Dodson KW, Pinkner JS, Fremont DH, Janetka JW, Remaut H, Gordon JI, Hultgren SJ.

Nature. 2017 Jun 22;546(7659):528-532. doi: 10.1038/nature22972. Epub 2017 Jun 14.

14.

Rational design strategies for FimH antagonists: new drugs on the horizon for urinary tract infection and Crohn's disease.

Mydock-McGrane LK, Hannan TJ, Janetka JW.

Expert Opin Drug Discov. 2017 Jul;12(7):711-731. doi: 10.1080/17460441.2017.1331216. Epub 2017 Jun 2. Review.

15.

Photoaffinity labeling with cholesterol analogues precisely maps a cholesterol-binding site in voltage-dependent anion channel-1.

Budelier MM, Cheng WWL, Bergdoll L, Chen ZW, Janetka JW, Abramson J, Krishnan K, Mydock-McGrane L, Covey DF, Whitelegge JP, Evers AS.

J Biol Chem. 2017 Jun 2;292(22):9294-9304. doi: 10.1074/jbc.M116.773069. Epub 2017 Apr 10.

16.

Click Chemistry Reagent for Identification of Sites of Covalent Ligand Incorporation in Integral Membrane Proteins.

Budelier MM, Cheng WW, Bergdoll L, Chen ZW, Abramson J, Krishnan K, Qian M, Covey DF, Janetka JW, Evers AS.

Anal Chem. 2017 Feb 21;89(4):2636-2644. doi: 10.1021/acs.analchem.6b05003. Epub 2017 Feb 9.

17.

Antivirulence C-Mannosides as Antibiotic-Sparing, Oral Therapeutics for Urinary Tract Infections.

Mydock-McGrane L, Cusumano Z, Han Z, Binkley J, Kostakioti M, Hannan T, Pinkner JS, Klein R, Kalas V, Crowley J, Rath NP, Hultgren SJ, Janetka JW.

J Med Chem. 2016 Oct 27;59(20):9390-9408. Epub 2016 Oct 14.

18.

α-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer.

Han Z, Harris PK, Karmakar P, Kim T, Owusu BY, Wildman SA, Klampfer L, Janetka JW.

ChemMedChem. 2016 Mar 17;11(6):585-99. doi: 10.1002/cmdc.201500600. Epub 2016 Feb 17.

PMID:
26889658
19.

Characterization of parasite-specific indels and their proposed relevance for selective anthelminthic drug targeting.

Wang Q, Heizer E, Rosa BA, Wildman SA, Janetka JW, Mitreva M.

Infect Genet Evol. 2016 Apr;39:201-211. doi: 10.1016/j.meegid.2016.01.025. Epub 2016 Jan 30.

20.

Antivirulence Isoquinolone Mannosides: Optimization of the Biaryl Aglycone for FimH Lectin Binding Affinity and Efficacy in the Treatment of Chronic UTI.

Jarvis C, Han Z, Kalas V, Klein R, Pinkner JS, Ford B, Binkley J, Cusumano CK, Cusumano Z, Mydock-McGrane L, Hultgren SJ, Janetka JW.

ChemMedChem. 2016 Feb 17;11(4):367-73. doi: 10.1002/cmdc.201600006. Epub 2016 Jan 26.

21.

Mannose-derived FimH antagonists: a promising anti-virulence therapeutic strategy for urinary tract infections and Crohn's disease.

Mydock-McGrane LK, Cusumano ZT, Janetka JW.

Expert Opin Ther Pat. 2016;26(2):175-97. doi: 10.1517/13543776.2016.1131266. Epub 2016 Jan 22. Review.

PMID:
26651364
22.

Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.

Franco FM, Jones DE, Harris PK, Han Z, Wildman SA, Jarvis CM, Janetka JW.

Bioorg Med Chem. 2015 May 15;23(10):2328-43. doi: 10.1016/j.bmc.2015.03.072. Epub 2015 Apr 4.

PMID:
25882520
23.

Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.

Han Z, Harris PK, Jones DE, Chugani R, Kim T, Agarwal M, Shen W, Wildman SA, Janetka JW.

ACS Med Chem Lett. 2014 Oct 9;5(11):1219-24. doi: 10.1021/ml500254r. eCollection 2014 Nov 13.

24.

A FimH inhibitor prevents acute bladder infection and treats chronic cystitis caused by multidrug-resistant uropathogenic Escherichia coli ST131.

Totsika M, Kostakioti M, Hannan TJ, Upton M, Beatson SA, Janetka JW, Hultgren SJ, Schembri MA.

J Infect Dis. 2013 Sep;208(6):921-8. doi: 10.1093/infdis/jit245. Epub 2013 Jun 3.

25.

Combinatorial small-molecule therapy prevents uropathogenic Escherichia coli catheter-associated urinary tract infections in mice.

Guiton PS, Cusumano CK, Kline KA, Dodson KW, Han Z, Janetka JW, Henderson JP, Caparon MG, Hultgren SJ.

Antimicrob Agents Chemother. 2012 Sep;56(9):4738-45. doi: 10.1128/AAC.00447-12. Epub 2012 Jun 25.

26.

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.

Yang B, Hird AW, Russell DJ, Fauber BP, Dakin LA, Zheng X, Su Q, Godin R, Brassil P, Devereaux E, Janetka JW.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4907-11. doi: 10.1016/j.bmcl.2012.04.104. Epub 2012 Apr 30.

PMID:
22704236
27.

Distinguishing the contribution of type 1 pili from that of other QseB-misregulated factors when QseC is absent during urinary tract infection.

Kostakioti M, Hadjifrangiskou M, Cusumano CK, Hannan TJ, Janetka JW, Hultgren SJ.

Infect Immun. 2012 Aug;80(8):2826-34. doi: 10.1128/IAI.00283-12. Epub 2012 Jun 4.

28.

Lead optimization studies on FimH antagonists: discovery of potent and orally bioavailable ortho-substituted biphenyl mannosides.

Han Z, Pinkner JS, Ford B, Chorell E, Crowley JM, Cusumano CK, Campbell S, Henderson JP, Hultgren SJ, Janetka JW.

J Med Chem. 2012 Apr 26;55(8):3945-59. doi: 10.1021/jm300165m. Epub 2012 Apr 13.

29.

Treatment and prevention of urinary tract infection with orally active FimH inhibitors.

Cusumano CK, Pinkner JS, Han Z, Greene SE, Ford BA, Crowley JR, Henderson JP, Janetka JW, Hultgren SJ.

Sci Transl Med. 2011 Nov 16;3(109):109ra115. doi: 10.1126/scitranslmed.3003021.

30.

Death by releasing the breaks: CHK1 inhibitors as cancer therapeutics.

Ma CX, Janetka JW, Piwnica-Worms H.

Trends Mol Med. 2011 Feb;17(2):88-96. doi: 10.1016/j.molmed.2010.10.009. Epub 2010 Nov 17. Review.

PMID:
21087899
31.

Structure-based drug design and optimization of mannoside bacterial FimH antagonists.

Han Z, Pinkner JS, Ford B, Obermann R, Nolan W, Wildman SA, Hobbs D, Ellenberger T, Cusumano CK, Hultgren SJ, Janetka JW.

J Med Chem. 2010 Jun 24;53(12):4779-92. doi: 10.1021/jm100438s.

32.

Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.

Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Markland W, Namchuk MN, Nanthakumar S, Poondru S, Straub J, ter Haar E, Xie X.

J Med Chem. 2009 Oct 22;52(20):6362-8. doi: 10.1021/jm900630q.

PMID:
19827834
33.

Checkpoint kinase inhibitors: a review of the patent literature.

Janetka JW, Ashwell S.

Expert Opin Ther Pat. 2009 Feb;19(2):165-97. doi: 10.1517/13543770802653622. Review.

PMID:
19441917
34.

AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies.

Zabludoff SD, Deng C, Grondine MR, Sheehy AM, Ashwell S, Caleb BL, Green S, Haye HR, Horn CL, Janetka JW, Liu D, Mouchet E, Ready S, Rosenthal JL, Queva C, Schwartz GK, Taylor KJ, Tse AN, Walker GE, White AM.

Mol Cancer Ther. 2008 Sep;7(9):2955-66. doi: 10.1158/1535-7163.MCT-08-0492.

35.

Keeping checkpoint kinases in line: new selective inhibitors in clinical trials.

Ashwell S, Janetka JW, Zabludoff S.

Expert Opin Investig Drugs. 2008 Sep;17(9):1331-40. doi: 10.1517/13543784.17.9.1331 . Review.

PMID:
18694366
36.

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.

Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4242-8. doi: 10.1016/j.bmcl.2008.05.016. Epub 2008 May 6.

PMID:
18547806
37.

Inhibitors of checkpoint kinases: from discovery to the clinic.

Janetka JW, Ashwell S, Zabludoff S, Lyne P.

Curr Opin Drug Discov Devel. 2007 Jul;10(4):473-86. Review.

PMID:
17659489
38.

Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.

Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X.

J Med Chem. 2007 Mar 22;50(6):1280-7. Epub 2007 Feb 15.

PMID:
17300186
40.

Enantioconvergent synthesis of (-)-(2R,5S)-1-allyl-2,5-dimethylpiperazine, an intermediate to delta-opioid receptor ligands.

Janetka JW, Furness MS, Zhang X, Coop A, Folk JE, Mattson MV, Jacobson AE, Rice KC.

J Org Chem. 2003 May 16;68(10):3976-80.

PMID:
12737580
41.

A cyclic side-chain-linked biphenyl ether tripeptide: H3N(+)-cyclo-[Phe(4-O)Phe-Phe(3-O)]-OMe.Cl-.

Janetka JW, Satyshur KA, Rich DH.

Acta Crystallogr C. 1996 Dec 15;52 ( Pt 12):3112-4.

PMID:
9015901

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