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1

Neoceptors: reengineering GPCRs to recognize tailored ligands

Kenneth A. Jacobson, Zhan-Guo Gao, Bruce T. Liang

Journal:

Trends in Pharmacological Sciences

Year:

2007

Language:

english

File:

PDF, 1.31 MB

english, 2007

2

Synthesis and Biological Evaluation of a New Series of 1,2,4-Triazolo[1,5- a ]-1,3,5-triazines as Human A 2A Adenosine Receptor Antagonists with Improved Water Solubility

Federico, Stephanie, Paoletta, Silvia, Cheong, Siew Lee, Pastorin, Giorgia, Cacciari, Barbara, Stragliotto, Stefano, Klotz, Karl Norbert, Siegel, Jeffrey, Gao, Zhan-Guo, Jacobson, Kenneth A., Moro, St

Journal:

Journal of Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 1.18 MB

english, 2011

3

Anti-ischemic effects of multivalent dendrimeric A3 adenosine receptor agonists in cultured cardiomyocytes and in the isolated rat heart

Bella Chanyshev, Asher Shainberg, Ahuva Isak, Alexandra Litinsky, Yelena Chepurko, Dilip K. Tosh, Khai Phan, Zhan-Guo Gao, Edith Hochhauser, Kenneth A. Jacobson

Journal:

Pharmacological Research

Year:

2012

Language:

english

File:

PDF, 1000 KB

english, 2012

4

Effects of rapid thermal annealing on the optical properties of InAs/(In)GaAs quantum dots with different areal density

Li, Zhan-Guo, You, Ming-hui, Liu, Guo-Jun, Gao, Xin, Li, Lin, Wang, Yong, Li, Lian-He

Journal:

Optik - International Journal for Light and Electron Optics

Year:

2014

Language:

english

File:

PDF, 463 KB

english, 2014

5

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin

Gao, Zhan-Guo, Jacobson, Kenneth A.

Journal:

Biochemical Pharmacology

Year:

2016

Language:

english

File:

PDF, 1.57 MB

english, 2016

6

Structural Connection between Activation Microswitch and Allosteric Sodium Site in GPCR Signaling

White, Kate L., Eddy, Matthew T., Gao, Zhan-Guo, Han, Gye Won, Lian, Tiffany, Deary, Alexander, Patel, Nilkanth, Jacobson, Kenneth A., Katritch, Vsevolod, Stevens, Raymond C.

Journal:

Year:

2018

Language:

english

File:

PDF, 3.18 MB

english, 2018

7

Partial Agonists for A3 Adenosine Receptors

Zhan-Guo Gao, Kenneth A. Jacobson

Journal:

Year:

2004

File:

PDF, 7 KB

2004

8

Engineering of A3 adenosine and P2Y nucleotide receptors and their ligands

Kenneth A. Jacobson, Hak Sung Kim, Gnana Ravi, Soo-Kyung Kim, Kyeong Lee, Aishe Chen, Wangzhong Chen, Seong Gon Kim, Dov Barak, Bruce T. Liang, Zhan-Guo Gao

Journal:

Drug Development Research

Year:

2003

Language:

english

File:

PDF, 143 KB

english, 2003

9

Progress in the pursuit of therapeutic adenosine receptor antagonists

Stefano Moro, Zhan-Guo Gao, Kenneth A. Jacobson, Giampiero Spalluto

Journal:

Medicinal Research Reviews

Year:

2006

Language:

english

File:

PDF, 570 KB

english, 2006

10

Structure–activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists

Kwan-Young Jung, Soo-Kyung Kim, Zhan-Guo Gao, Ariel S Gross, Neli Melman, Kenneth A Jacobson, Yong-Chul Kim

Journal:

Bioorganic & Medicinal Chemistry

Year:

2004

Language:

english

File:

PDF, 381 KB

english, 2004

11

Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands

Susanna Tchilibon, Soo-Kyung Kim, Zhan-Guo Gao, Brian A Harris, Joshua B Blaustein, Ariel S Gross, Heng T Duong, Neli Melman, Kenneth A Jacobson

Journal:

Bioorganic & Medicinal Chemistry

Year:

2004

Language:

english

File:

PDF, 585 KB

english, 2004

12

Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position

Michihiro Ohno, Zhan-Guo Gao, Philippe Van Rompaey, Susanna Tchilibon, Soo-Kyung Kim, Brian A Harris, Ariel S Gross, Heng T Duong, Serge Van Calenbergh, Kenneth A Jacobson

Journal:

Bioorganic & Medicinal Chemistry

Year:

2004

Language:

english

File:

PDF, 455 KB

english, 2004

13

Nucleotide analogues containing 2-oxa-bicyclo[2.2.1]heptane and l-α-threofuranosyl ring systems: interactions with P2Y receptors

Michihiro Ohno, Stefano Costanzi, Hak Sung Kim, Veerle Kempeneers, Karen Vastmans, Piet Herdewijn, Savitri Maddileti, Zhan-Guo Gao, T. Kendall Harden, Kenneth A. Jacobson

Journal:

Bioorganic & Medicinal Chemistry

Year:

2004

Language:

english

File:

PDF, 554 KB

english, 2004

14

Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety

Philippe Van Rompaey, Kenneth A. Jacobson, Ariel S. Gross, Zhan-Guo Gao, Serge Van Calenbergh

Journal:

Bioorganic & Medicinal Chemistry

Year:

2005

Language:

english

File:

PDF, 234 KB

english, 2005

15

Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands

Liesbet Cosyn, Zhan-Guo Gao, Philippe Van Rompaey, Changrui Lu, Kenneth A. Jacobson, Serge Van Calenbergh

Journal:

Bioorganic & Medicinal Chemistry

Year:

2006

Language:

english

File:

PDF, 238 KB

english, 2006

16

Design and synthesis of 3′-ureidoadenosine-5′-uronamides: effects of the 3′-ureido group on binding to the A3 adenosine receptor

Lak Shin Jeong, Myong Jung Kim, Hea Ok Kim, Zhan-Guo Gao, Soo-Kyung Kim, Kenneth A. Jacobson, Moon Woo Chun

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2004

Language:

english

File:

PDF, 298 KB

english, 2004

17

Design, synthesis, and biological activity of N6-substituted-4′-thioadenosines at the human A3 adenosine receptor

Lak Shin Jeong, Hyuk Woo Lee, Hea Ok Kim, Ji Young Jung, Zhan-Guo Gao, Heng T. Duong, Srikar Rao, Kenneth A. Jacobson, Dae Hong Shin, Jeong A Lee, Prashantha Gunaga, Sang Kook Lee, Dong Zhe Jin, Moon

Journal:

Bioorganic & Medicinal Chemistry

Year:

2006

Language:

english

File:

PDF, 276 KB

english, 2006

18

Selective A3 adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system

Artem Melman, Ben Wang, Bhalchandra V. Joshi, Zhan-Guo Gao, Sonia de Castro, Cara L. Heller, Soo-Kyung Kim, Lak Shin Jeong, Kenneth A. Jacobson

Journal:

Bioorganic & Medicinal Chemistry

Year:

2008

Language:

english

File:

PDF, 629 KB

english, 2008

19

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

Shantanu Pal, Won Jun Choi, Seung Ah Choe, Cara L. Heller, Zhan-Guo Gao, Moshe Chinn, Kenneth A. Jacobson, Xiyan Hou, Sang Kook Lee, Hea Ok Kim, Lak Shin Jeong

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 274 KB

english, 2009

20

2-Dialkynyl derivatives of (N)-methanocarba nucleosides: ‘Clickable’ A3 adenosine receptor-selective agonists

Dilip K. Tosh, Moshe Chinn, Lena S. Yoo, Dong Wook Kang, Hans Luecke, Zhan-Guo Gao, Kenneth A. Jacobson

Journal:

Bioorganic & Medicinal Chemistry

Year:

2010

Language:

english

File:

PDF, 528 KB

english, 2010

21

Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand–receptor recognition process

Giorgia Pastorin, Stephanie Federico, Silvia Paoletta, Marta Corradino, Francesca Cateni, Barbara Cacciari, Karl-Norbert Klotz, Zhan-Guo Gao, Kenneth A. Jacobson, Giampiero Spalluto, Stefano Moro

Journal:

Bioorganic & Medicinal Chemistry

Year:

2010

Language:

english

File:

PDF, 1.20 MB

english, 2010

22

Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5′-ribofuran-uronamide moiety

Zhan-Guo Gao, Bhalchandra V. Joshi, Athena M. Klutz, Soo-Kyung Kim, Hyuk Woo Lee, Hea Ok Kim, Lak Shin Jeong, Kenneth A. Jacobson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 151 KB

english, 2006

23

Structure–activity relationships of 2-chloro-N6-substituted-4′-thioadenosine-5′-N,N-dialkyluronamides as human A3 adenosine receptor antagonists

Lak Shin Jeong, Hyuk Woo Lee, Hea Ok Kim, Dilip K. Tosh, Shantanu Pal, Won Jun Choi, Zhan-Guo Gao, Amit R. Patel, Wanda Williams, Kenneth A. Jacobson, Hee-Doo Kim

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 143 KB

english, 2008

24

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

Artem Melman, Zhan-Guo Gao, Deepmala Kumar, Tina C. Wan, Elizabeth Gizewski, John A. Auchampach, Kenneth A. Jacobson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 175 KB

english, 2008

25

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists

Bidhan A. Shinkre, T. Santhosh Kumar, Zhan-Guo Gao, Francesca Deflorian, Kenneth A. Jacobson, William C. Trenkle

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2010

Language:

english

File:

PDF, 645 KB

english, 2010

26

Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold

T. Santhosh Kumar, Shilpi Mishra, Francesca Deflorian, Lena S. Yoo, Khai Phan, Miklos Kecskés, Angela Szabo, Bidhan Shinkre, Zhan-Guo Gao, William Trenkle, Kenneth A. Jacobson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2011

Language:

english

File:

PDF, 687 KB

english, 2011

27

A Neoceptor Approach to Unraveling Microscopic Interactions between the Human A2A Adenosine Receptor and Its Agonists

Kenneth A. Jacobson, Michihiro Ohno, Heng T. Duong, Soo-Kyung Kim, Susanna Tchilibon, Michal Cˇesnek, Antonín Holý, Zhan-Guo Gao

Journal:

Chemistry & Biology

Year:

2005

Language:

english

File:

PDF, 322 KB

english, 2005

28

Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor

Soo-Kyung Kim, Zhan-Guo Gao, Lak Shin Jeong, Kenneth A. Jacobson

Journal:

Journal of Molecular Graphics and Modelling

Year:

2006

Language:

english

File:

PDF, 2.24 MB

english, 2006

29

Design, synthesis and binding affinity of 3′-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands

Moo Hong Lim, Hea Ok Kim, Hyung Ryong Moon, Seung Jin Lee, Moon Woo Chun, Zhan-Guo Gao, Neli Melman, Kenneth A Jacobson, Joong Hyup Kim, Lak Shin Jeong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 172 KB

english, 2003

30

Corrigendum to ‘Design, Synthesis and Binding Affinity of 3′-Fluoro Analogues of C1-IB-MECA as Adenosine A3 Receptor Ligands’[Bioorg. Med. Chem. Lett. 13 (2003) 817]†

Moo Hong Lim, Hea Ok Kim, Hyung Ryong Moon, Seung Jin Lee, Moon Woo Chun, Zhan-Guo Gao, Neli Melman, Kenneth A. Jacobson, Joong Hyup Kim, Lak Shin Jeong

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2003

Language:

english

File:

PDF, 72 KB

english, 2003

31

Flexible modulation of agonist efficacy at the human A3adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000

Zhan-Guo Gao, Kai Ye, Anikó Göblyös, Adriaan P IJzerman, Kenneth A Jacobson

Journal:

BMC Pharmacology

Year:

2008

Language:

english

File:

PDF, 1.71 MB

english, 2008

32

Enhanced A3adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates

Athena M Klutz, Zhan-Guo Gao, John Lloyd, Asher Shainberg, Kenneth A Jacobson

Journal:

Journal of Nanobiotechnology

Year:

2008

Language:

english

File:

PDF, 2.16 MB

english, 2008

33

Nucleoside conjugates of quantum dots for characterization of G protein-coupled receptors: strategies for immobilizing A2Aadenosine receptor agonists

Arijit Das, Gangadhar J Sanjayan, Miklós Kecskés, Lena Yoo, Zhan-Guo Gao, Kenneth A Jacobson

Journal:

Journal of Nanobiotechnology

Year:

2010

Language:

english

File:

PDF, 2.10 MB

english, 2010

34

Measurement of wurtzite ZnO/rutile TiO2heterojunction band offsets by x-ray photoelectron spectroscopy

Jun Wang, Xiang-Lin Liu, An-Li Yang, Gao-Lin Zheng, Shao-Yan Yang, Hong-Yuan Wei, Qin-Sheng Zhu, Zhan-Guo Wang

Journal:

Applied Physics A: Materials Science & Processing

Year:

2011

Language:

english

File:

PDF, 659 KB

english, 2011

35

Signaling of the human P2Y1receptor measured by a yeast growth assay with comparisons to assays of phospholipase C and calcium mobilization in 1321N1 human astrocytoma cells

Ronald T. Niebauer, Zhan-Guo Gao, Bo Li, Jürgen Wess, Kenneth A. Jacobson

Journal:

Purinergic Signalling

Year:

2005

Language:

english

File:

PDF, 262 KB

english, 2005

36

Application of the functionalized congener approach to dendrimer-based signaling agents acting through A2Aadenosine receptors

Yoonkyung Kim, Athena M. Klutz, Béatrice Hechler, Zhan-Guo Gao, Christian Gachet, Kenneth A. Jacobson

Journal:

Purinergic Signalling

Year:

2009

Language:

english

File:

PDF, 705 KB

english, 2009

37

Synthesis and pharmacological characterization of [125I]MRS1898, a high-affinity, selective radioligand for the rat A3adenosine receptor

Zhan-Guo Gao, Bao Teng, Haitao Wu, Bhalchandra V. Joshi, Gary L. Griffiths, Kenneth A. Jacobson

Journal:

Purinergic Signalling

Year:

2009

Language:

english

File:

PDF, 205 KB

english, 2009

38

Design and synthesis of N6-substituted-4′-thioadenosine-5′-uronamides as potent and selective human A3 adenosine receptor agonists

Won Jun Choi, Hyuk Woo Lee, Hea Ok Kim, Moshe Chinn, Zhan-Guo Gao, Amit Patel, Kenneth A. Jacobson, Hyung Ryong Moon, Young Hoon Jung, Lak Shin Jeong

Journal:

Bioorganic & Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 309 KB

english, 2009

39

The influence of pentavalent Nb substitution for Zr on electrical property of oxide-ion conductor Gd2Zr2O7

Xiao-Liang Xia, Shuai Gao, Zhan-Guo Liu, Jia-Hu Ouyang

Journal:

Electrochimica Acta

Year:

2010

Language:

english

File:

PDF, 566 KB

english, 2010

40

Adenosine receptors as therapeutic targets

Jacobson, Kenneth A., Gao, Zhan-Guo

Journal:

Nature Reviews Drug Discovery

Year:

2006

Language:

english

File:

PDF, 969 KB

english, 2006

41

Optimization of Adenosine 5′-Carboxamide Derivatives as Adenosine Receptor Agonists Using Structure-Based Ligand Design and Fragment Screening

Tosh, Dilip K., Phan, Khai, Gao, Zhan-Guo, Gakh, Andrei A., Xu, Fei, Deflorian, Francesca, Abagyan, Ruben, Stevens, Raymond C., Jacobson, Kenneth A., Katritch, Vsevolod

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 5.04 MB

english, 2012

42

Structure-Guided Design of A 3 Adenosine Receptor-Selective Nucleosides: Combination of 2-Arylethynyl and Bicyclo[3.1.0]hexane Substitutions

Tosh, Dilip K., Deflorian, Francesca, Phan, Khai, Gao, Zhan-Guo, Wan, Tina C., Gizewski, Elizabeth, Auchampach, John A., Jacobson, Kenneth A.

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 514 KB

english, 2012

43

Emerging adenosine receptor agonists – an update

Gao, Zhan-Guo, Jacobson, Kenneth A

Journal:

Expert Opinion on Emerging Drugs

Year:

2011

Language:

english

File:

PDF, 302 KB

english, 2011

44

Structure−Activity Relationships of 2-Chloro-N6-substituted-4‘-thioadenosine-5‘-uronamides as Highly Potent and Selective Agonists at the Human A3 Adenosine Receptor

Jeong, Lak Shin, Lee, Hyuk Woo, Jacobson, Kenneth A., Kim, Hea Ok, Shin, Dae Hong, Lee, Jeong A, Gao, Zhan-Guo, Lu, Changrui, Duong, Heng T., Gunaga, Prashantha

Journal:

Journal of Medicinal Chemistry

Year:

2006

Language:

english

File:

PDF, 259 KB

english, 2006

45

Emerging adenosine receptor agonists

Gao, Zhan-Guo, Jacobson, Kenneth A

Journal:

Expert Opinion on Emerging Drugs

Year:

2007

Language:

english

File:

PDF, 248 KB

english, 2007

46

Evaluation of Molecular Modeling of Agonist Binding in Light of the Crystallographic Structure of an Agonist-Bound A2A Adenosine Receptor

Deflorian, Francesca, Kumar, T. Santhosh, Phan, Khai, Gao, Zhan-Guo, Xu, Fei, Wu, Huixian, Katritch, Vsevolod, Stevens, Raymond C., Jacobson, Kenneth A.

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 4.32 MB

english, 2012

47

G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions

Kenneth A. Jacobson, Ramachandran Balasubramanian, Francesca Deflorian, Zhan-Guo Gao

Journal:

Purinergic Signalling

Year:

2012

Language:

english

File:

PDF, 529 KB

english, 2012

48

Competitive and allosteric binding of 2α-DHET and its optical isomers to rat cardiac muscarinic receptors

Zhan-guo Gao, Chuan-gui Liu

Journal:

European Journal of Pharmacology: Molecular Pharmacology

Year:

1995

Language:

english

File:

PDF, 450 KB

english, 1995

49

Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety

Zhan-Guo Gao, Lak Shin Jeong, Hyung Ryong Moon, Hea Ok Kim, Won Jun Choi, Dae Hong Shin, Eleonora Elhalem, Maria J. Comin, Neli Melman, Liaman Mamedova, Ariel S. Gross, Juan B. Rodriguez, Kenneth A. J

Journal:

Biochemical Pharmacology

Year:

2004

Language:

english

File:

PDF, 246 KB

english, 2004

50

Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors

Liaman K Mamedova, Bhalchandra V Joshi, Zhan-Guo Gao, Ivar von Kügelgen, Kenneth A Jacobson

Journal:

Biochemical Pharmacology

Year:

2004

Language:

english

File:

PDF, 177 KB

english, 2004