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Publikationer i urvalet

18 träffar

Bibliografisk träff 2023-08-22

Discovery of WLB-89462, a New Drug-like and Highly Selective σ2 Receptor Ligand with Neuroprotective Properties.

Christmann U, Díaz JL, Pascual R, Bordas M, Álvarez I, Monroy X, Porras M, Yeste S, Reinoso RF, Merlos M, Vela JM, Almansa C.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.3c01060

Bibliografisk träff 2023-08-03

Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.

Dichiara M, Ambrosio FA, Lee SM, Ruiz-Cantero MC, Lombino J, Coricello A, Costa G, Shah D, Costanzo G, Pasquinucci L, Son KN, Cosentino G, González-Cano R, Marrazzo A, Aakalu VK, Cobos EJ, Alcaro S, Amata E.

J Med Chem · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.3c00959

Bibliografisk träff 2023-03-15

Development of Fluorescent 4-[4-(3H-Spiro[isobenzofuran-1,4'-piperidin]-1'-yl)butyl]indolyl Derivatives as High-Affinity Probes to Enable the Study of σ Receptors via Fluorescence-Based Techniques.

Abatematteo FS, Majellaro M, Montsch B, Prieto-Díaz R, Niso M, Contino M, Stefanachi A, Riganti C, Mangiatordi GF, Delre P, Heffeter P, Sotelo E, Abate C.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.2c01227

Bibliografisk träff 2023-01-24

Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.

Roy J, Kyani A, Hanafi M, Xu Y, Takyi-Williams J, Sun D, Osman EEA, Neamati N.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.2c01769

Bibliografisk träff 2022-09-26

Structure-activity relationships of mixed σ1R/σ2R ligands with antiproliferative and anticancer effects.

Fallica AN, Ciaffaglione V, Modica MN, Pittalà V, Salerno L, Amata E, Marrazzo A, Romeo G, Intagliata S.

Bioorg Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1016/j.bmc.2022.117032

Bibliografisk träff 2022-06-17

Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.

Zampieri D, Fortuna S, Romano M, Amata E, Dichiara M, Marrazzo A, Pasquinucci L, Turnaturi R, Mamolo MG.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2022.128860

Bibliografisk träff 2020-10-07

Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective σ2R/TMEM97 ligands.

Xie XY, Li YY, Ma WH, Chen AF, Sun YT, Lee JY, Riad A, Xu DH, Mach RH, Huang YS.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112906

Bibliografisk träff 2020-04-30

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.

Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL, Tummino TA, Hüttenhain R, Kaake RM, Richards AL, Tutuncuoglu B, Foussard H, Batra J, Haas K, Modak M, Kim M, Haas P, Polacco BJ, Braberg H, Fabius JM, Eckhardt M, Soucheray M, Bennett MJ, Cakir M, McGregor MJ, Li Q, Meyer B, Roesch F, Vallet T, Mac Kain A, Miorin L, Moreno E, Naing ZZC, Zhou Y, Peng S, Shi Y, Zhang Z, Shen W, Kirby IT, Melnyk JE, Chorba JS, Lou K, Dai SA, Barrio-Hernandez I, Memon D, Hernandez-Armenta C, Lyu J, Mathy CJP, Perica T, Pilla KB, Ganesan SJ, Saltzberg DJ, Rakesh R, Liu X, Rosenthal SB, Calviello L, Venkataramanan S, Liboy-Lugo J, Lin Y, Huang XP, Liu Y, Wankowicz SA, Bohn M, Safari M, Ugur FS, Koh C, Savar NS, Tran QD, Shengjuler D, Fletcher SJ, O'Neal MC, Cai Y, Chang JCJ, Broadhurst DJ, Klippsten S, Sharp PP, Wenzell NA, Kuzuoglu-Ozturk D, Wang HY, Trenker R, Young JM, Cavero DA, Hiatt J, Roth TL, Rathore U, Subramanian A, Noack J, Hubert M, Stroud RM, Frankel AD, Rosenberg OS, Verba KA, Agard DA, Ott M, Emerman M, Jura N, von Zastrow M, Verdin E, Ashworth A, Schwartz O, d'Enfert C, Mukherjee S, Jacobson M, Malik HS, Fujimori DG, Ideker T, Craik CS, Floor SN, Fraser JS, Gross JD, Sali A, Roth BL, Ruggero D, Taunton J, Kortemme T, Beltrao P, Vignuzzi M, García-Sastre A, Shokat KM, Shoichet BK, Krogan NJ.

Nature · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1038/s41586-020-2286-9

Bibliografisk träff 2018-10-24

Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.

Bergkemper M, Kronenberg E, Thum S, Börgel F, Daniliuc C, Schepmann D, Nieto FR, Brust P, Reinoso RF, Alvarez I, Wünsch B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.8b01183

Bibliografisk träff 2018-08-15

New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation.

Zampieri D, Romano M, Menegazzi R, Mamolo MG.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2018.08.016

Bibliografisk träff 2017-11-09

Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.

Sun YT, Wang GF, Yang YQ, Jin F, Wang Y, Xie XY, Mach RH, Huang YS.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.11.016

Bibliografisk träff 2016-08-31

Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents.

Rui M, Rossi D, Marra A, Paolillo M, Schinelli S, Curti D, Tesei A, Cortesi M, Zamagni A, Laurini E, Pricl S, Schepmann D, Wűnsch B, Urban E, Pace V, Collina S.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2016.08.067

Bibliografisk träff 2014-05-12

Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands.

Bai S, Li S, Xu J, Peng X, Sai K, Chu W, Tu Z, Zeng C, Mach RH.

J Med Chem · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article · DOI 10.1021/jm5001453

Bibliografisk träff 2013-06-18

The σ2 receptor: a novel protein for the imaging and treatment of cancer.

Mach RH, Zeng C, Hawkins WG.

J Med Chem · research-article; review; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1021/jm301545c

Bibliografisk träff 2011-08-29

Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.

Mésangeau C, Amata E, Alsharif W, Seminerio MJ, Robson MJ, Matsumoto RR, Poupaert JH, McCurdy CR.

Eur J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.ejmech.2011.08.031

Bibliografisk träff 2007-09-26

Substituted benzylaminoalkylindoles with preference for the sigma2 binding site.

Mamolo MG, Zampieri D, Zanette C, Florio C, Collina S, Urbano M, Azzolina O, Vio L.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2007.09.012

Bibliografisk träff 1995-05-01

Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.

Perregaard J, Moltzen EK, Meier E, Sánchez C.

J Med Chem · comparative study; journal article · DOI 10.1021/jm00011a019

Bibliografisk träff 1995-05-01

Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.

Moltzen EK, Perregaard J, Meier E.

J Med Chem · journal article · DOI 10.1021/jm00011a020

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Publikationer i urvalet

Discovery of WLB-89462, a New Drug-like and Highly Selective σ<sub>2</sub> Receptor Ligand with Neuroprotective Properties.

Discovery of AD258 as a Sigma Receptor Ligand with Potent Antiallodynic Activity.

Development of Fluorescent 4-[4-(3<i>H</i>-Spiro[isobenzofuran-1,4'-piperidin]-1'-yl)butyl]indolyl Derivatives as High-Affinity Probes to Enable the Study of σ Receptors via Fluorescence-Based Techniques.

Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.

Structure-activity relationships of mixed σ<sub>1</sub>R/σ<sub>2</sub>R ligands with antiproliferative and anticancer effects.

Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.

Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective σ<sub>2</sub>R/TMEM97 ligands.

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.

Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic σ Receptor Ligands with Exocyclic Amino Moiety.

New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation.

Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.

Synthesis and biological evaluation of new aryl-alkyl(alkenyl)-4-benzylpiperidines, novel Sigma Receptor (SR) modulators, as potential anticancer-agents.

Synthesis and structure-activity relationship studies of conformationally flexible tetrahydroisoquinolinyl triazole carboxamide and triazole substituted benzamide analogues as σ2 receptor ligands.

The σ2 receptor: a novel protein for the imaging and treatment of cancer.

Synthesis and pharmacological evaluation of indole-based sigma receptor ligands.

Substituted benzylaminoalkylindoles with preference for the sigma2 binding site.

Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles.

Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 2. Spiro-joined benzofuran, isobenzofuran, and benzopyran piperidines.