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Items: 45

1.

Risdiplam distributes and increases SMN protein in both the central nervous system and peripheral organs.

Poirier A, Weetall M, Heinig K, Bucheli F, Schoenlein K, Alsenz J, Bassett S, Ullah M, Senn C, Ratni H, Naryshkin N, Paushkin S, Mueller L.

Pharmacol Res Perspect. 2018 Nov 29;6(6):e00447. doi: 10.1002/prp2.447. eCollection 2018 Dec.

2.

The minor gentamicin complex component, X2, is a potent premature stop codon readthrough molecule with therapeutic potential.

Friesen WJ, Johnson B, Sierra J, Zhuo J, Vazirani P, Xue X, Tomizawa Y, Baiazitov R, Morrill C, Ren H, Babu S, Moon YC, Branstrom A, Mollin A, Hedrick J, Sheedy J, Elfring G, Weetall M, Colacino JM, Welch EM, Peltz SW.

PLoS One. 2018 Oct 25;13(10):e0206158. doi: 10.1371/journal.pone.0206158. eCollection 2018.

3.

Targeting of Hematologic Malignancies with PTC299, A Novel Potent Inhibitor of Dihydroorotate Dehydrogenase with Favorable Pharmaceutical Properties.

Cao L, Weetall M, Trotta C, Cintron K, Ma J, Kim MJ, Furia B, Romfo C, Graci JD, Li W, Du J, Sheedy J, Hedrick J, Risher N, Yeh S, Qi H, Arasu T, Hwang S, Lennox W, Kong R, Petruska J, Moon YC, Babiak J, Davis TW, Jacobson A, Almstead NG, Branstrom A, Colacino JM, Peltz SW.

Mol Cancer Ther. 2019 Jan;18(1):3-16. doi: 10.1158/1535-7163.MCT-18-0863. Epub 2018 Oct 23.

PMID:
30352802
4.

Correction to Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-Negative Bacteria.

Gerasyuto AI, Arnold MA, Wang J, Chen G, Zhang X, Smith S, Woll MG, Baird J, Zhang N, Almstead NG, Narasimhan J, Peddi S, Dumble M, Sheedy J, Weetall M, Branstrom AA, Prasad JVN, Karp GM.

J Med Chem. 2018 Oct 25;61(20):9394. doi: 10.1021/acs.jmedchem.8b01538. Epub 2018 Oct 16. No abstract available.

5.

BMI1 is a therapeutic target in recurrent medulloblastoma.

Bakhshinyan D, Venugopal C, Adile AA, Garg N, Manoranjan B, Hallett R, Wang X, Mahendram S, Vora P, Vijayakumar T, Subapanditha M, Singh M, Kameda-Smith MM, Qazi M, McFarlane N, Mann A, Ajani OA, Yarascavitch B, Ramaswamy V, Farooq H, Morrissy S, Cao L, Sydorenko N, Baiazitov R, Du W, Sheedy J, Weetall M, Moon YC, Lee CS, Kwiecien JM, Delaney KH, Doble B, Cho YJ, Mitra S, Kaplan D, Taylor MD, Davis TW, Singh SK.

Oncogene. 2018 Oct 22. doi: 10.1038/s41388-018-0549-9. [Epub ahead of print]

PMID:
30348991
6.

Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 ( SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA).

Ratni H, Ebeling M, Baird J, Bendels S, Bylund J, Chen KS, Denk N, Feng Z, Green L, Guerard M, Jablonski P, Jacobsen B, Khwaja O, Kletzl H, Ko CP, Kustermann S, Marquet A, Metzger F, Mueller B, Naryshkin NA, Paushkin SV, Pinard E, Poirier A, Reutlinger M, Weetall M, Zeller A, Zhao X, Mueller L.

J Med Chem. 2018 Aug 9;61(15):6501-6517. doi: 10.1021/acs.jmedchem.8b00741. Epub 2018 Jul 25.

PMID:
30044619
7.

Inhibition of BMI1, a Therapeutic Approach in Endometrial Cancer.

Buechel M, Dey A, Dwivedi SKD, Crim A, Ding K, Zhang R, Mukherjee P, Moore KN, Cao L, Branstrom A, Weetall M, Baird J, Bhattacharya R.

Mol Cancer Ther. 2018 Oct;17(10):2136-2143. doi: 10.1158/1535-7163.MCT-17-1192. Epub 2018 Jul 19.

PMID:
30026381
8.

Targeting of BMI-1 expression by the novel small molecule PTC596 in mantle cell lymphoma.

Maeda A, Nishida Y, Weetall M, Cao L, Branstrom A, Ishizawa J, Nii T, Schober WD, Abe Y, Matsue K, Yoshimura M, Kimura S, Kojima K.

Oncotarget. 2018 Jun 19;9(47):28547-28560. doi: 10.18632/oncotarget.25558. eCollection 2018 Jun 19.

9.

Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.

Gerasyuto AI, Arnold MA, Wang J, Chen G, Zhang X, Smith S, Woll MG, Baird J, Zhang N, Almstead NG, Narasimhan J, Peddi S, Dumble M, Sheedy J, Weetall M, Branstrom AA, Prasad JVN, Karp GM.

J Med Chem. 2018 May 24;61(10):4456-4475. doi: 10.1021/acs.jmedchem.8b00114. Epub 2018 May 14. Erratum in: J Med Chem. 2018 Oct 25;61(20):9394.

10.

4-Hydroxy-2-pyridones: Discovery and evaluation of a novel class of antibacterial agents targeting DNA synthesis.

Arnold MA, Gerasyuto AI, Wang J, Du W, Gorske YJK, Arasu T, Baird J, Almstead NG, Narasimhan J, Peddi S, Ginzburg O, Lue SW, Hedrick J, Sheedy J, Lagaud G, Branstrom AA, Weetall M, Prasad JVNV, Karp GM.

Bioorg Med Chem Lett. 2017 Nov 15;27(22):5014-5021. doi: 10.1016/j.bmcl.2017.10.006. Epub 2017 Oct 5.

PMID:
29032026
11.

Identification of benzazole compounds that induce HIV-1 transcription.

Graci JD, Michaels D, Chen G, Schiralli Lester GM, Nodder S, Weetall M, Karp GM, Gu Z, Colacino JM, Henderson AJ.

PLoS One. 2017 Jun 28;12(6):e0179100. doi: 10.1371/journal.pone.0179100. eCollection 2017.

12.

Discovery of a Novel Class of Survival Motor Neuron 2 Splicing Modifiers for the Treatment of Spinal Muscular Atrophy.

Pinard E, Green L, Reutlinger M, Weetall M, Naryshkin NA, Baird J, Chen KS, Paushkin SV, Metzger F, Ratni H.

J Med Chem. 2017 May 25;60(10):4444-4457. doi: 10.1021/acs.jmedchem.7b00406. Epub 2017 May 4.

PMID:
28441483
13.

The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells.

Nishida Y, Maeda A, Kim MJ, Cao L, Kubota Y, Ishizawa J, AlRawi A, Kato Y, Iwama A, Fujisawa M, Matsue K, Weetall M, Dumble M, Andreeff M, Davis TW, Branstrom A, Kimura S, Kojima K.

Blood Cancer J. 2017 Feb 17;7(2):e527. doi: 10.1038/bcj.2017.8.

14.

The nucleoside analog clitocine is a potent and efficacious readthrough agent.

Friesen WJ, Trotta CR, Tomizawa Y, Zhuo J, Johnson B, Sierra J, Roy B, Weetall M, Hedrick J, Sheedy J, Takasugi J, Moon YC, Babu S, Baiazitov R, Leszyk JD, Davis TW, Colacino JM, Peltz SW, Welch EM.

RNA. 2017 Apr;23(4):567-577. doi: 10.1261/rna.060236.116. Epub 2017 Jan 17.

15.

Discovery of Novel Small Molecule Inhibitors of VEGF Expression in Tumor Cells Using a Cell-Based High Throughput Screening Platform.

Cao L, Weetall M, Bombard J, Qi H, Arasu T, Lennox W, Hedrick J, Sheedy J, Risher N, Brooks PC, Trifillis P, Trotta C, Moon YC, Babiak J, Almstead NG, Colacino JM, Davis TW, Peltz SW.

PLoS One. 2016 Dec 16;11(12):e0168366. doi: 10.1371/journal.pone.0168366. eCollection 2016.

16.

Functional rescue of REP1 following treatment with PTC124 and novel derivative PTC-414 in human choroideremia fibroblasts and the nonsense-mediated zebrafish model.

Moosajee M, Tracey-White D, Smart M, Weetall M, Torriano S, Kalatzis V, da Cruz L, Coffey P, Webster AR, Welch E.

Hum Mol Genet. 2016 Aug 15;25(16):3416-3431. doi: 10.1093/hmg/ddw184. Epub 2016 Jun 21.

PMID:
27329764
17.

Phase 1 Study of Safety, Tolerability, and Pharmacokinetics of PTC299, an Inhibitor of Stress-Regulated Protein Translation.

Weetall M, Davis T, Elfring G, Northcutt V, Cao L, Moon YC, Riebling P, Dali M, Hirawat S, Babiak J, Colacino J, Almstead N, Spiegel R, Peltz SW.

Clin Pharmacol Drug Dev. 2016 Jul;5(4):296-305. doi: 10.1002/cpdd.240. Epub 2016 Feb 2.

18.

Discovery and Optimization of Small Molecule Splicing Modifiers of Survival Motor Neuron 2 as a Treatment for Spinal Muscular Atrophy.

Woll MG, Qi H, Turpoff A, Zhang N, Zhang X, Chen G, Li C, Huang S, Yang T, Moon YC, Lee CS, Choi S, Almstead NG, Naryshkin NA, Dakka A, Narasimhan J, Gabbeta V, Welch E, Zhao X, Risher N, Sheedy J, Weetall M, Karp GM.

J Med Chem. 2016 Jul 14;59(13):6070-85. doi: 10.1021/acs.jmedchem.6b00460. Epub 2016 Jul 6.

PMID:
27299569
19.

Specific Correction of Alternative Survival Motor Neuron 2 Splicing by Small Molecules: Discovery of a Potential Novel Medicine To Treat Spinal Muscular Atrophy.

Ratni H, Karp GM, Weetall M, Naryshkin NA, Paushkin SV, Chen KS, McCarthy KD, Qi H, Turpoff A, Woll MG, Zhang X, Zhang N, Yang T, Dakka A, Vazirani P, Zhao X, Pinard E, Green L, David-Pierson P, Tuerck D, Poirier A, Muster W, Kirchner S, Mueller L, Gerlach I, Metzger F.

J Med Chem. 2016 Jul 14;59(13):6086-100. doi: 10.1021/acs.jmedchem.6b00459. Epub 2016 Jul 6.

PMID:
27299419
20.

SMN Protein Can Be Reliably Measured in Whole Blood with an Electrochemiluminescence (ECL) Immunoassay: Implications for Clinical Trials.

Zaworski P, von Herrmann KM, Taylor S, Sunshine SS, McCarthy K, Risher N, Newcomb T, Weetall M, Prior TW, Swoboda KJ, Chen KS, Paushkin S.

PLoS One. 2016 Mar 8;11(3):e0150640. doi: 10.1371/journal.pone.0150640. eCollection 2016.

21.

Pharmacokinetics, pharmacodynamics, and efficacy of a small-molecule SMN2 splicing modifier in mouse models of spinal muscular atrophy.

Zhao X, Feng Z, Ling KK, Mollin A, Sheedy J, Yeh S, Petruska J, Narasimhan J, Dakka A, Welch EM, Karp G, Chen KS, Metzger F, Ratni H, Lotti F, Tisdale S, Naryshkin NA, Pellizzoni L, Paushkin S, Ko CP, Weetall M.

Hum Mol Genet. 2016 May 15;25(10):1885-1899. Epub 2016 Feb 29.

22.

Pharmacologically induced mouse model of adult spinal muscular atrophy to evaluate effectiveness of therapeutics after disease onset.

Feng Z, Ling KK, Zhao X, Zhou C, Karp G, Welch EM, Naryshkin N, Ratni H, Chen KS, Metzger F, Paushkin S, Weetall M, Ko CP.

Hum Mol Genet. 2016 Mar 1;25(5):964-75. doi: 10.1093/hmg/ddv629. Epub 2016 Jan 11.

PMID:
26758873
23.

Discovery of 2-(4-sulfonamidophenyl)-indole 3-carboxamides as potent and selective inhibitors with broad hepatitis C virus genotype activity targeting HCV NS4B.

Zhang N, Turpoff A, Zhang X, Huang S, Liu Y, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Pichardo J, Colacino J, Lahser F, Ingravallo P, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):594-601. doi: 10.1016/j.bmcl.2015.11.065. Epub 2015 Nov 19.

PMID:
26652483
24.

6-(Azaindol-2-yl)pyridine-3-sulfonamides as potent and selective inhibitors targeting hepatitis C virus NS4B.

Chen G, Ren H, Zhang N, Lennox W, Turpoff A, Paget S, Li C, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Colacino J, Lahser F, Zhao X, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):781-6. doi: 10.1016/j.bmcl.2014.12.093. Epub 2015 Jan 7.

PMID:
25613678
25.

Motor neuron disease. SMN2 splicing modifiers improve motor function and longevity in mice with spinal muscular atrophy.

Naryshkin NA, Weetall M, Dakka A, Narasimhan J, Zhao X, Feng Z, Ling KK, Karp GM, Qi H, Woll MG, Chen G, Zhang N, Gabbeta V, Vazirani P, Bhattacharyya A, Furia B, Risher N, Sheedy J, Kong R, Ma J, Turpoff A, Lee CS, Zhang X, Moon YC, Trifillis P, Welch EM, Colacino JM, Babiak J, Almstead NG, Peltz SW, Eng LA, Chen KS, Mull JL, Lynes MS, Rubin LL, Fontoura P, Santarelli L, Haehnke D, McCarthy KD, Schmucki R, Ebeling M, Sivaramakrishnan M, Ko CP, Paushkin SV, Ratni H, Gerlach I, Ghosh A, Metzger F.

Science. 2014 Aug 8;345(6197):688-93. doi: 10.1126/science.1250127.

26.

Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B.

Zhang N, Zhang X, Zhu J, Turpoff A, Chen G, Morrill C, Huang S, Lennox W, Kakarla R, Liu R, Li C, Ren H, Almstead N, Venkatraman S, Njoroge FG, Gu Z, Clausen V, Graci J, Jung SP, Zheng Y, Colacino JM, Lahser F, Sheedy J, Mollin A, Weetall M, Nomeir A, Karp GM.

J Med Chem. 2014 Mar 13;57(5):2121-35. doi: 10.1021/jm401621g. Epub 2013 Dec 4.

PMID:
24266880
27.

Discovery of novel HCV inhibitors: synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B.

Zhang X, Zhang N, Chen G, Turpoff A, Ren H, Takasugi J, Morrill C, Zhu J, Li C, Lennox W, Paget S, Liu Y, Almstead N, Njoroge FG, Gu Z, Komatsu T, Clausen V, Espiritu C, Graci J, Colacino J, Lahser F, Risher N, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3947-53. doi: 10.1016/j.bmcl.2013.04.049. Epub 2013 Apr 30.

PMID:
23683597
28.

Discovery of N-(4'-(indol-2-yl)phenyl)sulfonamides as novel inhibitors of HCV replication.

Chen G, Ren H, Turpoff A, Arefolov A, Wilde R, Takasugi J, Khan A, Almstead N, Gu Z, Komatsu T, Freund C, Breslin J, Colacino J, Hedrick J, Weetall M, Karp GM.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3942-6. doi: 10.1016/j.bmcl.2013.04.050. Epub 2013 Apr 30.

PMID:
23683596
29.

Identification of PTC725, an orally bioavailable small molecule that selectively targets the hepatitis C Virus NS4B protein.

Gu Z, Graci JD, Lahser FC, Breslin JJ, Jung SP, Crona JH, McMonagle P, Xia E, Liu S, Karp G, Zhu J, Huang S, Nomeir A, Weetall M, Almstead NG, Peltz SW, Tong X, Ralston R, Colacino JM.

Antimicrob Agents Chemother. 2013 Jul;57(7):3250-61. doi: 10.1128/AAC.00527-13. Epub 2013 Apr 29.

30.

BMI1 as a novel target for drug discovery in cancer.

Cao L, Bombard J, Cintron K, Sheedy J, Weetall ML, Davis TW.

J Cell Biochem. 2011 Oct;112(10):2729-41. doi: 10.1002/jcb.23234. Review.

PMID:
21678481
31.

PTC124 targets genetic disorders caused by nonsense mutations.

Welch EM, Barton ER, Zhuo J, Tomizawa Y, Friesen WJ, Trifillis P, Paushkin S, Patel M, Trotta CR, Hwang S, Wilde RG, Karp G, Takasugi J, Chen G, Jones S, Ren H, Moon YC, Corson D, Turpoff AA, Campbell JA, Conn MM, Khan A, Almstead NG, Hedrick J, Mollin A, Risher N, Weetall M, Yeh S, Branstrom AA, Colacino JM, Babiak J, Ju WD, Hirawat S, Northcutt VJ, Miller LL, Spatrick P, He F, Kawana M, Feng H, Jacobson A, Peltz SW, Sweeney HL.

Nature. 2007 May 3;447(7140):87-91. Epub 2007 Apr 22.

PMID:
17450125
32.

Immunologic pathways in a quantitative model of immunosuppression based on rejection of an allogeneic or xenogeneic tumor graft.

Hammond-McKibben D, Saulnier M, Zhang J, Risher N, Lake P, Weetall M.

Transplantation. 2005 Apr 27;79(8):889-96.

PMID:
15849540
33.

Pharmacodynamic evaluation of the neutralization of endotoxin by PMX622 in mice.

Lake P, DeLeo J, Cerasoli F, Logdberg L, Weetall M, Handley D.

Antimicrob Agents Chemother. 2004 Aug;48(8):2987-92.

34.

Divergent pathways of gene expression are activated by the RAGE ligands S100b and AGE-BSA.

Valencia JV, Mone M, Zhang J, Weetall M, Buxton FP, Hughes TE.

Diabetes. 2004 Mar;53(3):743-51.

35.
36.

T-cell depletion and graft survival induced by anti-human CD3 immunotoxins in human CD3epsilon transgenic mice.

Weetall M, Digan ME, Hugo R, Mathew S, Hopf C, Tart-Risher N, Zhang J, Shi V, Fu F, Hammond-McKibben D, West S, Brack R, Brinkmann V, Bergman R, Neville D Jr, Lake P.

Transplantation. 2002 May 27;73(10):1658-66.

PMID:
12042656
37.

Combinatorial approaches to inhibitors of VLA-4: piperazine-peptoid-bisarylureas.

Lewis I, Rohde B, Mengus M, Weetall M, Maida S, Hugo R, Lake P.

Mol Divers. 2000;5(2):61-73.

PMID:
11865647
38.

Improved binding of a bivalent single-chain immunotoxin results in increased efficacy for in vivo T-cell depletion.

Thompson J, Stavrou S, Weetall M, Hexham JM, Digan ME, Wang Z, Woo JH, Yu Y, Mathias A, Liu YY, Ma S, Gordienko I, Lake P, Neville DM Jr.

Protein Eng. 2001 Dec;14(12):1035-41.

PMID:
11809934
39.

Design and synthesis of potent and selective inhibitors of integrin VLA-4.

Wattanasin S, Weidmann B, Roche D, Myers S, Xing A, Guo Q, Sabio M, von Matt P, Hugo R, Maida S, Lake P, Weetall M.

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2955-8.

PMID:
11677134
40.

A homogeneous fluorometric assay for measuring cell adhesion to immobilized ligand using V-well microtiter plates.

Weetall M, Hugo R, Friedman C, Maida S, West S, Wattanasin S, Bouhel R, Weitz-Schmidt G, Lake P.

Anal Biochem. 2001 Jun 15;293(2):277-87.

PMID:
11399044
41.

A high-capacity quantitative mouse model of drug-mediated immunosuppression based on rejection of an allogeneic subcutaneous tumor.

Hammond-McKibben D, Lake P, Zhang J, Tart-Risher N, Hugo R, Weetall M.

J Pharmacol Exp Ther. 2001 Jun;297(3):1144-51.

42.

Absorption and disposition of a tripeptoid and a tetrapeptide in the rat.

Wang Y, Lin H, Tullman R, Jewell CF Jr, Weetall ML, Tse FL.

Biopharm Drug Dispos. 1999 Mar;20(2):69-75.

PMID:
10206321
43.

Heterologous desensitization of the high affinity receptor for IgE (Fc epsilon R1) on RBL cells.

Weetall M, Holowka D, Baird B.

J Immunol. 1993 May 1;150(9):4072-83.

PMID:
8473750
44.

Mapping the site of interaction between murine IgE and its high affinity receptor with chimeric Ig.

Weetall M, Shopes B, Holowka D, Baird B.

J Immunol. 1990 Dec 1;145(11):3849-54.

PMID:
2147205
45.

Recombinant human IgG1-murine IgE chimeric Ig. Construction, expression, and binding to human Fc gamma receptors.

Shopes B, Weetall M, Holowka D, Baird B.

J Immunol. 1990 Dec 1;145(11):3842-8.

PMID:
2147204

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