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(Satyakam Singh) Page | 1 Satyakam Singh 21 Cheyenne Ct. Coram, New York 11727 347.933.2829 [email protected] Publications 1. Shukla, Suneet; Chufán, Eduardo; Singh, Satyakam; Skoumbourdis, Amanda; Kapoor, Khyati; Boxer, Matthew; Duveau, Damien; Thomas, Craig; Talele, Tanaji; Ambudkar, Suresh. " Elucidation of the structural basis of interaction of the BCR-ABL kinase inhibitor, nilotinib (Tasigna®) with the human ABC drug transporter P-glycoprotein " Leukemia (www.nature.com)accepted on Jan 03, 2014. 2. Satyakam Singh, Nagarajan Rajendra Prasad, Khyati Kapoor, Eduardo E. Chufan, Bhargav A. Patel,Suresh V. Ambudkar, Tanaji T. Talele. "Design, synthesis and biological evaluation of ( S)-valine thiazole-derived cyclic and non-cyclic peptidomimetic oligomers as modulators of human P- glycoprotein (ABCB1)" ChemBioChem 2014 Jan 3;15(1):157-69 (PhD thesis work) 3. Eduardo E. Chufan, Khyati Kapoor, Hong-May Sim, Satyakam Singh, Tanaji T. Talele, Stewart R. Durell, and Suresh V. Ambudkar. "Multiple transport-active binding sites are available for a single substrate on human P-glycoprotein (ABCB1)" PLoS ONE 2013 Dec 5;8(12):e82463. 4. Singh, S.; Makwana, D. K.; Buckley, T.; Agrawal, A.; Koduru, S. V.; Tiwari, A. K. Clinical significance of PARP-1 inhibitors in cancer chemotherapy. Translational Clinical Biology 2013,1,10. 5. Tirtha K. Das, Dibyendu Dana, Suneeta S. Paroly, Senthil K. Perumal, Satyakam Singh, Hugo Jhun, Jay Pendse, Ross L. Cagan, Tanaji T. Talele, Sanjai Kumar. “Centrosomal Kinase Nek2 Cooperates With Oncogenic Pathways To Promote Metastasis” Oncogenesis (www.nature.com/oncsis) 2013, 2, e69. 6. He, D.; Zhao, X.; Chen, X.; Fang, Y.; Singh, S.; Talele, T. T.; Qiu, H.; Liang, Y.; Wang, X.; Zhang, G.; Chen, Z.; Fu, L. BIRB796, the Inhibitor of p38 Mitogen-Activated Protein Kinase, Enhances the Efficacy of Chemotherapeutic Agents in ABCB1 Overexpression Cells. PLoS ONE., 2013, 8, e54181. 7. Tiwari, A. K.; Sodani, K.; Dai, C. L.; Abuznait, A. H.; Singh, S.; Xiao, Z. J.; Patel, A.; Talele, T. T.; Fu, L.; Kaddoumi, A.; Gallo, J. M.; Chen, Z. S. Nilotinib potentiates anticancer drug sensitivity in murine ABCB1-, ABCG2-, and ABCC10-multidrug resistance xenograft models. Cancer Lett. 2013, 328,307-317. 8. Saurabh G Vispute, Jun-Jiang Chen, Yue-Li Sun, Kamlesh S Sodani, Satyakam Singh, Yihang Pan, Tanaji Talele, Charles R Ashby Jr, Zhe-Sheng Chen "Vemurafenib (PLX4032, Zelboraf®), a BRAF Inhibitor, Modulates ABCB1-, ABCG2-, and ABCC10-Mediated Multidrug Resistance". Journal of Cancer Research. 2013, 2(4), 307 9. Patel A, Tiwari AK, Sodani K, Singh S, Chen ZS. " PD173074, a selective FGFR inhibitor, reverses ABCB1-mediated drug resistance in cancer cells" Cancer Chemotherapy and Pharmacology, 2013, 72(1), 189-199. 10. Kulkarni, S. S*.; Singh, S*.; Talele, T. T. Synthesis and SAR optimization of quinazolin-4(3H)- ones as poly(ADP-ribose)polymerase-1 inhibitors. Eur. J. Med. Chem . 2012, 50, 264-273. (*Co-first author) 11. Patel, M. R.; Pandya, K. G.; Lau-Cam, C. A.; Singh, S.; Talele, T. T. Design and synthesis of N-substituted indazole-3-carboxamides as poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Chem. Biol. Drug Des . 2012, 79, 488-496.

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Page 1: Satyakam Singh 21 Cheyenne Ct. Coram, New York …d2oqb2vjj999su.cloudfront.net/.../SatyakamSingh_Publicatons.pdf(Satyakam Singh) Page | 1 Satyakam ... Publications 1. Shukla, Suneet;

(Satyakam Singh) Page | 1

Satyakam Singh

21 Cheyenne Ct. Coram, New York 11727 ▪ 347.933.2829 ▪ [email protected]

Publications

1. Shukla, Suneet; Chufán, Eduardo; Singh, Satyakam; Skoumbourdis, Amanda; Kapoor, Khyati;

Boxer, Matthew; Duveau, Damien; Thomas, Craig; Talele, Tanaji; Ambudkar, Suresh. " Elucidation of

the structural basis of interaction of the BCR-ABL kinase inhibitor, nilotinib (Tasigna®) with the

human ABC drug transporter P-glycoprotein " Leukemia (www.nature.com)accepted on Jan 03, 2014.

2. Satyakam Singh, Nagarajan Rajendra Prasad, Khyati Kapoor, Eduardo E. Chufan, Bhargav A.

Patel,Suresh V. Ambudkar, Tanaji T. Talele. "Design, synthesis and biological evaluation of (S)-valine

thiazole-derived cyclic and non-cyclic peptidomimetic oligomers as modulators of human P-

glycoprotein (ABCB1)" ChemBioChem 2014 Jan 3;15(1):157-69 (PhD thesis work)

3. Eduardo E. Chufan, Khyati Kapoor, Hong-May Sim, Satyakam Singh, Tanaji T. Talele, Stewart R.

Durell, and Suresh V. Ambudkar. "Multiple transport-active binding sites are available for a single

substrate on human P-glycoprotein (ABCB1)" PLoS ONE 2013 Dec 5;8(12):e82463.

4. Singh, S.; Makwana, D. K.; Buckley, T.; Agrawal, A.; Koduru, S. V.; Tiwari, A. K. Clinical

significance of PARP-1 inhibitors in cancer chemotherapy. Translational Clinical Biology 2013,1,10.

5. Tirtha K. Das, Dibyendu Dana, Suneeta S. Paroly, Senthil K. Perumal, Satyakam Singh, Hugo Jhun,

Jay Pendse, Ross L. Cagan, Tanaji T. Talele, Sanjai Kumar. “Centrosomal Kinase Nek2 Cooperates

With Oncogenic Pathways To Promote Metastasis” Oncogenesis (www.nature.com/oncsis)

2013, 2, e69.

6. He, D.; Zhao, X.; Chen, X.; Fang, Y.; Singh, S.; Talele, T. T.; Qiu, H.; Liang, Y.; Wang, X.; Zhang,

G.; Chen, Z.; Fu, L. BIRB796, the Inhibitor of p38 Mitogen-Activated Protein Kinase, Enhances the

Efficacy of Chemotherapeutic Agents in ABCB1 Overexpression Cells. PLoS ONE., 2013, 8, e54181.

7. Tiwari, A. K.; Sodani, K.; Dai, C. L.; Abuznait, A. H.; Singh, S.; Xiao, Z. J.; Patel, A.; Talele, T. T.;

Fu, L.; Kaddoumi, A.; Gallo, J. M.; Chen, Z. S. Nilotinib potentiates anticancer drug sensitivity in

murine ABCB1-, ABCG2-, and ABCC10-multidrug resistance xenograft models. Cancer

Lett. 2013, 328,307-317.

8. Saurabh G Vispute, Jun-Jiang Chen, Yue-Li Sun, Kamlesh S Sodani, Satyakam Singh, Yihang Pan,

Tanaji Talele, Charles R Ashby Jr, Zhe-Sheng Chen "Vemurafenib (PLX4032, Zelboraf®), a BRAF

Inhibitor, Modulates ABCB1-, ABCG2-, and ABCC10-Mediated Multidrug Resistance". Journal of

Cancer Research. 2013, 2(4), 307

9. Patel A, Tiwari AK, Sodani K, Singh S, Chen ZS. " PD173074, a selective FGFR inhibitor,

reverses ABCB1-mediated drug resistance in cancer cells" Cancer Chemotherapy and

Pharmacology, 2013, 72(1), 189-199.

10. Kulkarni, S. S*.; Singh, S*.; Talele, T. T. Synthesis and SAR optimization of quinazolin-4(3H)-

ones as poly(ADP-ribose)polymerase-1 inhibitors. Eur. J. Med. Chem. 2012, 50, 264-273. (*Co-first

author)

11. Patel, M. R.; Pandya, K. G.; Lau-Cam, C. A.; Singh, S.; Talele, T. T. Design and synthesis of

N-substituted indazole-3-carboxamides as poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.

Chem. Biol. Drug Des. 2012, 79, 488-496.

Page 2: Satyakam Singh 21 Cheyenne Ct. Coram, New York …d2oqb2vjj999su.cloudfront.net/.../SatyakamSingh_Publicatons.pdf(Satyakam Singh) Page | 1 Satyakam ... Publications 1. Shukla, Suneet;

(Satyakam Singh) Page | 2

12. Sun, Y. L.; Kathawala, R. J.; Singh, S.; Talele, T. T.; Chen, Z. S. Zafirlukast antagonizes ATP-

binding cassette subfamily G member 2-mediated multidrug resistance. Anticancer

Drugs 2012, 23, 865-873.

13. Sodani, K.; Tiwari, A. K.; Singh, S.; Talele, T. T.; Chen, Z. S. GW583340 and GW2974, human

EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance.

Biochem.Pharmacol. 2012, 83, 1613-1622.

14. Cheng, C.; Liu, Z. G.; Zhang, H.; Xie, J. D.; Chen, X. G.; Zhao, X. Q.; Wang, F.; Liang, Y. J.;

Chen, L. K.; Singh, S.; Talele, T. T.; Chen, Z. S.; Zhong, F. T.; Fu, L. W. Enhancing

Chemosensitivity in ABCB1- and ABCG2-Overexpressing Cells and Cancer Stem-like Cells by An

Aurora Kinase Inhibitor CCT129202. Mol. Pharm. 2012.

15. Liu, K. J.; He, J. H.; Su, X. D.; Sim, H. M.; Xie, J. D.; Chen, X. G.; Wang, F.; Liang, Y. J.; Singh,

S.; Talele, T. T.; Ambudkar, S. V.; Chen, Z. S.; Wu, H. Y.; Fu, L. W. Saracatinib (AZD0530) is a

potent modulator of ABCB1-mediated multidrug resistance in vitro and in vivo. Int. J. Cancer. 2012.

16. Zhao, X. Q, Xie, J. D, Chen, X. G, Sim, H. M, Zhang, X, Liang, Y. J, Singh, S, Talele, T. T,

Ambudkar, S. V, Chen, Z. S, Fu, L. W. Neratinib reverses ATP-binding cassette B1-mediated

chemotherapeutic drug resistance in vitro, in vivo, and ex vivo. Mol. Pharmacol. 2012, 82,47-58.

17. Bhatt, A.; Patel, P. D.; Patel, M. R.; Singh, S.; Lau-Cam, C. A.; Talele, T. T. CoMSIA study on

substituted aryl alkanoic acid analogs as GPR40 agonists. Chem. Biol. Drug Des. 2011, 77, 361-372.

18. Ding, P. R.; Tiwari, A. K.; Ohnuma, S.; Lee, J. W.; An, X.; Dai, C. L.; Lu, Q. S.; Singh, S.; Yang,

D. H.; Talele, T. T.; Ambudkar, S. V.; Chen, Z. S. The phosphodiesterase-5 inhibitor vardenafil is a

potent inhibitor of ABCB1/P-glycoprotein transporter. PLoS One 2011, 6, e19329.

19. Shi, Z.; Tiwari, A. K.; Shukla, S.; Robey, R. W.; Singh, S.; Kim, I. W.; Bates, S. E.; Peng, X.;

Abraham, I.; Ambudkar, S. V.; Talele, T. T.; Fu, L. W.; Chen, Z. S. Sildenafil reverses ABCB1- and

ABCG2-mediated chemotherapeutic drug resistance. Cancer Res. 2011, 71, 3029-3041.

20. Yan, Y. Y.; Zheng, L. S.; Zhang, X.; Chen, L. K.; Singh, S.; Wang, F.; Zhang, J. Y.; Liang, Y. J.;

Dai, C. L.; Gu, L. Q.; Zeng, M. S.; Talele, T. T.; Chen, Z. S.; Fu, L. W. Blockade of Her2/neu binding

to Hsp90 by emodin azide methyl anthraquinone derivative induces proteasomal degradation of

Her2/neu.

Mol. Pharm. 2011, 8, 1687-1697.

21. Hardej, D, Ashby, C. R, Jr; Khadtare, N. S, Kulkarni, S. S, Singh, S, Talele, T. T. The synthesis of

phenylalanine-derived C5-substituted rhodanines and their activity against selected methicillin-resistant

Staphylococcus aureus (MRSA) strains. Eur. J. Med. Chem. 2010, 45, 5827-5832.

22. Talele, T. T.; Arora, P.; Kulkarni, S. S.; Patel, M. R.; Singh, S.; Chudayeu, M.; Kaushik-Basu, N.

Structure-based virtual screening, synthesis and SAR of novel inhibitors of hepatitis C virus NS5B

polymerase. Bioorg. Med. Chem. 2010, 18, 4630-4638.

23. Singh, S.; Soni, L. K.; Gupta, M. K.; Prabhakar, Y. S.; Kaskhedikar, S. G. QSAR studies on

benzoylaminobenzoic acid derivatives as inhibitors of beta-ketoacyl-acyl carrier protein synthase III.

Eur. J. Med. Chem. 2008, 43, 1071-1080.

Page 3: Satyakam Singh 21 Cheyenne Ct. Coram, New York …d2oqb2vjj999su.cloudfront.net/.../SatyakamSingh_Publicatons.pdf(Satyakam Singh) Page | 1 Satyakam ... Publications 1. Shukla, Suneet;

(Satyakam Singh) Page | 3

Manuscript Submitted

1. Satyakam Singh, Rajendra Prasad Nagarajan, Bhargav A. Patel, Suresh V. Ambudkar, Tanaji T.

Talele. Design, synthesis and biological evaluation of thiazole analogues containing privilege

scaffolds as inhibitors of P-glycoprotein (Submitted to Journal of Medicinal Chemistry).(PhD thesis

work).

2. Kamlesh Sodani, Atish Patel, Satyakam Singh, Nagaraju Anreddy, Dong-Hua Yang, Priyank

Kumar, Tanaji T. Talele, Zhe-Sheng Chen, Telatinib reverses chemotherapeutic multidrug resistance

by inhibiting ABCG2 efflux transporter in vitro and in vivo (Submitted to Molecular Pharmaceutics).

Poster Presentations

1. Sodani K, Tiwari AK, Singh S, Patel A, Xiao Z, Chen J, Sun Y, Talele TT, and Chen ZS.

GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-

mediated drug resistance. 103rd American Association for Cancer Research, Chicago, IL, Mar 31-Apr

4, 2012.

2. Tiwari AK, Shi Z, Shukla S, Singh S, Talele TT, Ambudkar SV, Chen ZS. Sildenafil, reverses

ABCB1/Pgp and ABCG2/BCRP/MXR mediated multidrug resistance. 102nd American Association

for Cancer Research (AACR), Orlando, FL, USA April 1-5, 2011.

3. Tiwari AK, Shi Z, Shukla S, Singh S, Chen JJ, Patel A, Ambudkar SV, Chen ZS. A new function of

Sildenafil (Viagra ™) as a multidrug resistance modulator. 2011 NJPhast Scholarship awards,

Hanover Marriot, NJ, USA May 19, 2011.

4. Singh S, Patel PD, Patel MR, Kulkarni S, Talele TT. Structure-based CoMSIA studies on

roscovitine derivatives as inhibitors of cyclin-dependent kinases and casein kinase 1, 238th ACS

National Meeting, Washington, DC, United States, August 16-20, 2009 (2009), MEDI-279.

5. Patel PD, Singh S, Kocsis B, Kocsis E, Talele TT. Synthesis and SAR studies of substituted

pyrazole derivatives possessing antifungal action, 238th ACS National Meeting, Washington, DC,

United States, August 16-20, 2009 (2009), MEDI-439.

6. Singh, S, Soni, L. K, Gupta, M. K, Prabhakar, Y. S, Kaskhedikar, S. G. "QSAR studies on

benzoylaminobenzoic acid derivatives as inhibitors of beta-ketoacyl-acyl carrier protein synthase III."

58th IPC (Indian Pharmaceutical Congress), MUMBAI on 1-3 Dec 2006. *(Best poster presentation

award)

7. Atish Patel, Kamlesh Sodani, Amit K. Tiwari, Satyakam Singh, Nagaraju Anreddy, Tanaji T.

Talele, Ralph Stephani, Suresh V. Ambudkar, Zhe-Sheng Chen “PD173074, a selective FGFR

inhibitor, reverses ABCB1 mediated drug resistance in cancer cells” 104th American Association for

Cancer Research (AACR) 2013, Washington DC.

8. Atish Patel, Kamlesh Sodani, Amit K. Tiwari, Satyakam Singh, Nagaraju Anreddy, Tanaji T.

Talele, Ralph Stephani, Suresh V. Ambudkar, Zhe-Sheng Chen “PD173074, a selective FGFR

inhibitor, reverses ABCB1 mediated drug resistance in cancer cells” Gorden Research Conference:

Multi-Drug Efflux Systems, Ventura, CA.