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Items: 15

1.

Neuroactive Steroid N-Methyl-d-aspartate Receptor Positive Allosteric Modulators: Synthesis, SAR, and Pharmacological Activity.

La DS, Salituro FG, Martinez Botella G, Griffin AM, Bai Z, Ackley MA, Dai J, Doherty JJ, Harrison BL, Hoffmann EC, Kazdoba TM, Lewis MC, Quirk MC, Robichaud AJ.

J Med Chem. 2019 Aug 22;62(16):7526-7542. doi: 10.1021/acs.jmedchem.9b00591. Epub 2019 Aug 13.

PMID:
31390523
2.

Targeting the MAPK Signaling Pathway in Cancer: Promising Preclinical Activity with the Novel Selective ERK1/2 Inhibitor BVD-523 (Ulixertinib).

Germann UA, Furey BF, Markland W, Hoover RR, Aronov AM, Roix JJ, Hale M, Boucher DM, Sorrell DA, Martinez-Botella G, Fitzgibbon M, Shapiro P, Wick MJ, Samadani R, Meshaw K, Groover A, DeCrescenzo G, Namchuk M, Emery CM, Saha S, Welsch DJ.

Mol Cancer Ther. 2017 Nov;16(11):2351-2363. doi: 10.1158/1535-7163.MCT-17-0456. Epub 2017 Sep 22.

3.

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.

Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Blanco MJ, Belfort GM, Dai J, Loya CM, Ackley MA, Althaus AL, Grossman SJ, Hoffmann E, Doherty JJ, Robichaud AJ.

J Med Chem. 2017 Sep 28;60(18):7810-7819. doi: 10.1021/acs.jmedchem.7b00846. Epub 2017 Aug 17.

PMID:
28753313
4.

Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models.

Hammond RS, Althaus AL, Ackley MA, Maciag C, Martinez Botella G, Salituro FG, Robichaud AJ, Doherty JJ.

Epilepsy Res. 2017 Aug;134:16-25. doi: 10.1016/j.eplepsyres.2017.05.001. Epub 2017 May 7.

PMID:
28521115
5.

Negishi cross-coupling enabled synthesis of novel NAD(+)-dependent DNA ligase inhibitors and SAR development.

Murphy-Benenato KE, Gingipalli L, Boriack-Sjodin PA, Martinez-Botella G, Carcanague D, Eyermann CJ, Gowravaram M, Harang J, Hale MR, Ioannidis G, Jahic H, Johnstone M, Kutschke A, Laganas VA, Loch JT 3rd, Miller MD, Oguto H, Patel SJ.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5172-7. doi: 10.1016/j.bmcl.2015.09.075. Epub 2015 Oct 14.

PMID:
26463129
6.

Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr-/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator.

Martin BS, Martinez-Botella G, Loya CM, Salituro FG, Robichaud AJ, Huntsman MM, Ackley MA, Doherty JJ, Corbin JG.

J Neurosci Res. 2016 Jun;94(6):568-78. doi: 10.1002/jnr.23632. Epub 2015 Aug 26.

7.

Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases.

Farmer LJ, Ledeboer MW, Hoock T, Arnost MJ, Bethiel RS, Bennani YL, Black JJ, Brummel CL, Chakilam A, Dorsch WA, Fan B, Cochran JE, Halas S, Harrington EM, Hogan JK, Howe D, Huang H, Jacobs DH, Laitinen LM, Liao S, Mahajan S, Marone V, Martinez-Botella G, McCarthy P, Messersmith D, Namchuk M, Oh L, Penney MS, Pierce AC, Raybuck SA, Rugg A, Salituro FG, Saxena K, Shannon D, Shlyakter D, Swenson L, Tian SK, Town C, Wang J, Wang T, Wannamaker MW, Winquist RJ, Zuccola HJ.

J Med Chem. 2015 Sep 24;58(18):7195-216. doi: 10.1021/acs.jmedchem.5b00301. Epub 2015 Sep 10.

PMID:
26230873
8.

Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.

Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Shen K, Belfort GM, Loya CM, Ackley MA, Grossman SJ, Hoffmann E, Jia S, Wang J, Doherty JJ, Robichaud AJ.

J Med Chem. 2015 Apr 23;58(8):3500-11. doi: 10.1021/acs.jmedchem.5b00032. Epub 2015 Apr 14.

PMID:
25799373
9.

Antibacterial inhibitors of Gram-positive thymidylate kinase: structure-activity relationships and chiral preference of a new hydrophobic binding region.

Kawatkar SP, Keating TA, Olivier NB, Breen JN, Green OM, Guler SY, Hentemann MF, Loch JT, McKenzie AR, Newman JV, Otterson LG, Martínez-Botella G.

J Med Chem. 2014 Jun 12;57(11):4584-97. doi: 10.1021/jm500463c. Epub 2014 Jun 3.

PMID:
24828090
10.

Structural basis for isoform selectivity in a class of benzothiazole inhibitors of phosphoinositide 3-kinase γ.

Collier PN, Martinez-Botella G, Cornebise M, Cottrell KM, Doran JD, Griffith JP, Mahajan S, Maltais F, Moody CS, Huck EP, Wang T, Aronov AM.

J Med Chem. 2015 Jan 8;58(1):517-21. doi: 10.1021/jm500362j. Epub 2014 May 2.

PMID:
24754609
11.

Sulfonylpiperidines as novel, antibacterial inhibitors of Gram-positive thymidylate kinase (TMK).

Martínez-Botella G, Loch JT, Green OM, Kawatkar SP, Olivier NB, Boriack-Sjodin PA, Keating TA.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):169-73. doi: 10.1016/j.bmcl.2012.10.128. Epub 2012 Nov 5.

PMID:
23206863
12.

Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).

Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA.

J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24.

PMID:
23043329
13.

In vivo validation of thymidylate kinase (TMK) with a rationally designed, selective antibacterial compound.

Keating TA, Newman JV, Olivier NB, Otterson LG, Andrews B, Boriack-Sjodin PA, Breen JN, Doig P, Dumas J, Gangl E, Green OM, Guler SY, Hentemann MF, Joseph-McCarthy D, Kawatkar S, Kutschke A, Loch JT, McKenzie AR, Pradeepan S, Prasad S, Martínez-Botella G.

ACS Chem Biol. 2012 Nov 16;7(11):1866-72. doi: 10.1021/cb300316n. Epub 2012 Aug 28.

PMID:
22908966
14.

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
15.

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

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