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Publications

Acharya, B., Saha, D., Armstrong, D., Lakkaniga, N.R. and Frett, B., 2022. FLT3 Inhibitors for Acute Myeloid Leukemia: Successes, Defeats, and Emerging Paradigms. RSC Medicinal Chemistry 2022.

Zhang, L., Moccia, M., Briggs, D.C., Bharate, J.B., Lakkaniga, N.R., Knowles, P., Yan, W., Tran, P., Kharbanda, A., Wang, X. and Leung, Y.K., 2022. Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose. Journal of Medicinal Chemistry, 65(2), pp.1536-1551.

Moccia, M., Yang, D., Lakkaniga, N. R., Frett, B., McConnell, N., Zhang, L., ... & Carlomagno, F. (2021). Targeted activity of the small molecule kinase inhibitor Pz-1 towards RET and TRK kinases. Scientific Reports, 11(1), 16103.

Zhang, L., Lakkaniga, N.R., Bharate, J.B., Mcconnell, N., Wang, X., Kharbanda, A., Leung, Y.K., Frett, B., Shah, N.P. and Li, H.Y., 2021. Discovery of imidazo [1, 2-a] pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor. European journal of medicinal chemistry, 225, p.113776.

Bowroju, S.K., Penthala, N.R., Lakkaniga, N.R., Balasubramaniam, M., Ayyadevara, S., Reis, R.J.S. and Crooks, P.A., 2021. Novel hydroxybenzylamine-deoxyvasicinone hybrids as anticholinesterase therapeutics for Alzheimer’s disease. Bioorganic & Medicinal Chemistry, 45, p.116311.

Saha, D., Ryan, K.R., Lakkaniga, N.R., Acharya, B., Garcia, N.G., Smith, E.L. and Frett, B., 2021. Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. Journal of Medicinal Chemistry, 64(16), pp.11747-11773.

Saha, D., Ryan, K.R., Lakkaniga, N.R., Smith, E.L. and Frett, B., 2021. Pyrazoloadenine inhibitors of the RET lung cancer oncoprotein discovered by a fragment optimization approach. ChemMedChem, 16(10), pp.1605-1608.

Lakkaniga, N. R., Zhang, L., Belachew, B.A., Naresh, G., Frett, B., Li, H.Y. Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for a reduced myelosuppression profile. European Journal of Medicinal Chemistry 2020, 203, 112589. https://doi.org/10.1016/j.ejmech.2020.112589 

Lakkaniga, N. R., Gunaganti, N., Zhang, L., Frett, B., & Li, H. Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation. European Journal of Medicinal Chemistry 2020, 206, 112691. https://doi.org/10.1016/j.ejmech.2020.112691

Lakkaniga, N. R.; Balasubramaniam, M.; Zhang, S.; Frett, B.; Li, H.-Y. Structural Characterization of the Aurora Kinase B “DFG-Flip” Using Metadynamics. The AAPS Journal 2020, 22 (14). https://doi.org/10.1208/s12248-019-0399-6 

Balasubramaniam, M.*, Lakkaniga, N.R.*, Dera, A.,Fayi, M.A., Abohashrh, M., Ahmad, I., Chandramoorthy, H.C., Rajagopalan, P. FCX-146, a potent allosteric inhibitor of Akt Kinase in cancer cells: Lead optimization of the second-generation arylidene indanone scaffold. Biotechnology and Applied Biochemistry . https://doi.org/10.1002/bab.1896 [Co-first author] 

Moccia, M., Frett, B., Zhang, L., Lakkaniga, N. R., Briggs, D., Chauhan, R., Brescia, A., Federico, G., Santoro, M., McDonald, N., Li, H., Carlomagno, F. Bioisosteric discovery of NPA101.3, a second generation RET/VEGFR2 inhibitor optimized for single-agent polypharmacology. Journal of medicinal chemistry, 63(9), pp. 4506-4516. https://doi.org/10.1021/acs.jmedchem.9b01336 

Naresh, G., Lakkaniga, N.R., Kharbanda, A., Yan, W., Frett, B. and Li, H.Y., 2019. Use of Imidazo [1, 2‐a] pyridine as a Carbonyl Surrogate in a Mannich‐Like, Catalyst Free, One‐Pot Reaction. European Journal of Organic Chemistry, 2019(4), pp.770-777. https://doi.org/10.1002/ejoc.201801430 

Saha, D., Kharbanda, A., Yan, W., Lakkaniga, N.R., Frett, B. and Li, H.Y., 2019. The Exploration of Chirality for Improved Druggability within the Human Kinome. Journal of medicinal chemistry,  63(2), pp. 441-469. https://doi.org/10.1021/acs.jmedchem.9b00640 

Gunaganti, N., Kharbanda, A., Lakkaniga, N. R., Zhang, L., Cooper, R., Li, H. Y., & Frett, B. (2018). Catalyst free, C-3 functionalization of imidazo [1, 2-a] pyridines to rapidly access new chemical space for drug discovery efforts. Chemical communications, 54(92), 12954-12957. https://doi.org/10.1039/c8cc07063f 

Yan, W., Lakkaniga, N.R., Carlomagno, F., Santoro, M., McDonald, N.Q., Lv, F., Gunaganti, N., Frett, B. and Li, H.Y., 2018. Insights into current tropomyosin receptor kinase (TRK) inhibitors: development and clinical application. Journal of medicinal chemistry, 62(4), pp.1731-1760. https://doi.org/10.1021/acs.jmedchem.8b01092 

Bharate, J. B., McConnell, N., Naresh, G., Zhang, L., Lakkaniga, N. R., Ding, L., ... & Li, H. Y.(2018). Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4, 6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. Scientific reports, 8(1), 3722. https://doi.org/10.1038/s41598-018-21839-3 

Krishna, H., Agarwal, A., Chamola, V., Lakkaniga, N.R., Hassija, V., Sikdar, B, "A Review on the Role of Machine Learning in Enabling IoT Based Healthcare Applications", IEEE Access, vol. 9, pp. 38859 - 38890, 2021. https://doi.org/10.1109/ACCESS.2021.3059858

 

Saha, D., Ryan, K., Lakkaniga, N.R., Frett., B. (2021) Pyrazoloadenines as Inhibitors for the RET Lung Cancer Oncoprotein Discovered via a Phenotypic Fragment-Based Approach. ChemMedChem, 16(10), 1605-1608. https://doi.org/10.1002/cmdc.202100013 

 

Rohmetra, H., Raghunath, N., Narang, P., Chamola, V., Lakkaniga, N.R.*, AI-enabled remote monitoring of vital signs for COVID-19: Methods, Prospects and Challenges. Computing [Corresponding author]. https://doi.org/10.1007/s00607-021-00937-7 

Manuscripts in Review

Kelm, J., Lakkaniga, N.R., Serafimovski, S., Gavande, N. Ras Mutations: Seemingly Undruggable Only Until Drugged. Angawandte Chemie (IF: 13.00)

Lakkaniga, N. R., Wang, Z., Kharbanda, A., Li., H.Y. Revisiting Aurora Kinase B: a promising therapeutic target for cancer therapy. Journal of medicinal chemistry (IF: 6.2)

Conferences

Lakkaniga, N.R. Discovery of the first non-ATP-competitive Aurora B inhibitor with improved selectivity. Arkansas Academy of Sciences,  April 2021, Fort Smith, USA.

Lakkaniga, N.R., Balasubramaniam, M., Frett, B., Li, H.Y. Insights into the DFG-flip and mechanism of activation of Aurora Kinase B by metadynamics. Drug Discovery and Development Colloquium, June 2019, Little Rock, Arkansas. [First prize for outstanding presentation]


Lakkaniga, N.R., Balasubramaniam, M., Frett, B., Li, H.Y. Insights into the DFG-flip and mechanism of activation of Aurora Kinase B by metadynamics. American Chemical Society (ACS) Southwest Regional Meeting (SWRM), November 2018, Little Rock, Arkansas.

Lakkaniga, N.R., Frett, B., Li, H.Y., Ma, M-L., Hu, W. Structure based drug discovery of imidazo[1,2α]pyridine derivatives as Nek2 inhibitors. Discovery and Development Colloquium, June 2017, Little Rock, Arkansas.


Kharbanda, A., Gunaganti, N., Lakkaniga, N. R., Zhang, L., Cooper, R., Li, H. Y., & Frett,B. Catalyst-free, c-3 functionalization of imidazo[1,2-a] pyridines to explore new chemical Scope. Drug Discovery and Development Colloquium, June 2019, Little Rock, Arkansas.

Zhang, L., Bharate, J. B., McConnell, N., Naresh, G., Lakkaniga, N. R., Ding, L., Frett, B., Neil, S., & Li, H. Y. Discovery Of Pyrimidine-4,6-Diamine Derivatives As Type-II Inhibitors Of FLT3 Selective Against c-KIT.American Chemical Society (ACS) Southwest Regional Meeting (SWRM), November 2018, Little Rock, Arkansas.

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