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Publikationer i urvalet

51 träffar

Bibliografisk träff 2022-03-02

Selective A3 Adenosine Receptor Antagonist Radioligand for Human and Rodent Species.

Suresh RR, Gao ZG, Salmaso V, Chen E, Campbell RG, Poe RB, Liston TE, Jacobson KA.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.1c00685

Bibliografisk träff 2022-01-10

Interaction of A3 adenosine receptor ligands with the human multidrug transporter ABCG2.

Abel B, Murakami M, Tosh DK, Yu J, Lusvarghi S, Campbell RG, Gao ZG, Jacobson KA, Ambudkar SV.

Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2022.114103

Bibliografisk träff 2021-08-26

Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A3 Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary.

Lee Y, Hou X, Lee JH, Nayak A, Alexander V, Sharma PK, Chang H, Phan K, Gao ZG, Jacobson KA, Choi S, Jeong LS.

J Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.1c00239

Bibliografisk träff 2021-07-13

Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.

Jacobson KA, Salmaso V, Suresh RR, Tosh DK.

RSC Med Chem · review-article; review; journal article · DOI 10.1039/d1md00167a

Bibliografisk träff 2020-04-09

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A3 Adenosine Receptors: Affinity Enhancement by N6-(2-Phenylethyl) Substitution.

Tosh DK, Salmaso V, Rao H, Bitant A, Fisher CL, Lieberman DI, Vorbrüggen H, Reitman ML, Gavrilova O, Gao ZG, Auchampach JA, Jacobson KA.

J Med Chem · research support, n.i.h., intramural; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.0c00235

Bibliografisk träff 2020-02-14

Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A3 Receptor Agonists.

Tosh DK, Salmaso V, Rao H, Campbell R, Bitant A, Gao ZG, Auchampach JA, Jacobson KA.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.9b00637

Bibliografisk träff 2019-11-28

Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.

An S, Yu J, Choi H, Ko H, Ahn S, Shin JC, Pyo JJ, Jeong LS, Noh M.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.115226

Bibliografisk träff 2018-08-20

[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A3 adenosine receptor subtype.

Federico S, Margiotta E, Salmaso V, Pastorin G, Kachler S, Klotz KN, Moro S, Spalluto G.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2018.08.042

Bibliografisk träff 2017-11-09

Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine receptor.

Cosimelli B, Greco G, Laneri S, Novellino E, Sacchi A, Collina S, Rossi D, Cosconati S, Barresi E, Taliani S, Trincavelli ML, Martini C.

Medchemcomm · research-article; journal article · DOI 10.1039/c7md00375g

Bibliografisk träff 2017-08-28

Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.

Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M.

J Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.7b00805

Bibliografisk träff 2017-05-05

Exploring the Role of N6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ∇.

Petrelli R, Scortichini M, Kachler S, Boccella S, Cerchia C, Torquati I, Del Bello F, Salvemini D, Novellino E, Luongo L, Maione S, Jacobson KA, Lavecchia A, Klotz KN, Cappellacci L.

J Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.7b00291

Bibliografisk träff 2017-04-19

N6-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A3 Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation.

Yu J, Zhao LX, Park J, Lee HW, Sahu PK, Cui M, Moss SM, Hammes E, Warnick E, Gao ZG, Noh M, Choi S, Ahn HC, Choi J, Jacobson KA, Jeong LS.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/acs.jmedchem.7b00241

Bibliografisk träff 2016-12-09

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists.

Tosh DK, Ciancetta A, Warnick E, Crane S, Gao ZG, Jacobson KA.

J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.6b01183

Bibliografisk träff 2016-02-18

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.

Tosh DK, Ciancetta A, Warnick E, O'Connor R, Chen Z, Gizewski E, Crane S, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem · research support, n.i.h., intramural; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.5b01998

Bibliografisk träff 2015-09-21

Tactical Approaches to Interconverting GPCR Agonists and Antagonists.

Dosa PI, Amin EA.

J Med Chem · review; journal article · DOI 10.1021/acs.jmedchem.5b00982

Bibliografisk träff 2014-11-25

In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.

Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem · research support, n.i.h., intramural; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm501021n

Bibliografisk träff 2014-05-23

Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.

Toti KS, Moss SM, Paoletta S, Gao ZG, Jacobson KA, Van Calenbergh S.

Bioorg Med Chem · research support, n.i.h., intramural; research-article; journal article · DOI 10.1016/j.bmc.2014.05.036

Bibliografisk träff 2013-09-08

Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.

Taliani S, Trincavelli ML, Cosimelli B, Laneri S, Severi E, Barresi E, Pugliesi I, Daniele S, Giacomelli C, Greco G, Novellino E, Martini C, Da Settimo F.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2013.09.001

Bibliografisk träff 2013-07-03

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.

Paoletta S, Tosh DK, Finley A, Gizewski ET, Moss SM, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem · research support, n.i.h., intramural; research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/jm4007966

Bibliografisk träff 2012-11-05

Fluorescent ligands for adenosine receptors.

Kozma E, Jayasekara PS, Squarcialupi L, Paoletta S, Moro S, Federico S, Spalluto G, Jacobson KA.

Bioorg Med Chem Lett · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; review; journal article · DOI 10.1016/j.bmcl.2012.10.112

Bibliografisk träff 2012-04-17

Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.

Baraldi PG, Preti D, Borea PA, Varani K.

J Med Chem · review; journal article · DOI 10.1021/jm300087j

Bibliografisk träff 2012-02-07

3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.

Taliani S, Pugliesi I, Barresi E, Simorini F, Salerno S, La Motta C, Marini AM, Cosimelli B, Cosconati S, Di Maro S, Marinelli L, Daniele S, Trincavelli ML, Greco G, Novellino E, Martini C, Da Settimo F.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm201177b

Bibliografisk träff 2009-10-12

Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.

Choi WJ, Lee HW, Kim HO, Chinn M, Gao ZG, Patel A, Jacobson KA, Moon HR, Jung YH, Jeong LS.

Bioorg Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.bmc.2009.10.011

Bibliografisk träff 2009-09-06

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Yuan J, Johnson RL, Huang R, Wichterman J, Jiang H, Hayton K, Fidock DA, Wellems TE, Inglese J, Austin CP, Su XZ.

Nat Chem Biol · research support, n.i.h., intramural; research-article; journal article; research support, n.i.h., extramural · DOI 10.1038/nchembio.215

Bibliografisk träff 2009-04-01

Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.

Kim Y, de Castro S, Gao ZG, Ijzerman AP, Jacobson KA.

J Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm801659w

Bibliografisk träff 2009-03-25

Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.

Pal S, Choi WJ, Choe SA, Heller CL, Gao ZG, Chinn M, Jacobson KA, Hou X, Lee SK, Kim HO, Jeong LS.

Bioorg Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.bmc.2009.03.034

Bibliografisk träff 2008-09-30

Topological descriptors in modeling the agonistic activity of human A3 adenosine receptor ligands: the derivatives of 2-chloro-N(6)-substituted-4'-thioadenosine-5'-uronamide.

Sharma S, Sharma BK, Sharma SK, Singh P, Prabhakar YS.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2008.09.022

Bibliografisk träff 2008-09-24

Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.

Jeong LS, Pal S, Choe SA, Choi WJ, Jacobson KA, Gao ZG, Klutz AM, Hou X, Kim HO, Lee HW, Lee SK, Tosh DK, Moon HR.

J Med Chem · research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm8008647

Bibliografisk träff 2008-08-07

Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.

Melman A, Wang B, Joshi BV, Gao ZG, Castro Sd, Heller CL, Kim SK, Jeong LS, Jacobson KA.

Bioorg Med Chem · research support, n.i.h., intramural; research-article; journal article · DOI 10.1016/j.bmc.2008.08.007

Bibliografisk träff 2008-04-04

Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.

Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.

Bioorg Med Chem Lett · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2008.04.001

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Publikationer i urvalet

Selective A<sub>3</sub> Adenosine Receptor Antagonist Radioligand for Human and Rodent Species.

Interaction of A<sub>3</sub> adenosine receptor ligands with the human multidrug transporter ABCG2.

Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A<sub>3</sub> Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary.

Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A<sub>3</sub> Adenosine Receptors: Affinity Enhancement by <i>N</i><sup>6</sup>-(2-Phenylethyl) Substitution.

Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A<sub>3</sub> Receptor Agonists.

Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.

[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A<sub>3</sub> adenosine receptor subtype.

Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A<sub>3</sub> adenosine receptor.

Polypharmacology of N<sup>6</sup>-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A<sub>3</sub> Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.

Exploring the Role of N<sup>6</sup>-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ∇.

N<sup>6</sup>-Substituted 5'-N-Methylcarbamoyl-4'-selenoadenosines as Potent and Selective A<sub>3</sub> Adenosine Receptor Agonists with Unusual Sugar Puckering and Nucleobase Orientation.

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT<sub>2B</sub>/5HT<sub>2C</sub> Serotonin Receptor Antagonists.

Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.

Tactical Approaches to Interconverting GPCR Agonists and Antagonists.

In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.

Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.

Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.

Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.

Fluorescent ligands for adenosine receptors.

Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.

3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.

Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.

Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.

Topological descriptors in modeling the agonistic activity of human A3 adenosine receptor ligands: the derivatives of 2-chloro-N(6)-substituted-4'-thioadenosine-5'-uronamide.

Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.

Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.

Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.