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Items: 1 to 50 of 167

1.

Age- and stress-associated C. elegans granulins impair lysosomal function and induce a compensatory HLH-30/TFEB transcriptional response.

Butler VJ, Gao F, Corrales CI, Cortopassi WA, Caballero B, Vohra M, Ashrafi K, Cuervo AM, Jacobson MP, Coppola G, Kao AW.

PLoS Genet. 2019 Aug 9;15(8):e1008295. doi: 10.1371/journal.pgen.1008295. eCollection 2019 Aug.

2.

ATP-Competitive Inhibitors Midostaurin and Avapritinib Have Distinct Resistance Profiles in Exon 17-Mutant KIT.

Apsel Winger B, Cortopassi WA, Garrido Ruiz D, Ding L, Jang K, Leyte-Vidal A, Zhang N, Esteve-Puig R, Jacobson MP, Shah NP.

Cancer Res. 2019 Aug 15;79(16):4283-4292. doi: 10.1158/0008-5472.CAN-18-3139. Epub 2019 Jul 3.

PMID:
31270078
3.

Multi-Granulin Domain Peptides Bind to Pro-Cathepsin D and Stimulate Its Enzymatic Activity More Effectively Than Progranulin in Vitro.

Butler VJ, Cortopassi WA, Gururaj S, Wang AL, Pierce OM, Jacobson MP, Kao AW.

Biochemistry. 2019 Jun 11;58(23):2670-2674. doi: 10.1021/acs.biochem.9b00275. Epub 2019 May 24.

PMID:
31099551
4.

Tau repeat regions contain conserved histidine residues that modulate microtubule-binding in response to changes in pH.

Charafeddine RA, Cortopassi WA, Lak P, Tan R, McKenney RJ, Jacobson MP, Barber DL, Wittmann T.

J Biol Chem. 2019 May 31;294(22):8779-8790. doi: 10.1074/jbc.RA118.007004. Epub 2019 Apr 16.

PMID:
30992364
5.

Conformational Dynamics of the HIV-Vif Protein Complex.

Ball KA, Chan LM, Stanley DJ, Tierney E, Thapa S, Ta HM, Burton L, Binning JM, Jacobson MP, Gross JD.

Biophys J. 2019 Apr 23;116(8):1432-1445. doi: 10.1016/j.bpj.2019.03.014. Epub 2019 Mar 23.

PMID:
30961890
6.

Structure-based identification of novel CK2 inhibitors with a linear 2-propenone scaffold as anti-cancer agents.

Qi X, Zhang N, Zhao L, Hu L, Cortopassi WA, Jacobson MP, Li X, Zhong R.

Biochem Biophys Res Commun. 2019 Apr 30;512(2):208-212. doi: 10.1016/j.bbrc.2019.03.016. Epub 2019 Mar 14.

PMID:
30878184
7.

Covalent Modification and Regulation of the Nuclear Receptor Nurr1 by a Dopamine Metabolite.

Bruning JM, Wang Y, Oltrabella F, Tian B, Kholodar SA, Liu H, Bhattacharya P, Guo S, Holton JM, Fletterick RJ, Jacobson MP, England PM.

Cell Chem Biol. 2019 May 16;26(5):674-685.e6. doi: 10.1016/j.chembiol.2019.02.002. Epub 2019 Mar 7.

PMID:
30853418
8.

Progranulin Stimulates the In Vitro Maturation of Pro-Cathepsin D at Acidic pH.

Butler VJ, Cortopassi WA, Argouarch AR, Ivry SL, Craik CS, Jacobson MP, Kao AW.

J Mol Biol. 2019 Mar 1;431(5):1038-1047. doi: 10.1016/j.jmb.2019.01.027. Epub 2019 Jan 25.

PMID:
30690031
9.

Probing the Electrostatic and Steric Requirements for Substrate Binding in Human Platelet-Type 12-Lipoxygenase.

Aleem AM, Tsai WC, Tena J, Alvarez G, Deschamps J, Kalyanaraman C, Jacobson MP, Holman T.

Biochemistry. 2019 Feb 12;58(6):848-857. doi: 10.1021/acs.biochem.8b01167. Epub 2019 Jan 4.

PMID:
30565457
10.

Inhibitor binding mode and allosteric regulation of Na+-glucose symporters.

Bisignano P, Ghezzi C, Jo H, Polizzi NF, Althoff T, Kalyanaraman C, Friemann R, Jacobson MP, Wright EM, Grabe M.

Nat Commun. 2018 Dec 7;9(1):5245. doi: 10.1038/s41467-018-07700-1.

11.

Structure-based Discovery of Novel CK2α-Binding Cyclic Peptides with Anti-cancer Activity.

Tang S, Zhang N, Zhou Y, Cortopassi WA, Jacobson MP, Zhao LJ, Zhong RG.

Mol Inform. 2019 Mar;38(3):e1800089. doi: 10.1002/minf.201800089. Epub 2018 Oct 11.

PMID:
30307134
12.

Exploration of Benzothiazole Rhodacyanines as Allosteric Inhibitors of Protein-Protein Interactions with Heat Shock Protein 70 (Hsp70).

Shao H, Li X, Moses MA, Gilbert LA, Kalyanaraman C, Young ZT, Chernova M, Journey SN, Weissman JS, Hann B, Jacobson MP, Neckers L, Gestwicki JE.

J Med Chem. 2018 Jul 26;61(14):6163-6177. doi: 10.1021/acs.jmedchem.8b00583. Epub 2018 Jul 13.

13.

Exposure-safety and efficacy response relationships and population pharmacokinetics of eslicarbazepine acetate.

Gidal BE, Jacobson MP, Ben-Menachem E, Carreño M, Blum D, Soares-da-Silva P, Falcão A, Rocha F, Moreira J, Grinnell T, Ludwig E, Fiedler-Kelly J, Passarell J, Sunkaraneni S.

Acta Neurol Scand. 2018 Sep;138(3):203-211. doi: 10.1111/ane.12950. Epub 2018 May 6.

14.

A recurrent kinase domain mutation in PRKCA defines chordoid glioma of the third ventricle.

Goode B, Mondal G, Hyun M, Ruiz DG, Lin YH, Van Ziffle J, Joseph NM, Onodera C, Talevich E, Grenert JP, Hewedi IH, Snuderl M, Brat DJ, Kleinschmidt-DeMasters BK, Rodriguez FJ, Louis DN, Yong WH, Lopes MB, Rosenblum MK, Butowski N, Tihan T, Bollen AW, Phillips JJ, Wiita AP, Yeh I, Jacobson MP, Bastian BC, Perry A, Solomon DA.

Nat Commun. 2018 Feb 23;9(1):810. doi: 10.1038/s41467-018-02826-8.

15.

High-throughput screen for inhibitors of protein-protein interactions in a reconstituted heat shock protein 70 (Hsp70) complex.

Taylor IR, Dunyak BM, Komiyama T, Shao H, Ran X, Assimon VA, Kalyanaraman C, Rauch JN, Jacobson MP, Zuiderweg ERP, Gestwicki JE.

J Biol Chem. 2018 Mar 16;293(11):4014-4025. doi: 10.1074/jbc.RA117.001575. Epub 2018 Feb 2.

16.

Prediction of enzymatic pathways by integrative pathway mapping.

Calhoun S, Korczynska M, Wichelecki DJ, San Francisco B, Zhao S, Rodionov DA, Vetting MW, Al-Obaidi NF, Lin H, O'Meara MJ, Scott DA, Morris JH, Russel D, Almo SC, Osterman AL, Gerlt JA, Jacobson MP, Shoichet BK, Sali A.

Elife. 2018 Jan 29;7. pii: e31097. doi: 10.7554/eLife.31097.

17.

Evolutionarily Conserved Roles for Blood-Brain Barrier Xenobiotic Transporters in Endogenous Steroid Partitioning and Behavior.

Hindle SJ, Munji RN, Dolghih E, Gaskins G, Orng S, Ishimoto H, Soung A, DeSalvo M, Kitamoto T, Keiser MJ, Jacobson MP, Daneman R, Bainton RJ.

Cell Rep. 2017 Oct 31;21(5):1304-1316. doi: 10.1016/j.celrep.2017.10.026.

18.

Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.

Boehm M, Beaumont K, Jones R, Kalgutkar AS, Zhang L, Atkinson K, Bai G, Brown JA, Eng H, Goetz GH, Holder BR, Khunte B, Lazzaro S, Limberakis C, Ryu S, Shapiro MJ, Tylaska L, Yan J, Turner R, Leung SSF, Ramaseshan M, Price DA, Liras S, Jacobson MP, Earp DJ, Lokey RS, Mathiowetz AM, Menhaji-Klotz E.

J Med Chem. 2017 Dec 14;60(23):9653-9663. doi: 10.1021/acs.jmedchem.7b01028. Epub 2017 Oct 30.

19.

Development of 5N-Bicalutamide, a High-Affinity Reversible Covalent Antiandrogen.

de Jesus Cortez F, Nguyen P, Truillet C, Tian B, Kuchenbecker KM, Evans MJ, Webb P, Jacobson MP, Fletterick RJ, England PM.

ACS Chem Biol. 2017 Dec 15;12(12):2934-2939. doi: 10.1021/acschembio.7b00702. Epub 2017 Nov 2.

PMID:
28981251
20.

Cancer-associated arginine-to-histidine mutations confer a gain in pH sensing to mutant proteins.

White KA, Ruiz DG, Szpiech ZA, Strauli NB, Hernandez RD, Jacobson MP, Barber DL.

Sci Signal. 2017 Sep 5;10(495). pii: eaam9931. doi: 10.1126/scisignal.aam9931.

21.

Prominent features of the amino acid mutation landscape in cancer.

Szpiech ZA, Strauli NB, White KA, Ruiz DG, Jacobson MP, Barber DL, Hernandez RD.

PLoS One. 2017 Aug 24;12(8):e0183273. doi: 10.1371/journal.pone.0183273. eCollection 2017.

22.

Synthesis of the Ca2+-mobilizing messengers NAADP and cADPR by intracellular CD38 enzyme in the mouse heart: Role in β-adrenoceptor signaling.

Lin WK, Bolton EL, Cortopassi WA, Wang Y, O'Brien F, Maciejewska M, Jacobson MP, Garnham C, Ruas M, Parrington J, Lei M, Sitsapesan R, Galione A, Terrar DA.

J Biol Chem. 2017 Aug 11;292(32):13243-13257. doi: 10.1074/jbc.M117.789347. Epub 2017 May 24.

23.

Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin.

Metcalf B, Chuang C, Dufu K, Patel MP, Silva-Garcia A, Johnson C, Lu Q, Partridge JR, Patskovska L, Patskovsky Y, Almo SC, Jacobson MP, Hua L, Xu Q, Gwaltney SL 2nd, Yee C, Harris J, Morgan BP, James J, Xu D, Hutchaleelaha A, Paulvannan K, Oksenberg D, Li Z.

ACS Med Chem Lett. 2017 Jan 23;8(3):321-326. doi: 10.1021/acsmedchemlett.6b00491. eCollection 2017 Mar 9.

24.

Structure-Activity Relationship and Molecular Mechanics Reveal the Importance of Ring Entropy in the Biosynthesis and Activity of a Natural Product.

Tran HL, Lexa KW, Julien O, Young TS, Walsh CT, Jacobson MP, Wells JA.

J Am Chem Soc. 2017 Feb 22;139(7):2541-2544. doi: 10.1021/jacs.6b10792. Epub 2017 Feb 13.

25.

Dihedral Angle-Based Sampling of Natural Product Polyketide Conformations: Application to Permeability Prediction.

Wang Q, Sciabola S, Barreiro G, Hou X, Bai G, Shapiro MJ, Koehn F, Villalobos A, Jacobson MP.

J Chem Inf Model. 2016 Nov 28;56(11):2194-2206. Epub 2016 Oct 21.

PMID:
27731994
26.

Human 15-LOX-1 active site mutations alter inhibitor binding and decrease potency.

Armstrong M, van Hoorebeke C, Horn T, Deschamps J, Freedman JC, Kalyanaraman C, Jacobson MP, Holman T.

Bioorg Med Chem. 2016 Nov 1;24(21):5380-5387. doi: 10.1016/j.bmc.2016.08.063. Epub 2016 Aug 31.

27.

GluA1 signal peptide determines the spatial assembly of heteromeric AMPA receptors.

He XY, Li YJ, Kalyanaraman C, Qiu LL, Chen C, Xiao Q, Liu WX, Zhang W, Yang JJ, Chen G, Jacobson MP, Shi YS.

Proc Natl Acad Sci U S A. 2016 Sep 20;113(38):E5645-54. doi: 10.1073/pnas.1524358113. Epub 2016 Sep 6.

28.

Defining the Product Chemical Space of Monoterpenoid Synthases.

Tian B, Poulter CD, Jacobson MP.

PLoS Comput Biol. 2016 Aug 12;12(8):e1005053. doi: 10.1371/journal.pcbi.1005053. eCollection 2016 Aug.

29.

Disulfide-Trapping Identifies a New, Effective Chemical Probe for Activating the Nuclear Receptor Human LRH-1 (NR5A2).

de Jesus Cortez F, Suzawa M, Irvy S, Bruning JM, Sablin E, Jacobson MP, Fletterick RJ, Ingraham HA, England PM.

PLoS One. 2016 Jul 28;11(7):e0159316. doi: 10.1371/journal.pone.0159316. eCollection 2016.

30.

Exhaustive Conformational Sampling of Complex Fused Ring Macrocycles Using Inverse Kinematics.

Coutsias EA, Lexa KW, Wester MJ, Pollock SN, Jacobson MP.

J Chem Theory Comput. 2016 Sep 13;12(9):4674-87. doi: 10.1021/acs.jctc.6b00250. Epub 2016 Aug 4.

31.

Assignment of function to a domain of unknown function: DUF1537 is a new kinase family in catabolic pathways for acid sugars.

Zhang X, Carter MS, Vetting MW, San Francisco B, Zhao S, Al-Obaidi NF, Solbiati JO, Thiaville JJ, de Crécy-Lagard V, Jacobson MP, Almo SC, Gerlt JA.

Proc Natl Acad Sci U S A. 2016 Jul 19;113(29):E4161-9. doi: 10.1073/pnas.1605546113. Epub 2016 Jul 11.

32.

Non-degradative Ubiquitination of Protein Kinases.

Ball KA, Johnson JR, Lewinski MK, Guatelli J, Verschueren E, Krogan NJ, Jacobson MP.

PLoS Comput Biol. 2016 Jun 2;12(6):e1004898. doi: 10.1371/journal.pcbi.1004898. eCollection 2016 Jun.

33.

Simple Predictive Models of Passive Membrane Permeability Incorporating Size-Dependent Membrane-Water Partition.

Leung SS, Sindhikara D, Jacobson MP.

J Chem Inf Model. 2016 May 23;56(5):924-9. doi: 10.1021/acs.jcim.6b00005. Epub 2016 May 2.

PMID:
27135806
34.

Conversion to eslicarbazepine acetate monotherapy: A pooled analysis of 2 phase III studies.

Sperling MR, French J, Jacobson MP, Pazdera L, Gough M, Cheng H, Grinnell T, Blum D; Study 045 and 046 Investigators.

Neurology. 2016 Mar 22;86(12):1095-102. doi: 10.1212/WNL.0000000000002497. Epub 2016 Feb 24.

35.

A potent and selective inhibitor targeting human and murine 12/15-LOX.

Armstrong MM, Freedman CJ, Jung JE, Zheng Y, Kalyanaraman C, Jacobson MP, Simeonov A, Maloney DJ, van Leyen K, Jadhav A, Holman TR.

Bioorg Med Chem. 2016 Mar 15;24(6):1183-90. doi: 10.1016/j.bmc.2016.01.042. Epub 2016 Jan 21.

36.

Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni.

Long T, Neitz RJ, Beasley R, Kalyanaraman C, Suzuki BM, Jacobson MP, Dissous C, McKerrow JH, Drewry DH, Zuercher WJ, Singh R, Caffrey CR.

PLoS Negl Trop Dis. 2016 Jan 11;10(1):e0004356. doi: 10.1371/journal.pntd.0004356. eCollection 2016 Jan.

37.

Beyond cyclosporine A: conformation-dependent passive membrane permeabilities of cyclic peptide natural products.

Ahlbach CL, Lexa KW, Bockus AT, Chen V, Crews P, Jacobson MP, Lokey RS.

Future Med Chem. 2015;7(16):2121-30. doi: 10.4155/fmc.15.78. Epub 2015 Jun 12.

38.

Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides.

Schwochert J, Turner R, Thang M, Berkeley RF, Ponkey AR, Rodriguez KM, Leung SS, Khunte B, Goetz G, Limberakis C, Kalgutkar AS, Eng H, Shapiro MJ, Mathiowetz AM, Price DA, Liras S, Jacobson MP, Lokey RS.

Org Lett. 2015 Jun 19;17(12):2928-31. doi: 10.1021/acs.orglett.5b01162. Epub 2015 Jun 5.

PMID:
26046483
39.

Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products.

Bockus AT, Lexa KW, Pye CR, Kalgutkar AS, Gardner JW, Hund KC, Hewitt WM, Schwochert JA, Glassey E, Price DA, Mathiowetz AM, Liras S, Jacobson MP, Lokey RS.

J Med Chem. 2015 Jun 11;58(11):4581-9. doi: 10.1021/acs.jmedchem.5b00128. Epub 2015 May 20.

PMID:
25950816
40.

Computational-guided discovery and characterization of a sesquiterpene synthase from Streptomyces clavuligerus.

Chow JY, Tian BX, Ramamoorthy G, Hillerich BS, Seidel RD, Almo SC, Jacobson MP, Poulter CD.

Proc Natl Acad Sci U S A. 2015 May 5;112(18):5661-6. doi: 10.1073/pnas.1505127112. Epub 2015 Apr 21.

41.

Efficacy and safety of conversion to monotherapy with eslicarbazepine acetate in adults with uncontrolled partial-onset seizures: a historical-control phase III study.

Jacobson MP, Pazdera L, Bhatia P, Grinnell T, Cheng H, Blum D; study 046 team.

BMC Neurol. 2015 Mar 28;15:46. doi: 10.1186/s12883-015-0305-5.

42.

Characteristics and acute outcomes of ICU patients with initial presentation of seizure.

Tobochnik S, Gutierrez C, Jacobson MP.

Seizure. 2015 Mar;26:94-7. doi: 10.1016/j.seizure.2015.01.016. Epub 2015 Feb 4.

43.

Synthesis and enzymatic studies of bisubstrate analogues for farnesyl diphosphate synthase.

Ramamoorthy G, Pugh ML, Tian BX, Phan RM, Perez LB, Jacobson MP, Poulter CD.

J Org Chem. 2015 Apr 17;80(8):3902-13. doi: 10.1021/acs.joc.5b00202. Epub 2015 Mar 26.

PMID:
25734506
44.

A Fragment-Based Ligand Screen Against Part of a Large Protein Machine: The ND1 Domains of the AAA+ ATPase p97/VCP.

Chimenti MS, Bulfer SL, Neitz RJ, Renslo AR, Jacobson MP, James TL, Arkin MR, Kelly MJ.

J Biomol Screen. 2015 Jul;20(6):788-800. doi: 10.1177/1087057115570550. Epub 2015 Feb 17.

PMID:
25690569
45.

A unique cis-3-hydroxy-l-proline dehydratase in the enolase superfamily.

Zhang X, Kumar R, Vetting MW, Zhao S, Jacobson MP, Almo SC, Gerlt JA.

J Am Chem Soc. 2015 Feb 4;137(4):1388-91. doi: 10.1021/ja5103986. Epub 2015 Jan 26.

PMID:
25608448
46.

Experimental strategies for functional annotation and metabolism discovery: targeted screening of solute binding proteins and unbiased panning of metabolomes.

Vetting MW, Al-Obaidi N, Zhao S, San Francisco B, Kim J, Wichelecki DJ, Bouvier JT, Solbiati JO, Vu H, Zhang X, Rodionov DA, Love JD, Hillerich BS, Seidel RD, Quinn RJ, Osterman AL, Cronan JE, Jacobson MP, Gerlt JA, Almo SC.

Biochemistry. 2015 Jan 27;54(3):909-31. doi: 10.1021/bi501388y. Epub 2015 Jan 16.

47.

Cell-permeable cyclic peptides from synthetic libraries inspired by natural products.

Hewitt WM, Leung SS, Pye CR, Ponkey AR, Bednarek M, Jacobson MP, Lokey RS.

J Am Chem Soc. 2015 Jan 21;137(2):715-21. doi: 10.1021/ja508766b. Epub 2015 Jan 8.

PMID:
25517352
48.

Predicting the functions and specificity of triterpenoid synthases: a mechanism-based multi-intermediate docking approach.

Tian BX, Wallrapp FH, Holiday GL, Chow JY, Babbitt PC, Poulter CD, Jacobson MP.

PLoS Comput Biol. 2014 Oct 9;10(10):e1003874. doi: 10.1371/journal.pcbi.1003874. eCollection 2014 Oct.

49.

A new coarse-grained model for E. coli cytoplasm: accurate calculation of the diffusion coefficient of proteins and observation of anomalous diffusion.

Hasnain S, McClendon CL, Hsu MT, Jacobson MP, Bandyopadhyay P.

PLoS One. 2014 Sep 2;9(9):e106466. doi: 10.1371/journal.pone.0106466. eCollection 2014.

50.

Design of reversible, cysteine-targeted Michael acceptors guided by kinetic and computational analysis.

Krishnan S, Miller RM, Tian B, Mullins RD, Jacobson MP, Taunton J.

J Am Chem Soc. 2014 Sep 10;136(36):12624-30. doi: 10.1021/ja505194w. Epub 2014 Sep 2. Erratum in: J Am Chem Soc. 2014 Dec 17;136(50):17690.

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