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Items: 1 to 50 of 94

1.

Identification of Pirin as a Molecular Target of the CCG-1423/CCG-203971 Series of Antifibrotic and Antimetastatic Compounds.

Lisabeth EM, Kahl D, Gopallawa I, Haynes SE, Misek SA, Campbell PL, Dexheimer TS, Khanna D, Fox DA, Jin X, Martin BR, Larsen SD, Neubig RR.

ACS Pharmacol Transl Sci. 2019 Apr 12;2(2):92-100. doi: 10.1021/acsptsci.8b00048. Epub 2019 Mar 18.

2.

Discovery and Optimization of Triazine Nitrile Inhibitors of Toxoplasma gondii Cathepsin L for the Potential Treatment of Chronic Toxoplasmosis in the CNS.

Zwicker JD, Smith D, Guerra AJ, Hitchens JR, Haug N, Vander Roest S, Lee P, Wen B, Sun D, Wang L, Keep R, Xiang J, Carruthers VB, Larsen SD.

ACS Chem Neurosci. 2020 Feb 6. doi: 10.1021/acschemneuro.9b00674. [Epub ahead of print]

PMID:
32027110
3.

Pre- and Post-Race Intestinal Microbiota in Long-Distance Sled Dogs and Associations with Performance.

Tysnes KR, Angell IL, Fjellanger I, Larsen SD, Søfteland SR, Robertson LJ, Skancke E, Rudi K.

Animals (Basel). 2020 Jan 25;10(2). pii: E204. doi: 10.3390/ani10020204.

4.

The Rate of Infectious Complications After Intrathecal Drug Delivery System Implant for Cancer-Related Pain Is Low Despite Frequent Concurrent Anticancer Treatment or Leukopenia.

Sindt JE, Larsen SD, Dalley AP, Collier WH, Brogan SE.

Anesth Analg. 2020 Jan 23. doi: 10.1213/ANE.0000000000004639. [Epub ahead of print]

PMID:
31990731
5.

Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.

Rowlands RA, Cato MC, Waldschmidt HV, Bouley RA, Chen Q, Avramova L, Larsen SD, Tesmer JJG, White AD.

ACS Med Chem Lett. 2019 Nov 12;10(12):1628-1634. doi: 10.1021/acsmedchemlett.9b00365. eCollection 2019 Dec 12.

PMID:
31857838
6.

Rho-mediated signaling promotes BRAF inhibitor resistance in de-differentiated melanoma cells.

Misek SA, Appleton KM, Dexheimer TS, Lisabeth EM, Lo RS, Larsen SD, Gallo KA, Neubig RR.

Oncogene. 2020 Feb;39(7):1466-1483. doi: 10.1038/s41388-019-1074-1. Epub 2019 Oct 28.

PMID:
31659259
7.

Pregnancy or cord 25-hydroxyvitamin D is not associated with measures of body fat or adiposity in children from three months to three years of age. An Odense Child Cohort study.

Larsen SD, Christensen ME, Dalgård C, Lykkedegn S, Andersen LB, Andersen MS, Glintborg D, Christesen HT.

Clin Nutr. 2019 Aug 8. pii: S0261-5614(19)30305-X. doi: 10.1016/j.clnu.2019.07.023. [Epub ahead of print]

PMID:
31471164
8.

Correction to "Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine".

Waldschmidt HV, Homan KT, Cato MC, Cruz-Rodríguez O, Cannavo A, Wilson MW, Song J, Cheung JY, Koch WJ, Tesmer JJG, Larsen SD.

J Med Chem. 2019 Jun 27;62(12):5920. doi: 10.1021/acs.jmedchem.9b00844. Epub 2019 Jun 12. No abstract available.

PMID:
31188593
9.

5-Aryl-1,3,4-oxadiazol-2-ylthioalkanoic Acids: A Highly Potent New Class of Inhibitors of Rho/Myocardin-Related Transcription Factor (MRTF)/Serum Response Factor (SRF)-Mediated Gene Transcription as Potential Antifibrotic Agents for Scleroderma.

Kahl DJ, Hutchings KM, Lisabeth EM, Haak AJ, Leipprandt JR, Dexheimer T, Khanna D, Tsou PS, Campbell PL, Fox DA, Wen B, Sun D, Bailie M, Neubig RR, Larsen SD.

J Med Chem. 2019 May 9;62(9):4350-4369. doi: 10.1021/acs.jmedchem.8b01772. Epub 2019 Apr 18.

10.

A Pan-ALDH1A Inhibitor Induces Necroptosis in Ovarian Cancer Stem-like Cells.

Chefetz I, Grimley E, Yang K, Hong L, Vinogradova EV, Suciu R, Kovalenko I, Karnak D, Morgan CA, Chtcherbinine M, Buchman C, Huddle B, Barraza S, Morgan M, Bernstein KA, Yoon E, Lombard DB, Bild A, Mehta G, Romero I, Chiang CY, Landen C, Cravatt B, Hurley TD, Larsen SD, Buckanovich RJ.

Cell Rep. 2019 Mar 12;26(11):3061-3075.e6. doi: 10.1016/j.celrep.2019.02.032.

11.

Synthesis of deuterium-labelled amlexanox and its metabolic stability against mouse, rat, and human microsomes.

Gan X, Wilson MW, Beyett TS, Wen B, Sun D, Larsen SD, Tesmer JJG, Saltiel AR, Showalter HD.

J Labelled Comp Radiopharm. 2019 May 15;62(5):202-208. doi: 10.1002/jlcr.3716. Epub 2019 Apr 3.

PMID:
30828860
12.

Blood pressure in 3-year-old girls associates inversely with umbilical cord serum 25-hydroxyvitamin D: an Odense Child Cohort study.

Larsen SD, Dalgård C, Christensen ME, Lykkedegn S, Andersen LB, Andersen M, Glintborg D, Christesen HT.

Endocr Connect. 2018 Dec 1;7(12):1236-1244. doi: 10.1530/EC-18-0308.

13.

Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes.

Dumas ME, Chen GY, Kendrick ND, Xu G, Larsen SD, Jana S, Waterson AG, Bauer JA, Hancock W, Sulikowski GA, Ohi R.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):148-154. doi: 10.1016/j.bmcl.2018.12.008. Epub 2018 Dec 4.

14.

In vitro and in vivo delivery of a sustained release nanocarrier-based formulation of an MRTF/SRF inhibitor in conjunctival fibrosis.

Tagalakis AD, Madaan S, Larsen SD, Neubig RR, Khaw PT, Rodrigues I, Goyal S, Lim KS, Yu-Wai-Man C.

J Nanobiotechnology. 2018 Nov 27;16(1):97. doi: 10.1186/s12951-018-0425-3.

15.

PPARγ-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.

Tanis SP, Colca JR, Parker TT, Artman GD 3rd, Larsen SD, McDonald WG, Gadwood RC, Kletzien RF, Zeller JB, Lee PH, Adams WJ.

Bioorg Med Chem. 2018 Dec 1;26(22):5870-5884. doi: 10.1016/j.bmc.2018.10.033. Epub 2018 Nov 2. No abstract available.

PMID:
30429097
16.

Blood pressure in 3-year-old girls associates inversely with umbilical cord serum 25-hydroxyvitamin D.

Larsen SD, Dalgård C, Christensen ME, Lykkedegn S, Andersen LB, Andersen M, Glintborg D, Christesen HT.

Endocr Connect. 2018 Oct 1. pii: /journals/ec/aop/ec-18-0308.xml. doi: 10.1530/EC-18-0308. [Epub ahead of print]

17.

Structure-Based Optimization of a Novel Class of Aldehyde Dehydrogenase 1A (ALDH1A) Subfamily-Selective Inhibitors as Potential Adjuncts to Ovarian Cancer Chemotherapy.

Huddle BC, Grimley E, Buchman CD, Chtcherbinine M, Debnath B, Mehta P, Yang K, Morgan CA, Li S, Felton J, Sun D, Mehta G, Neamati N, Buckanovich RJ, Hurley TD, Larsen SD.

J Med Chem. 2018 Oct 11;61(19):8754-8773. doi: 10.1021/acs.jmedchem.8b00930. Epub 2018 Sep 28.

18.

A novel inverse association between cord 25-hydroxyvitamin D and leg length in boys up to three years. An Odense Child Cohort study.

Christensen ME, Beck-Nielsen SS, Dalgård C, Larsen SD, Lykkedegn S, Kyhl HB, Husby S, Christesen HT.

PLoS One. 2018 Jun 11;13(6):e0198724. doi: 10.1371/journal.pone.0198724. eCollection 2018.

19.

Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.

Zwicker JD, Diaz NA, Guerra AJ, Kirchhoff PD, Wen B, Sun D, Carruthers VB, Larsen SD.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1972-1980. doi: 10.1016/j.bmcl.2018.03.020. Epub 2018 Mar 9.

20.

Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.

Waldschmidt HV, Bouley R, Kirchhoff PD, Lee P, Tesmer JJG, Larsen SD.

Bioorg Med Chem Lett. 2018 May 15;28(9):1507-1515. doi: 10.1016/j.bmcl.2018.03.082. Epub 2018 Mar 30.

21.

Gedunin- and Khivorin-Derivatives Are Small-Molecule Partial Agonists for Adhesion G Protein-Coupled Receptors GPR56/ADGRG1 and GPR114/ADGRG5.

Stoveken HM, Larsen SD, Smrcka AV, Tall GG.

Mol Pharmacol. 2018 May;93(5):477-488. doi: 10.1124/mol.117.111476. Epub 2018 Feb 23.

22.

Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.

Bouley R, Waldschmidt HV, Cato MC, Cannavo A, Song J, Cheung JY, Yao XQ, Koch WJ, Larsen SD, Tesmer JJG.

Mol Pharmacol. 2017 Dec;92(6):707-717. doi: 10.1124/mol.117.110130. Epub 2017 Oct 25.

23.

Minor Structural Variations of Small Molecules Tune Regulatory Activities toward Pathological Factors in Alzheimer's Disease.

Beck MW, Derrick JS, Suh JM, Kim M, Korshavn KJ, Kerr RA, Cho WJ, Larsen SD, Ruotolo BT, Ramamoorthy A, Lim MH.

ChemMedChem. 2017 Nov 22;12(22):1828-1838. doi: 10.1002/cmdc.201700456. Epub 2017 Oct 9.

24.

Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis.

Yu-Wai-Man C, Spencer-Dene B, Lee RMH, Hutchings K, Lisabeth EM, Treisman R, Bailly M, Larsen SD, Neubig RR, Khaw PT.

Sci Rep. 2017 Mar 31;7(1):518. doi: 10.1038/s41598-017-00212-w.

25.

Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors Based on Paroxetine.

Waldschmidt HV, Homan KT, Cato MC, Cruz-Rodríguez O, Cannavo A, Wilson MW, Song J, Cheung JY, Koch WJ, Tesmer JJ, Larsen SD.

J Med Chem. 2017 Apr 13;60(7):3052-3069. doi: 10.1021/acs.jmedchem.7b00112. Epub 2017 Mar 29. Erratum in: J Med Chem. 2019 Jun 27;62(12):5920.

26.

Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.

Hutchings KM, Lisabeth EM, Rajeswaran W, Wilson MW, Sorenson RJ, Campbell PL, Ruth JH, Amin A, Tsou PS, Leipprandt JR, Olson SR, Wen B, Zhao T, Sun D, Khanna D, Fox DA, Neubig RR, Larsen SD.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749. doi: 10.1016/j.bmcl.2017.02.070. Epub 2017 Mar 10.

27.

Histological and clinical evaluation of the hard palate mucous membrane graft for treatment of lower eyelid retraction.

Larsen SD, Heegaard S, Toft PB.

Acta Ophthalmol. 2017 May;95(3):295-298. doi: 10.1111/aos.13321. Epub 2016 Dec 20.

28.

Inhibitors of Mycobacterium tuberculosis DosRST signaling and persistence.

Zheng H, Colvin CJ, Johnson BK, Kirchhoff PD, Wilson M, Jorgensen-Muga K, Larsen SD, Abramovitch RB.

Nat Chem Biol. 2017 Feb;13(2):218-225. doi: 10.1038/nchembio.2259. Epub 2016 Dec 19.

PMID:
27992879
29.

Optimisation of Intestinal Fibrosis and Survival in the Mouse S. Typhimurium Model for Anti-fibrotic Drug Discovery and Preclinical Applications.

Johnson LA, Rodansky ES, Moons DS, Larsen SD, Neubig RR, Higgins PDR.

J Crohns Colitis. 2017 Jun 1;11(6):724-736. doi: 10.1093/ecco-jcc/jjw210.

30.

Pharmacological Inhibition of Myocardin-related Transcription Factor Pathway Blocks Lung Metastases of RhoC-Overexpressing Melanoma.

Haak AJ, Appleton KM, Lisabeth EM, Misek SA, Ji Y, Wade SM, Bell JL, Rockwell CE, Airik M, Krook MA, Larsen SD, Verhaegen M, Lawlor ER, Neubig RR.

Mol Cancer Ther. 2017 Jan;16(1):193-204. doi: 10.1158/1535-7163.MCT-16-0482. Epub 2016 Nov 11.

31.

Structure-mechanism-based engineering of chemical regulators targeting distinct pathological factors in Alzheimer's disease.

Beck MW, Derrick JS, Kerr RA, Oh SB, Cho WJ, Lee SJ, Ji Y, Han J, Tehrani ZA, Suh N, Kim S, Larsen SD, Kim KS, Lee JY, Ruotolo BT, Lim MH.

Nat Commun. 2016 Oct 13;7:13115. doi: 10.1038/ncomms13115.

32.

CARP-1 functional mimetics are novel inhibitors of drug-resistant triple negative breast cancers.

Cheriyan VT, Muthu M, Patel K, Sekhar S, Rajeswaran W, Larsen SD, Polin L, Levi E, Singh M, Rishi AK.

Oncotarget. 2016 Nov 8;7(45):73370-73388. doi: 10.18632/oncotarget.12333.

33.

Blockade of the renin-angiotensin system prevents acute and immunologically relevant colitis in murine models.

Okawada M, Wilson MW, Larsen SD, Lipka E, Hillfinger J, Teitelbaum DH.

Pediatr Surg Int. 2016 Dec;32(12):1103-1114. Epub 2016 Sep 26.

PMID:
27670279
34.

Occludin S471 Phosphorylation Contributes to Epithelial Monolayer Maturation.

Bolinger MT, Ramshekar A, Waldschmidt HV, Larsen SD, Bewley MC, Flanagan JM, Antonetti DA.

Mol Cell Biol. 2016 Jul 14;36(15):2051-66. doi: 10.1128/MCB.00053-16. Print 2016 Aug 1.

35.

Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.

Waldschmidt HV, Homan KT, Cruz-Rodríguez O, Cato MC, Waninger-Saroni J, Larimore KM, Cannavo A, Song J, Cheung JY, Kirchhoff PD, Koch WJ, Tesmer JJ, Larsen SD.

J Med Chem. 2016 Apr 28;59(8):3793-807. doi: 10.1021/acs.jmedchem.5b02000. Epub 2016 Apr 13.

36.

Identification and Testing of Novel CARP-1 Functional Mimetic Compounds as Inhibitors of Non-Small Cell Lung and Triple Negative Breast Cancers.

Muthu M, Somagoni J, Cheriyan VT, Munie S, Levi E, Ashour AE, Yassin AE, Alafeefy AM, Sochacki P, Polin LA, Reddy KB, Larsen SD, Singh M, Rishi AK.

J Biomed Nanotechnol. 2015 Sep;11(9):1608-27.

37.

Massive Bioaccumulation and Self-Assembly of Phenazine Compounds in Live Cells.

Min KA, Rajeswaran WG, Oldenbourg R, Harris G, Keswani RK, Chiang M, Rzeczycki P, Talattof A, Hafeez M, Horobin RW, Larsen SD, Stringer KA, Rosania GR.

Adv Sci (Weinh). 2015 Aug;2(8). pii: 1500025.

38.

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.

Homan KT, Waldschmidt HV, Glukhova A, Cannavo A, Song J, Cheung JY, Koch WJ, Larsen SD, Tesmer JJ.

J Biol Chem. 2015 Aug 21;290(34):20649-59. doi: 10.1074/jbc.M115.647370. Epub 2015 Jun 1.

39.

Discovery of anthranilamides as a novel class of inhibitors of neurotropic alphavirus replication.

Barraza SJ, Delekta PC, Sindac JA, Dobry CJ, Xiang J, Keep RF, Miller DJ, Larsen SD.

Bioorg Med Chem. 2015 Apr 1;23(7):1569-87. doi: 10.1016/j.bmc.2015.01.054. Epub 2015 Feb 11.

40.

Inhibition of myocardin-related transcription factor/serum response factor signaling decreases lung fibrosis and promotes mesenchymal cell apoptosis.

Sisson TH, Ajayi IO, Subbotina N, Dodi AE, Rodansky ES, Chibucos LN, Kim KK, Keshamouni VG, White ES, Zhou Y, Higgins PD, Larsen SD, Neubig RR, Horowitz JC.

Am J Pathol. 2015 Apr;185(4):969-86. doi: 10.1016/j.ajpath.2014.12.005. Epub 2015 Feb 11.

41.

A chimeric virus-mouse model system for evaluating the function and inhibition of papain-like proteases of emerging coronaviruses.

Deng X, Agnihothram S, Mielech AM, Nichols DB, Wilson MW, StJohn SE, Larsen SD, Mesecar AD, Lenschow DJ, Baric RS, Baker SC.

J Virol. 2014 Oct;88(20):11825-33. doi: 10.1128/JVI.01749-14. Epub 2014 Aug 6.

42.

Novel indole-2-carboxamide compounds are potent broad-spectrum antivirals active against western equine encephalitis virus in vivo.

Delekta PC, Dobry CJ, Sindac JA, Barraza SJ, Blakely PK, Xiang J, Kirchhoff PD, Keep RF, Irani DN, Larsen SD, Miller DJ.

J Virol. 2014 Oct;88(19):11199-214. doi: 10.1128/JVI.01671-14. Epub 2014 Jul 16.

43.

Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury.

Haak AJ, Tsou PS, Amin MA, Ruth JH, Campbell P, Fox DA, Khanna D, Larsen SD, Neubig RR.

J Pharmacol Exp Ther. 2014 Jun;349(3):480-6. doi: 10.1124/jpet.114.213520. Epub 2014 Apr 4.

44.

X-ray structural and biological evaluation of a series of potent and highly selective inhibitors of human coronavirus papain-like proteases.

Báez-Santos YM, Barraza SJ, Wilson MW, Agius MP, Mielech AM, Davis NM, Baker SC, Larsen SD, Mesecar AD.

J Med Chem. 2014 Mar 27;57(6):2393-412. doi: 10.1021/jm401712t. Epub 2014 Mar 14.

45.

Development of tag-free photoprobes for studies aimed at identifying the target of novel Group A Streptococcus antivirulence agents.

Yestrepsky BD, Kretz CA, Xu Y, Holmes A, Sun H, Ginsburg D, Larsen SD.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1538-44. doi: 10.1016/j.bmcl.2014.01.079. Epub 2014 Feb 7.

46.

The development and use of small molecule inhibitors of glycosphingolipid metabolism for lysosomal storage diseases.

Shayman JA, Larsen SD.

J Lipid Res. 2014 Jul;55(7):1215-25. doi: 10.1194/jlr.R047167. Epub 2014 Feb 17. Review.

47.

Redox modification of nuclear actin by MICAL-2 regulates SRF signaling.

Lundquist MR, Storaska AJ, Liu TC, Larsen SD, Evans T, Neubig RR, Jaffrey SR.

Cell. 2014 Jan 30;156(3):563-76. doi: 10.1016/j.cell.2013.12.035. Epub 2014 Jan 16.

48.

The role of HTS in drug discovery at the University of Michigan.

Larsen MJ, Larsen SD, Fribley A, Grembecka J, Homan K, Mapp A, Haak A, Nikolovska-Coleska Z, Stuckey JA, Sun D, Sherman DH.

Comb Chem High Throughput Screen. 2014 Mar;17(3):210-30. Review.

49.

Novel Rho/MRTF/SRF inhibitors block matrix-stiffness and TGF-β-induced fibrogenesis in human colonic myofibroblasts.

Johnson LA, Rodansky ES, Haak AJ, Larsen SD, Neubig RR, Higgins PD.

Inflamm Bowel Dis. 2014 Jan;20(1):154-65. doi: 10.1097/01.MIB.0000437615.98881.31.

50.

Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog.

Homan KT, Wu E, Wilson MW, Singh P, Larsen SD, Tesmer JJ.

Mol Pharmacol. 2014 Feb;85(2):237-48. doi: 10.1124/mol.113.089631. Epub 2013 Nov 12.

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