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Novel alanine serine cysteine transporter 2 (ASCT2) inhibitors based on sulfonamide and sulfonic acid ester scaffolds.

Ndaru E, Garibsingh RA, Shi Y, Wallace E, Zakrepine P, Wang J, Schlessinger A, Grewer C.

J Gen Physiol. 2019 Feb 4. pii: jgp.201812276. doi: 10.1085/jgp.201812276. [Epub ahead of print]


An IRAK1-PIN1 signalling axis drives intrinsic tumour resistance to radiation therapy.

Liu PH, Shah RB, Li Y, Arora A, Ung PM, Raman R, Gorbatenko A, Kozono S, Zhou XZ, Brechin V, Barbaro JM, Thompson R, White RM, Aguirre-Ghiso JA, Heymach JV, Lu KP, Silva JM, Panageas KS, Schlessinger A, Maki RG, Skinner HD, de Stanchina E, Sidi S.

Nat Cell Biol. 2019 Feb;21(2):203-213. doi: 10.1038/s41556-018-0260-7. Epub 2019 Jan 21.


Encounter and React: Computer-Guided Design of Covalent Inhibitors.

Ung PM, DeVita RJ, Schlessinger A.

Cell Chem Biol. 2019 Jan 17;26(1):6-8. doi: 10.1016/j.chembiol.2018.12.009.


SLC13A3 variants cause acute reversible leukoencephalopathy and α-ketoglutarate accumulation.

Dewulf JP, Wiame E, Dorboz I, Elmaleh-Bergès M, Imbard A, Dumitriu D, Rak M, Bourillon A, Helaers R, Malla A, Renaldo F, Boespflug-Tanguy O, Vincent MF, Benoist JF, Wevers RA, Schlessinger A, Van Schaftingen E, Nassogne MC, Schiff M.

Ann Neurol. 2019 Jan 11. doi: 10.1002/ana.25412. [Epub ahead of print]


Association of Autism Spectrum Disorder With Prenatal Exposure to Medication Affecting Neurotransmitter Systems.

Janecka M, Kodesh A, Levine SZ, Lusskin SI, Viktorin A, Rahman R, Buxbaum JD, Schlessinger A, Sandin S, Reichenberg A.

JAMA Psychiatry. 2018 Dec 1;75(12):1217-1224. doi: 10.1001/jamapsychiatry.2018.2728.


KinaMetrix: a web resource to investigate kinase conformations and inhibitor space.

Rahman R, Ung PM, Schlessinger A.

Nucleic Acids Res. 2019 Jan 8;47(D1):D361-D366. doi: 10.1093/nar/gky916.


Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity.

Kumar K, Man-Un Ung P, Wang P, Wang H, Li H, Andrews MK, Stewart AF, Schlessinger A, DeVita RJ.

Eur J Med Chem. 2018 Sep 5;157:1005-1016. doi: 10.1016/j.ejmech.2018.08.007. Epub 2018 Aug 22.


Homology Modeling Informs Ligand Discovery for the Glutamine Transporter ASCT2.

Garibsingh RA, Otte NJ, Ndaru E, Colas C, Grewer C, Holst J, Schlessinger A.

Front Chem. 2018 Jul 24;6:279. doi: 10.3389/fchem.2018.00279. eCollection 2018.


Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1).

Chien HC, Colas C, Finke K, Springer S, Stoner L, Zur AA, Venteicher B, Campbell J, Hall C, Flint A, Augustyn E, Hernandez C, Heeren N, Hansen L, Anthony A, Bauer J, Fotiadis D, Schlessinger A, Giacomini KM, Thomas AA.

J Med Chem. 2018 Aug 23;61(16):7358-7373. doi: 10.1021/acs.jmedchem.8b01007. Epub 2018 Aug 10.


Molecular Modeling of Drug-Transporter Interactions-An International Transporter Consortium Perspective.

Schlessinger A, Welch MA, van Vlijmen H, Korzekwa K, Swaan PW, Matsson P.

Clin Pharmacol Ther. 2018 Nov;104(5):818-835. doi: 10.1002/cpt.1174. Epub 2018 Aug 30.


Redefining the Protein Kinase Conformational Space with Machine Learning.

Ung PM, Rahman R, Schlessinger A.

Cell Chem Biol. 2018 Jul 19;25(7):916-924.e2. doi: 10.1016/j.chembiol.2018.05.002. Epub 2018 May 31.


Effects of Mutations and Ligands on the Thermostability of the l-Arginine/Agmatine Antiporter AdiC and Deduced Insights into Ligand-Binding of Human l-Type Amino Acid Transporters.

Ilgü H, Jeckelmann JM, Colas C, Ucurum Z, Schlessinger A, Fotiadis D.

Int J Mol Sci. 2018 Mar 20;19(3). pii: E918. doi: 10.3390/ijms19030918.


Correction: Generation of G protein-coupled receptor antibodies differentially sensitive to conformational states.

Heimann AS, Gupta A, Gomes I, Rahman R, Schlessinger A, Ferro ES, Unterwald EM, Devi LA.

PLoS One. 2018 Feb 15;13(2):e0193322. doi: 10.1371/journal.pone.0193322. eCollection 2018.


A whole-animal platform to advance a clinical kinase inhibitor into new disease space.

Sonoshita M, Scopton AP, Ung PMU, Murray MA, Silber L, Maldonado AY, Real A, Schlessinger A, Cagan RL, Dar AC.

Nat Chem Biol. 2018 Mar;14(3):291-298. doi: 10.1038/nchembio.2556. Epub 2018 Jan 22.


Multi-targeting Drug Community Challenge.

Schlessinger A, Abagyan R, Carlson HA, Dang KK, Guinney J, Cagan RL.

Cell Chem Biol. 2017 Dec 21;24(12):1434-1435. doi: 10.1016/j.chembiol.2017.12.006. No abstract available.


Chemical Modulation of the Human Oligopeptide Transporter 1, hPepT1.

Colas C, Masuda M, Sugio K, Miyauchi S, Hu Y, Smith DE, Schlessinger A.

Mol Pharm. 2017 Dec 4;14(12):4685-4693. doi: 10.1021/acs.molpharmaceut.7b00775. Epub 2017 Nov 15.


Generation of G protein-coupled receptor antibodies differentially sensitive to conformational states.

Heimann AS, Gupta A, Gomes I, Rayees R, Schlessinger A, Ferro ES, Unterwald EM, Devi LA.

PLoS One. 2017 Nov 1;12(11):e0187306. doi: 10.1371/journal.pone.0187306. eCollection 2017. Erratum in: PLoS One. 2018 Feb 15;13(2):e0193322.


Mapping Functionally Important Residues in the Na+/Dicarboxylate Cotransporter, NaDC1.

Colas C, Schlessinger A, Pajor AM.

Biochemistry. 2017 Aug 22;56(33):4432-4441. doi: 10.1021/acs.biochem.7b00503. Epub 2017 Aug 10.


Human Concentrative Nucleoside Transporter 3 (hCNT3, SLC28A3) Forms a Cyclic Homotrimer.

Stecula A, Schlessinger A, Giacomini KM, Sali A.

Biochemistry. 2017 Jul 11;56(27):3475-3483. doi: 10.1021/acs.biochem.7b00339. Epub 2017 Jun 29.


Structure activity relationships of benzylproline-derived inhibitors of the glutamine transporter ASCT2.

Singh K, Tanui R, Gameiro A, Eisenberg G, Colas C, Schlessinger A, Grewer C.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):398-402. doi: 10.1016/j.bmcl.2016.12.063. Epub 2016 Dec 27.


Impaired Amino Acid Transport at the Blood Brain Barrier Is a Cause of Autism Spectrum Disorder.

Tărlungeanu DC, Deliu E, Dotter CP, Kara M, Janiesch PC, Scalise M, Galluccio M, Tesulov M, Morelli E, Sonmez FM, Bilguvar K, Ohgaki R, Kanai Y, Johansen A, Esharif S, Ben-Omran T, Topcu M, Schlessinger A, Indiveri C, Duncan KE, Caglayan AO, Gunel M, Gleeson JG, Novarino G.

Cell. 2016 Dec 1;167(6):1481-1494.e18. doi: 10.1016/j.cell.2016.11.013.


GEN3VA: aggregation and analysis of gene expression signatures from related studies.

Gundersen GW, Jagodnik KM, Woodland H, Fernandez NF, Sani K, Dohlman AB, Ung PM, Monteiro CD, Schlessinger A, Ma'ayan A.

BMC Bioinformatics. 2016 Nov 15;17(1):461.


SLC Transporters: Structure, Function, and Drug Discovery.

Colas C, Ung PM, Schlessinger A.

Medchemcomm. 2016 Jun 1;7(6):1069-1081. Epub 2016 Mar 28.


LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates.

Zur AA, Chien HC, Augustyn E, Flint A, Heeren N, Finke K, Hernandez C, Hansen L, Miller S, Lin L, Giacomini KM, Colas C, Schlessinger A, Thomas AA.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5000-5006. doi: 10.1016/j.bmcl.2016.09.001. Epub 2016 Sep 3.


Molecular Basis for Redox Activation of Epidermal Growth Factor Receptor Kinase.

Truong TH, Ung PM, Palde PB, Paulsen CE, Schlessinger A, Carroll KS.

Cell Chem Biol. 2016 Jul 21;23(7):837-848. doi: 10.1016/j.chembiol.2016.05.017. Epub 2016 Jul 14.


Mutations in the Na(+)/citrate cotransporter NaCT (SLC13A5) in pediatric patients with epilepsy and developmental delay.

Klotz J, Porter BE, Colas C, Schlessinger A, Pajor AM.

Mol Med. 2016 May 26;22. doi: 10.2119/molmed.2016.00077.


Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.

Ung PM, Song W, Cheng L, Zhao X, Hu H, Chen L, Schlessinger A.

ACS Chem Biol. 2016 Jul 15;11(7):1908-16. doi: 10.1021/acschembio.6b00304. Epub 2016 May 11.


LAT-1 activity of meta-substituted phenylalanine and tyrosine analogs.

Augustyn E, Finke K, Zur AA, Hansen L, Heeren N, Chien HC, Lin L, Giacomini KM, Colas C, Schlessinger A, Thomas AA.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2616-2621. doi: 10.1016/j.bmcl.2016.04.023. Epub 2016 Apr 11.


Computing Substrate Selectivity in a Peptide Transporter.

Colas C, Smith DE, Schlessinger A.

Cell Chem Biol. 2016 Feb 18;23(2):211-213. doi: 10.1016/j.chembiol.2016.02.001.


Interaction of Bacillus subtilis Polynucleotide Phosphorylase and RNase Y: STRUCTURAL MAPPING AND EFFECT ON mRNA TURNOVER.

Salvo E, Alabi S, Liu B, Schlessinger A, Bechhofer DH.

J Biol Chem. 2016 Mar 25;291(13):6655-63. doi: 10.1074/jbc.M115.711044. Epub 2016 Jan 21.


Ligand Discovery for the Alanine-Serine-Cysteine Transporter (ASCT2, SLC1A5) from Homology Modeling and Virtual Screening.

Colas C, Grewer C, Otte NJ, Gameiro A, Albers T, Singh K, Shere H, Bonomi M, Holst J, Schlessinger A.

PLoS Comput Biol. 2015 Oct 7;11(10):e1004477. doi: 10.1371/journal.pcbi.1004477. eCollection 2015 Oct.


Environmental Pressure May Change the Composition Protein Disorder in Prokaryotes.

Vicedo E, Schlessinger A, Rost B.

PLoS One. 2015 Aug 7;10(8):e0133990. doi: 10.1371/journal.pone.0133990. eCollection 2015.


Structure-Based Identification of Inhibitors for the SLC13 Family of Na(+)/Dicarboxylate Cotransporters.

Colas C, Pajor AM, Schlessinger A.

Biochemistry. 2015 Aug 11;54(31):4900-8. doi: 10.1021/acs.biochem.5b00388. Epub 2015 Jul 30.


DFGmodel: predicting protein kinase structures in inactive states for structure-based discovery of type-II inhibitors.

Ung PM, Schlessinger A.

ACS Chem Biol. 2015 Jan 16;10(1):269-78. doi: 10.1021/cb500696t. Epub 2014 Dec 9.


Loss-of-function variants of SETD5 cause intellectual disability and the core phenotype of microdeletion 3p25.3 syndrome.

Kuechler A, Zink AM, Wieland T, Lüdecke HJ, Cremer K, Salviati L, Magini P, Najafi K, Zweier C, Czeschik JC, Aretz S, Endele S, Tamburrino F, Pinato C, Clementi M, Gundlach J, Maylahn C, Mazzanti L, Wohlleber E, Schwarzmayr T, Kariminejad R, Schlessinger A, Wieczorek D, Strom TM, Novarino G, Engels H.

Eur J Hum Genet. 2015 Jun;23(6):753-60. doi: 10.1038/ejhg.2014.165. Epub 2014 Aug 20.


Determinants of substrate and cation transport in the human Na+/dicarboxylate cotransporter NaDC3.

Schlessinger A, Sun NN, Colas C, Pajor AM.

J Biol Chem. 2014 Jun 13;289(24):16998-7008. doi: 10.1074/jbc.M114.554790. Epub 2014 May 7.


PredictProtein--an open resource for online prediction of protein structural and functional features.

Yachdav G, Kloppmann E, Kajan L, Hecht M, Goldberg T, Hamp T, Hönigschmid P, Schafferhans A, Roos M, Bernhofer M, Richter L, Ashkenazy H, Punta M, Schlessinger A, Bromberg Y, Schneider R, Vriend G, Sander C, Ben-Tal N, Rost B.

Nucleic Acids Res. 2014 Jul;42(Web Server issue):W337-43. doi: 10.1093/nar/gku366. Epub 2014 May 5.


Co-expression and co-localization of hub proteins and their partners are encoded in protein sequence.

Feiglin A, Ashkenazi S, Schlessinger A, Rost B, Ofran Y.

Mol Biosyst. 2014 Apr;10(4):787-94. doi: 10.1039/c3mb70411d. Epub 2014 Jan 23.


SLC classification: an update.

Schlessinger A, Yee SW, Sali A, Giacomini KM.

Clin Pharmacol Ther. 2013 Jul;94(1):19-23. doi: 10.1038/clpt.2013.73.


Structural basis for alternating access of a eukaryotic calcium/proton exchanger.

Waight AB, Pedersen BP, Schlessinger A, Bonomi M, Chau BH, Roe-Zurz Z, Risenmay AJ, Sali A, Stroud RM.

Nature. 2013 Jul 4;499(7456):107-10. doi: 10.1038/nature12233. Epub 2013 May 19.


Molecular modeling and ligand docking for solute carrier (SLC) transporters.

Schlessinger A, Khuri N, Giacomini KM, Sali A.

Curr Top Med Chem. 2013;13(7):843-56. Review.


Evolution of modular intraflagellar transport from a coatomer-like progenitor.

van Dam TJ, Townsend MJ, Turk M, Schlessinger A, Sali A, Field MC, Huynen MA.

Proc Natl Acad Sci U S A. 2013 Apr 23;110(17):6943-8. doi: 10.1073/pnas.1221011110. Epub 2013 Apr 8.


Crystal structure of a eukaryotic phosphate transporter.

Pedersen BP, Kumar H, Waight AB, Risenmay AJ, Roe-Zurz Z, Chau BH, Schlessinger A, Bonomi M, Harries W, Sali A, Johri AK, Stroud RM.

Nature. 2013 Apr 25;496(7446):533-6. doi: 10.1038/nature12042. Epub 2013 Mar 31.


Structure-based ligand discovery for the Large-neutral Amino Acid Transporter 1, LAT-1.

Geier EG, Schlessinger A, Fan H, Gable JE, Irwin JJ, Sali A, Giacomini KM.

Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5480-5. doi: 10.1073/pnas.1218165110. Epub 2013 Mar 18.


Coordinating the impact of structural genomics on the human α-helical transmembrane proteome.

Pieper U, Schlessinger A, Kloppmann E, Chang GA, Chou JJ, Dumont ME, Fox BG, Fromme P, Hendrickson WA, Malkowski MG, Rees DC, Stokes DL, Stowell MH, Wiener MC, Rost B, Stroud RM, Stevens RC, Sali A.

Nat Struct Mol Biol. 2013 Feb;20(2):135-8. doi: 10.1038/nsmb.2508. No abstract available.


High selectivity of the γ-aminobutyric acid transporter 2 (GAT-2, SLC6A13) revealed by structure-based approach.

Schlessinger A, Wittwer MB, Dahlin A, Khuri N, Bonomi M, Fan H, Giacomini KM, Sali A.

J Biol Chem. 2012 Nov 2;287(45):37745-56. doi: 10.1074/jbc.M112.388157. Epub 2012 Aug 29.


A common 5'-UTR variant in MATE2-K is associated with poor response to metformin.

Choi JH, Yee SW, Ramirez AH, Morrissey KM, Jang GH, Joski PJ, Mefford JA, Hesselson SE, Schlessinger A, Jenkins G, Castro RA, Johns SJ, Stryke D, Sali A, Ferrin TE, Witte JS, Kwok PY, Roden DM, Wilke RA, McCarty CA, Davis RL, Giacomini KM.

Clin Pharmacol Ther. 2011 Nov;90(5):674-84. doi: 10.1038/clpt.2011.165. Epub 2011 Sep 28.


Ligand discovery from a dopamine D3 receptor homology model and crystal structure.

Carlsson J, Coleman RG, Setola V, Irwin JJ, Fan H, Schlessinger A, Sali A, Roth BL, Shoichet BK.

Nat Chem Biol. 2011 Sep 18;7(11):769-78. doi: 10.1038/nchembio.662.


Structure-based discovery of prescription drugs that interact with the norepinephrine transporter, NET.

Schlessinger A, Geier E, Fan H, Irwin JJ, Shoichet BK, Giacomini KM, Sali A.

Proc Natl Acad Sci U S A. 2011 Sep 20;108(38):15810-5. doi: 10.1073/pnas.1106030108. Epub 2011 Sep 1.


Protein disorder--a breakthrough invention of evolution?

Schlessinger A, Schaefer C, Vicedo E, Schmidberger M, Punta M, Rost B.

Curr Opin Struct Biol. 2011 Jun;21(3):412-8. doi: 10.1016/ Epub 2011 Apr 20. Review.


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