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Site-Selective Antibody Functionalization via Orthogonally Reactive Arginine and Lysine Residues.

Hwang D, Nilchan N, Nanna AR, Li X, Cameron MD, Roush WR, Park H, Rader C.

Cell Chem Biol. 2019 Jun 11. pii: S2451-9456(19)30179-5. doi: 10.1016/j.chembiol.2019.05.010. [Epub ahead of print]


Discovery and Optimization of a Series of Sulfonamide Inverse Agonists for the Retinoic Acid Receptor-Related Orphan Receptor-α.

Doebelin C, He Y, Campbell S, Nuhant P, Kumar N, Koenig M, Garcia-Ordonez R, Chang MR, Roush WR, Lin L, Kahn S, Cameron MD, Griffin PR, Solt LA, Kamenecka TM.

Med Chem. 2019;15(6):676-684. doi: 10.2174/1573406415666190222124745.


Efficacy of novel selective NLRP3 inhibitors in human and murine retinal pigment epithelial cells.

Wang L, Schmidt S, Larsen PP, Meyer JH, Roush WR, Latz E, Holz FG, Krohne TU.

J Mol Med (Berl). 2019 Apr;97(4):523-532. doi: 10.1007/s00109-019-01753-5. Epub 2019 Feb 10.


Development of matrix metalloproteinase-13 inhibitors - A structure-activity/structure-property relationship study.

Fuerst R, Yong Choi J, Knapinska AM, Smith L, Cameron MD, Ruiz C, Fields GB, Roush WR.

Bioorg Med Chem. 2018 Oct 1;26(18):4984-4995. doi: 10.1016/j.bmc.2018.08.020. Epub 2018 Aug 20.


Targeting the NLRP3 inflammasome in inflammatory diseases.

Mangan MSJ, Olhava EJ, Roush WR, Seidel HM, Glick GD, Latz E.

Nat Rev Drug Discov. 2018 Sep;17(9):688. doi: 10.1038/nrd.2018.149. Epub 2018 Aug 17.


Systems analysis of intracellular pH vulnerabilities for cancer therapy.

Persi E, Duran-Frigola M, Damaghi M, Roush WR, Aloy P, Cleveland JL, Gillies RJ, Ruppin E.

Nat Commun. 2018 Jul 31;9(1):2997. doi: 10.1038/s41467-018-05261-x.


Targeting the NLRP3 inflammasome in inflammatory diseases.

Mangan MSJ, Olhava EJ, Roush WR, Seidel HM, Glick GD, Latz E.

Nat Rev Drug Discov. 2018 Aug;17(8):588-606. doi: 10.1038/nrd.2018.97. Epub 2018 Jul 20. Review. Erratum in: Nat Rev Drug Discov. 2018 Sep;17(9):688.


Identification of cysteine protease inhibitors as new drug leads against Naegleria fowleri.

Zyserman I, Mondal D, Sarabia F, McKerrow JH, Roush WR, Debnath A.

Exp Parasitol. 2018 May;188:36-41. doi: 10.1016/j.exppara.2018.03.010. Epub 2018 Mar 15.


4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection.

Calvet CM, Choi JY, Thomas D, Suzuki B, Hirata K, Lostracco-Johnson S, de Mesquita LB, Nogueira A, Meuser-Batista M, Silva TA, Siqueira-Neto JL, Roush WR, de Souza Pereira MC, McKerrow JH, Podust LM.

PLoS Negl Trop Dis. 2017 Dec 27;11(12):e0006132. doi: 10.1371/journal.pntd.0006132. eCollection 2017 Dec.


In Silico HTS and Structure Based Optimization of Indazole-Derived ULK1 Inhibitors.

Wood SD, Grant W, Adrados I, Choi JY, Alburger JM, Duckett DR, Roush WR.

ACS Med Chem Lett. 2017 Nov 22;8(12):1258-1263. doi: 10.1021/acsmedchemlett.7b00344. eCollection 2017 Dec 14.


Harnessing a catalytic lysine residue for the one-step preparation of homogeneous antibody-drug conjugates.

Nanna AR, Li X, Walseng E, Pedzisa L, Goydel RS, Hymel D, Burke TR Jr, Roush WR, Rader C.

Nat Commun. 2017 Oct 24;8(1):1112. doi: 10.1038/s41467-017-01257-1.


Novel Pharmacological Probes Reveal ABHD5 as a Locus of Lipolysis Control in White and Brown Adipocytes.

Rondini EA, Mladenovic-Lucas L, Roush WR, Halvorsen GT, Green AE, Granneman JG.

J Pharmacol Exp Ther. 2017 Dec;363(3):367-376. doi: 10.1124/jpet.117.243253. Epub 2017 Sep 19.


Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors.

Choi JY, Fuerst R, Knapinska AM, Taylor AB, Smith L, Cao X, Hart PJ, Fields GB, Roush WR.

J Med Chem. 2017 Jul 13;60(13):5816-5825. doi: 10.1021/acs.jmedchem.7b00514. Epub 2017 Jun 27.


Stolonidiol: Synthesis, Target Identification, and Mechanism for Choline Acetyltransferase Activation.

Mason JW, Schmid CL, Bohn LM, Roush WR.

J Am Chem Soc. 2017 Apr 26;139(16):5865-5869. doi: 10.1021/jacs.7b01083. Epub 2017 Apr 17.


CK1δ: an exploitable vulnerability in breast cancer.

Rosenberg LH, Cleveland JL, Roush WR, Duckett DR.

Ann Transl Med. 2016 Dec;4(23):474. doi: 10.21037/atm.2016.12.15. No abstract available.


Functional Roles of Acetylated Histone Marks at Mouse Meiotic Recombination Hot Spots.

Getun IV, Wu Z, Fallahi M, Ouizem S, Liu Q, Li W, Costi R, Roush WR, Cleveland JL, Bois PRJ.

Mol Cell Biol. 2017 Jan 19;37(3). pii: e00942-15. doi: 10.1128/MCB.00942-15. Print 2017 Feb 1.


Human Serum Albumin Domain I Fusion Protein for Antibody Conjugation.

Patterson JT, Wilson HD, Asano S, Nilchan N, Fuller RP, Roush WR, Rader C, Barbas CF 3rd.

Bioconjug Chem. 2016 Oct 19;27(10):2271-2275. Epub 2016 Sep 26.


Structure Based Design of CYP51 Inhibitors.

Choi JY, Roush WR.

Curr Top Med Chem. 2017;17(1):30-39. Review.


Chemically Programmed Bispecific Antibodies in Diabody Format.

Walseng E, Nelson CG, Qi J, Nanna AR, Roush WR, Goswami RK, Sinha SC, Burke TR Jr, Rader C.

J Biol Chem. 2016 Sep 9;291(37):19661-73. doi: 10.1074/jbc.M116.745588. Epub 2016 Jul 21.


Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.

Nair RN, Mishra JK, Li F, Tortosa M, Yang C, Doherty JR, Cameron M, Cleveland JL, Roush WR, Bannister TD.

Medchemcomm. 2016 May 1;7(5):900-905. Epub 2016 Feb 23.


Assessment of reagents for selenocysteine conjugation and the stability of selenocysteine adducts.

Pedzisa L, Li X, Rader C, Roush WR.

Org Biomol Chem. 2016 Jun 14;14(22):5141-7. doi: 10.1039/c6ob00775a. Epub 2016 May 17.


Fluorometric High-Throughput Screening Assay for Secreted Phospholipases A2 Using Phospholipid Vesicles.

Ewing H, Fernández-Vega V, Spicer TP, Chase P, Brown S, Scampavia L, Roush WR, Riley S, Rosen H, Hodder P, Lambeau G, Gelb MH.

J Biomol Screen. 2016 Aug;21(7):713-21. doi: 10.1177/1087057116646742. Epub 2016 May 4.


Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain.

Jones BD, Tochowicz A, Tang Y, Cameron MD, McCall LI, Hirata K, Siqueira-Neto JL, Reed SL, McKerrow JH, Roush WR.

ACS Med Chem Lett. 2015 Dec 15;7(1):77-82. doi: 10.1021/acsmedchemlett.5b00336. eCollection 2016 Jan 14.


Therapeutic targeting of casein kinase 1δ in breast cancer.

Rosenberg LH, Lafitte M, Quereda V, Grant W, Chen W, Bibian M, Noguchi Y, Fallahi M, Yang C, Chang JC, Roush WR, Cleveland JL, Duckett DR.

Sci Transl Med. 2015 Dec 16;7(318):318ra202. doi: 10.1126/scitranslmed.aac8773.


Endogenous and Synthetic ABHD5 Ligands Regulate ABHD5-Perilipin Interactions and Lipolysis in Fat and Muscle.

Sanders MA, Madoux F, Mladenovic L, Zhang H, Ye X, Angrish M, Mottillo EP, Caruso JA, Halvorsen G, Roush WR, Chase P, Hodder P, Granneman JG.

Cell Metab. 2015 Nov 3;22(5):851-60. doi: 10.1016/j.cmet.2015.08.023. Epub 2015 Sep 24.


Site-Specific Dual Antibody Conjugation via Engineered Cysteine and Selenocysteine Residues.

Li X, Patterson JT, Sarkar M, Pedzisa L, Kodadek T, Roush WR, Rader C.

Bioconjug Chem. 2015 Nov 18;26(11):2243-8. doi: 10.1021/acs.bioconjchem.5b00244. Epub 2015 Jul 24.


Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.

Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team.

Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Review.


Casein kinase 1δ is an APC/C(Cdh1) substrate that regulates cerebellar granule cell neurogenesis.

Penas C, Govek EE, Fang Y, Ramachandran V, Daniel M, Wang W, Maloof ME, Rahaim RJ, Bibian M, Kawauchi D, Finkelstein D, Han JL, Long J, Li B, Robbins DJ, Malumbres M, Roussel MF, Roush WR, Hatten ME, Ayad NG.

Cell Rep. 2015 Apr 14;11(2):249-60. doi: 10.1016/j.celrep.2015.03.016. Epub 2015 Apr 2.


Hrr25/CK1δ-directed release of Ltv1 from pre-40S ribosomes is necessary for ribosome assembly and cell growth.

Ghalei H, Schaub FX, Doherty JR, Noguchi Y, Roush WR, Cleveland JL, Stroupe ME, Karbstein K.

J Cell Biol. 2015 Mar 16;208(6):745-59. doi: 10.1083/jcb.201409056.


Targeting Ergosterol biosynthesis in Leishmania donovani: essentiality of sterol 14 alpha-demethylase.

McCall LI, El Aroussi A, Choi JY, Vieira DF, De Muylder G, Johnston JB, Chen S, Kellar D, Siqueira-Neto JL, Roush WR, Podust LM, McKerrow JH.

PLoS Negl Trop Dis. 2015 Mar 13;9(3):e0003588. doi: 10.1371/journal.pntd.0003588. eCollection 2015 Mar.


Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases.

Wang Y, Stowe RL, Pinello CE, Tian G, Madoux F, Li D, Zhao LY, Li JL, Wang Y, Wang Y, Ma H, Hodder P, Roush WR, Liao D.

Chem Biol. 2015 Feb 19;22(2):273-84. doi: 10.1016/j.chembiol.2014.12.015.


GSK3 inhibitors stabilize Wee1 and reduce cerebellar granule cell progenitor proliferation.

Penas C, Mishra JK, Wood SD, Schürer SC, Roush WR, Ayad NG.

Cell Cycle. 2015;14(3):417-24. doi: 10.4161/15384101.2014.974439.


Antiproliferation activity of a small molecule repressor of liver receptor homolog 1.

Corzo CA, Mari Y, Chang MR, Khan T, Kuruvilla D, Nuhant P, Kumar N, West GM, Duckett DR, Roush WR, Griffin PR.

Mol Pharmacol. 2015 Feb;87(2):296-304. doi: 10.1124/mol.114.095554. Epub 2014 Dec 3.


Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.

Vieira DF, Choi JY, Calvet CM, Siqueira-Neto JL, Johnston JB, Kellar D, Gut J, Cameron MD, McKerrow JH, Roush WR, Podust LM.

J Med Chem. 2014 Dec 11;57(23):10162-75. doi: 10.1021/jm501568b. Epub 2014 Nov 25.


Drug strategies targeting CYP51 in neglected tropical diseases.

Choi JY, Podust LM, Roush WR.

Chem Rev. 2014 Nov 26;114(22):11242-71. doi: 10.1021/cr5003134. Epub 2014 Oct 22. Review. No abstract available.


Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.

Spicer TP, Jiang J, Taylor AB, Choi JY, Hart PJ, Roush WR, Fields GB, Hodder PS, Minond D.

J Med Chem. 2014 Nov 26;57(22):9598-611. doi: 10.1021/jm501284e. Epub 2014 Nov 11.


4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.

Calvet CM, Vieira DF, Choi JY, Kellar D, Cameron MD, Siqueira-Neto JL, Gut J, Johnston JB, Lin L, Khan S, McKerrow JH, Roush WR, Podust LM.

J Med Chem. 2014 Aug 28;57(16):6989-7005. doi: 10.1021/jm500448u. Epub 2014 Aug 19.


Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors.

Wang H, Yang C, Doherty JR, Roush WR, Cleveland JL, Bannister TD.

J Med Chem. 2014 Sep 11;57(17):7317-24. doi: 10.1021/jm500640x. Epub 2014 Aug 22.


R-Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi.

Choi JY, Calvet CM, Vieira DF, Gunatilleke SS, Cameron MD, McKerrow JH, Podust LM, Roush WR.

ACS Med Chem Lett. 2014 Jan 22;5(4):434-9. doi: 10.1021/ml500010m. eCollection 2014 Apr 10.


Casein kinase 1δ-dependent Wee1 protein degradation.

Penas C, Ramachandran V, Simanski S, Lee C, Madoux F, Rahaim RJ, Chauhan R, Barnaby O, Schurer S, Hodder P, Steen J, Roush WR, Ayad NG.

J Biol Chem. 2014 Jul 4;289(27):18893-903. doi: 10.1074/jbc.M114.547661. Epub 2014 May 9.


ML302, a Novel Beta-lactamase (BLA) Inhibitor.

Spicer T, Minond D, Enogieru I, Saldanha SA, Allais C, Liu Q, Mercer BA, Roush WR, Hodder P.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2014 May 13].


Expanding the binding envelope of CYP51 inhibitors targeting Trypanosoma cruzi with 4-aminopyridyl-based sulfonamide derivatives.

Vieira DF, Choi JY, Roush WR, Podust LM.

Chembiochem. 2014 May 26;15(8):1111-20. doi: 10.1002/cbic.201402027. Epub 2014 Apr 25.


Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis.

Doherty JR, Yang C, Scott KE, Cameron MD, Fallahi M, Li W, Hall MA, Amelio AL, Mishra JK, Li F, Tortosa M, Genau HM, Rounbehler RJ, Lu Y, Dang CV, Kumar KG, Butler AA, Bannister TD, Hooper AT, Unsal-Kacmaz K, Roush WR, Cleveland JL.

Cancer Res. 2014 Feb 1;74(3):908-20. doi: 10.1158/0008-5472.CAN-13-2034. Epub 2013 Nov 27.


Generation of stereochemically defined tetrasubstituted enolborinates by 1,4-hydroboration of α,β-unsaturated morpholine carboxamides with (diisopinocampheyl)borane.

Allais C, Tsai AS, Nuhant P, Roush WR.

Angew Chem Int Ed Engl. 2013 Dec 2;52(49):12888-12891. doi: 10.1002/anie.201307302. Epub 2013 Oct 15.


Identification of Selective Agonists of the Transient Receptor Potential Channels 3 (TRPML3).

Saldanha SA, Grimm C, Allais C, Smith E, Ouizem S, Mercer BA, Roush WR, Heller S, Hodder P.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Mar 21 [updated 2013 Sep 3].


Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents.

Choi JY, Calvet CM, Gunatilleke SS, Ruiz C, Cameron MD, McKerrow JH, Podust LM, Roush WR.

J Med Chem. 2013 Oct 10;56(19):7651-68. doi: 10.1021/jm401067s. Epub 2013 Sep 30.

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