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Items: 17


Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).

Brooks CA, Barton LS, Behm DJ, Brnardic EJ, Costell MH, Holt DA, Jolivette LJ, Matthews JM, McAtee JJ, McCleland BW, Patterson JR, Pero JE, Rivero RA, Roethke TJ, Sanchez RM, Shenje R, Terrell LR, Lawhorn BG.

J Med Chem. 2019 Oct 24;62(20):9270-9280. doi: 10.1021/acs.jmedchem.9b01247. Epub 2019 Oct 9.


Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).

Brooks CA, Barton LS, Behm DJ, Eidam HS, Fox RM, Hammond M, Hoang TH, Holt DA, Hilfiker MA, Lawhorn BG, Patterson JR, Stoy P, Roethke TJ, Ye G, Zhao S, Thorneloe KS, Goodman KB, Cheung M.

ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233. doi: 10.1021/acsmedchemlett.9b00274. eCollection 2019 Aug 8.


Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.

Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG.

J Med Chem. 2018 Dec 27;61(24):11209-11220. doi: 10.1021/acs.jmedchem.8b01344. Epub 2018 Dec 12.


Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).

Brnardic EJ, Ye G, Brooks C, Donatelli C, Barton L, McAtee J, Sanchez RM, Shu A, Erhard K, Terrell L, Graczyk-Millbrandt G, He Y, Costell MH, Behm DJ, Roethke T, Stoy P, Holt DA, Lawhorn BG.

J Med Chem. 2018 Nov 8;61(21):9738-9755. doi: 10.1021/acs.jmedchem.8b01317. Epub 2018 Oct 18.


Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1.

Kallander LS, Washburn D, Hilfiker MA, Eidam HS, Lawhorn BG, Prendergast J, Fox R, Dowdell S, Manns S, Hoang T, Zhao S, Ye G, Hammond M, Holt DA, Roethke T, Hong X, Reid RA, Gampe R, Zhang H, Diaz E, Rendina AR, Quinn AM, Willette B.

ACS Med Chem Lett. 2018 Jul 2;9(7):736-740. doi: 10.1021/acsmedchemlett.8b00173. eCollection 2018 Jul 12.


4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors.

Philp J, Lawhorn BG, Graves AP, Shewchuk L, Rivera KL, Jolivette LJ, Holt DA, Gatto GJ Jr, Kallander LS.

J Med Chem. 2018 Apr 12;61(7):3076-3088. doi: 10.1021/acs.jmedchem.8b00125. Epub 2018 Mar 21.


Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.

Lawhorn BG, Tran T, Hong VS, Morgan LA, Le BT, Harpel MR, Jolivette L, Diaz E, Schwartz B, Gross JW, Tomaszek T, Semus S, Concha N, Smallwood A, Holt DA, Kallander LS.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4838-4843. doi: 10.1016/j.bmcl.2017.09.046. Epub 2017 Sep 23.


Substituent Effects on Drug-Receptor H-bond Interactions: Correlations Useful for the Design of Kinase Inhibitors.

Lawhorn BG, Philp J, Graves AP, Holt DA, Gatto GJ Jr, Kallander LS.

J Med Chem. 2016 Dec 8;59(23):10629-10641. Epub 2016 Nov 22.


GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.

Lawhorn BG, Philp J, Graves AP, Shewchuk L, Holt DA, Gatto GJ Jr, Kallander LS.

Bioorg Med Chem Lett. 2016 Jul 15;26(14):3355-3358. doi: 10.1016/j.bmcl.2016.05.033. Epub 2016 May 14.


Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).

Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS.

J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10.


Inhibition of the cardiomyocyte-specific kinase TNNI3K limits oxidative stress, injury, and adverse remodeling in the ischemic heart.

Vagnozzi RJ, Gatto GJ Jr, Kallander LS, Hoffman NE, Mallilankaraman K, Ballard VL, Lawhorn BG, Stoy P, Philp J, Graves AP, Naito Y, Lepore JJ, Gao E, Madesh M, Force T.

Sci Transl Med. 2013 Oct 16;5(207):207ra141. doi: 10.1126/scitranslmed.3006479.


Structure-activity relationship studies of fostriecin, cytostatin, and key analogs, with PP1, PP2A, PP5, and( beta12-beta13)-chimeras (PP1/PP2A and PP5/PP2A), provide further insight into the inhibitory actions of fostriecin family inhibitors.

Swingle MR, Amable L, Lawhorn BG, Buck SB, Burke CP, Ratti P, Fischer KL, Boger DL, Honkanen RE.

J Pharmacol Exp Ther. 2009 Oct;331(1):45-53. doi: 10.1124/jpet.109.155630. Epub 2009 Jul 10.


Total synthesis and evaluation of cytostatin, its C10-C11 diastereomers, and additional key analogues: impact on PP2A inhibition.

Lawhorn BG, Boga SB, Wolkenberg SE, Colby DA, Gauss CM, Swingle MR, Amable L, Honkanen RE, Boger DL.

J Am Chem Soc. 2006 Dec 27;128(51):16720-32.


Biosynthesis of the thiamin pyrimidine: the reconstitution of a remarkable rearrangement reaction.

Lawhorn BG, Mehl RA, Begley TP.

Org Biomol Chem. 2004 Sep 7;2(17):2538-46. Epub 2004 Aug 11.


A genetic screen for the identification of thiamin metabolic genes.

Lawhorn BG, Gerdes SY, Begley TP.

J Biol Chem. 2004 Oct 15;279(42):43555-9. Epub 2004 Jul 28.


Detection of four oxidation sites in viral prolyl-4-hydroxylase by top-down mass spectrometry.

Ge Y, Lawhorn BG, ElNaggar M, Sze SK, Begley TP, McLafferty FW.

Protein Sci. 2003 Oct;12(10):2320-6.


Top down characterization of larger proteins (45 kDa) by electron capture dissociation mass spectrometry.

Ge Y, Lawhorn BG, ElNaggar M, Strauss E, Park JH, Begley TP, McLafferty FW.

J Am Chem Soc. 2002 Jan 30;124(4):672-8.


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