Chouhan S, Sridaran D, Weimholt C, Luo J, Li T, Myles C. Hodgson, Luana N. Santos, Samantha Le Sommer, Koomen J, Fang B, Qu C-K, Yart A, Kontaridis M, Mahajan K, and Mahajan NP*. SHP2 as a primordial enzyme expunges Histone H3 pTyr-54 to Amend Androgen Receptor Homeostasis. Nature Communications, 2024.
Sridaran D, and Mahajan NP*. Tracking ACK1/TNK2 kinase: Signaling, Diseases and Therapeutic Implications. 2024.
Nguyen D, Urvashi M, Angappulige D, Aashna Doshi, Mahajan NP, Mahajan K. Amino Terminal Acetylation of HOXB13 Regulates the DNA Damage Response in Prostate Cancer. Cancers, 2024.
Duminduni H. Angappulige, Nimrod B. Gozal, Nicholas Pickersgill, Cody Weimholt, Jingqin Luo, S Rayamajhi, Ghazal Shadmani, Ziad Tarcha, Gerald L. Andriole, Barry A. Siegel, Nupam Mahajan, Eric H. Kim and Kiran Mahajan. Prostate-Specific Membrane Antigen–Targeted Imaging and Its Correlation with HOXB13 Expression. Journal of Nuclear Medicine, 2024.
Angappulige DH, Mahajan NP and Mahajan K. Epigenetic Underpinnings of Tumor-Immune Dynamics in Prostate Cancer Immune Suppression. Trends in Cancer, 2024.
Barashi N, Li T,Angappulige D, Zhang B, O’Gorman H, Nottingham C, Shetty AS, Ippolito J, Andriole G, Mahajan NP, Mahajan K. Symptomatic Benign Prostatic Hyperplasia with Suppressed Epigenetic Regulator HOXB13 Shows a Lower Incidence of Prostate Cancer Development. Cancers, Jan. 2024.
Sridaran D, Bradshaw E, DeSelm C, Pachynski R, Mahajan K, and Mahajan NP*. Prostate Cancer Immunotherapy: Improving Clinical Outcomes with a Multi-Pronged Approach. Cell Reports Medicine, Sept. 2023.
Nguyen T, Sridaran D, Chouhan S, Weimholt C, Wilson A, Luo J, Li T, Koomen J, Fang B, Putluri N, Sreekumar A, Feng FY, Mahajan K, and Mahajan NP*. Histone H2A Lys130 acetylation epigenetically regulates androgen production in prostate cancer.Nature Communications, 14, Article number: 3357, 2023.
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Sawant M, Wilson A, Sridaran D, Mahajan K, O’Conor C, Hagemann I, Luo J, Weimholt C, Li T, Roa J, Wu X, Pandey A, and Mahajan NP*. Epigenetic Reprogramming of Cell Cycle Genes by ACK1 Promotes Breast Cancer Resistance to CDK4/6 Inhibitor.Oncogene, 17 June, 2023.
Sridaran D, Chouhan S, Mahajan K, Weimholt C, Bhagwat S, Reimers M, Kim EH, Thakur MK, Pachynski RK, Seeliger MA, Miller WT, Feng FY, and Mahajan NP*. Inhibiting ACK1-mediated phosphorylation of C-terminal Src kinase counteracts prostate cancer immune checkpoint blockade resistance.Nature Communications, 13, Article number: 6929, 2022.
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Sawant M, Mahajan K, Weimholt C, Luo J, Kukshal V, Jez JM, Jeon MS, Zhang B, Li T, Fang B, Lawrence NJ, Luo Y, Lawrence HR, Feng FY, and Mahajan NP*. Chronologically modified androgen receptor in recurrent castration resistant prostate cancer and its therapeutic targeting. Science Translational Medicine, 2022.
Chouhan S, Sawant M, Weimholt C, Luo J, Sprung RW, Terrado M, Mueller DM, Earp HS and Mahajan NP*. ACK1/TNK2 Mediated Phosphorylation of ATP Synthase α-Subunit Selectively Augments Survival of Prostate Cancer While Engendering Mitochondrial Vulnerability.Autophagy, 2022.
Ghildiyal R., Sawant M, Renganathan A, Kim E, Luo J, Mahajan K, Feng F and Mahajan NP*. Loss of long non-coding RNA NXTAR in prostate cancer augments androgen receptor expression and enzalutamide resistance. Cancer Research, 82(1):155-168, 2022.
Nguyen DT, Yang W, Renganathan A, Weimholt C, Angappulige D, Nguyen T, Sprung RW, Andriole GL, Kim EH, MahajanNP, Kiran Mahajan. Acetylated HOXB13 Regulated Super Enhancer Genes Define Therapeutic Vulnerabilities of Castration-Resistant Prostate Cancer.Clinical Cancer Research, 2022.
Sjöström M, Zhao SG, Levy S, Zhang M, Ning Y, Shrestha R, …. Nupam P Mahajan, Primo N Lara Christopher P Evans, Phuoc T Tran, Edwin M Posadas, Chuan He, Xiao-Long Cui, Jiaoti Huang, Wilbert Zwart, Luke A Gilbert, Christopher A Maher, Paul C Boutros, Kim N Chi, Alan Ashworth, Eric J Small, Housheng H He, Alexander W Wyatt, David A Quigley, Felix Y Feng. The 5-hydroxymethylcytosine landscape of prostate cancer.Cancer Research, 2022.
Tahir R, Madugundu A, Udainiya S, Cutler J, Renuse S, Wang L, Pearson N, Mitchell C, Mahajan NP, Pandey A, Wu X. Proximity-dependent biotinylation to elucidate the interactome of TNK2 non-receptor tyrosine kinase.Journal of Proteome Research, 20(9):4566-4577, 2021.
Zhao S, Chen W, Li H, Foye A, Zhang M, Sjöström M, Aggarwal R, Playdle D, Liao A, Alumkal J, Das R, Chi K, Gleave M, Zoubeidi A, Reiter R, Rettig M, Witte O, Kim MY, Fong L, Spratt D, Morgan T, Bose R, Huang F, Li H, Chesner L, Shenoy T, Goodarzi H, Asangani I, Sandhu S, Lang J, MahajanNP, Lara P, Evans CP, Tomlins S, Wyatt A, Dehm S, Ashworth A, Gilbert L, Boutros P, Farh K, Maher C, Small E*, Quigley D*, Chinnaiyan A*, Feng F*. DNA methylation landscapes in advanced prostate cancer.Nature Genetics, 52(8):778-789, 2020.
Gu J, Qian L, Zhang G, Mahajan NP, Owonikoko T, Ramalingam SR, Sun SY. Inhibition of ACK1 delays and overcomes acquired resistance of EGFR mutant NSCLC cells to the third generation EGFR inhibitor, osimertinib.Lung Cancer 150:26-35. 2020.
Kim EH, Cao D, Mahajan NP, Andriole GL and Mahajan K. ACK1-AR and AR-HOXB13 Signaling Axis: Epigenetic Regulation of Lethal Prostate Cancers. Nucleic Acids Research Cancer, 2(3):zcaa018, 2020.
Bossan A, Ottman R, Andl T, Hasan MF, Mahajan N, Coppola D and Chakrabarti R. Expression of FGD4 positively correlates with the aggressive phenotype of prostate cancer.BMC Cancer 18:1257, 2018.
Mahajan K, Malla P, Lawrence H, Chen Z, Sinha CK, Malik R, Shukla S, Kim J, Coppola D, Lawrence N andMahajan NP*.ACK1 regulates histone Tyr-phosphorylation and AR gene expression in castration resistant prostate cancer. Cancer Cell, 2017.
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New class of small molecule inhibitor for prostate cancer
Mahajan NP*, Malla P, Bhagwat S, Sarnaik A, Kim J, Pilon-Thomas S, Weber J and Mahajan K*. WEE1 epigenetically modulates 5-hmC levels by pY37-H2B dependent regulation of IDH2 gene expression. Oncotarget , 2017
Mahajan NP*, Coppola D, Kim J, Lawrence H, Lawrence NJ andMahajan K*. Blockade of ACK1/TNK2 to squelch the survival of prostate cancer stem-like cells.Scientific Reports, 2018.
Wu X, Zahari MS, Renuse S, Bharbuiya MA, Rojas PL, Kelkar DS, Sterns V, Gabrielson E, Sukumar S, Malla P,Mahajan NP*, Pandey A*. The non-receptor Tyrosine kinase TNK2/ACK1 is a novel therapeutic target in triple negative breast cancer. Oncotarget, 2017.
Mahajan K andMahajan NP*. Cross talk of Tyrosine Kinases with the DNA Damage Signaling Pathways.Nucleic Acids Research, 2015.
Paranjape A, Soundararajan R, Werden S, Joseph R, Taube J, Liu H, Rodriguez-Canales J, Sphyris N, Wistuba I, Dhillon J,Mahajan N, Mahajan K, Chang J, Ittmann M, Maity S, Logothetis C, Miura N, Tang D, Mani S. Inhibition of FOXC2 restores epithelial phenotype and drug-sensitivity in prostate cancer cells with stem-like properties.Oncogene2016. Pubmed ID:26804168
Lawrence HR, Mahajan K, Liu Y, Zhang D, Tindal N, Huseyin M, Gevariya H, Kazi S, Ozcan S,Mahajan NP* and Lawrence NJ*. Development of novel ACK1 inhibitors using a fragment based approach.J Med Chem, 2015.
Mahajan K andMahajan NP*. ACK1/TNK2 Tyrosine Kinase: Molecular Signaling and Evolving Role in Cancers.Oncogene, 2015.
Mahajan K, Lawrence H, Lawrence NJ andMahajan NP*. ACK1 Tyrosine Kinase Interacts with Histone Demethylase KDM3A to Regulate the Mammary Tumor Oncogene HOXA1.Journal of Biological Chemistry 2014
Mahajan K andMahajan NP*. AKT goes cycling.Cancer Control2014. Pubmed ID:24955708
Mahajan K andMahajan NP*. WEE1 tyrosine kinase, a novel epigenetic modifier.Trends in Genetics2013. Pubmed ID:23537585
Linderoth E, Pilia G,Mahajan NP, Ferby I. Activated Cdc42-associated Kinase 1 (Ack1) Is Required for Tumor Necrosis Factor-related Apoptosis-inducing Ligand (TRAIL) Receptor Recruitment to Lipid Rafts and Induction of Cell Death.Journal of Biological Chemistry2013. Pubmed ID:24085293
Mahajan K andMahajan NP*. ACK1 tyrosine kinase: targeted inhibition to block cancer cell proliferation.Cancer Letters2013. Pubmed ID:23597703
Buchwald M, Pietschmann K, Brand P, Gunther A,Mahajan NP, Heinzel T and Kramer OH. SIAH ubiquitin ligases target the nonreceptor tyrosine kinase ACK1 for ubiquitinylation and proteosomal degradation.Oncogene2013. Pubmed ID:23208506
Mahajan K, Coppola D, Rawal B, Chen YA, Lawrence H, Engelman RW, Lawrence NJ andMahajan NP*. Ack1 mediated androgen receptor phosphorylation modulates radiation resistance in castration resistant prostate cancer.Journal of Biological Chemistry2012. Pubmed ID:22566699
Mahajan K andMahajan NP*. PI3K-independent AKT activation: A Treasure Trove of Novel Therapeutics.Journal of Cellular Physiology2012. Pubmed ID:22307544
Mahajan K, Coppola D, Lawrence H, Luo Y, Zhu W, Chen AJ, Lawrence NJ,Mahajan NP*. Ack1 correlates with pancreatic cancer progression.American Journal of Pathology2012. Pubmed ID:22322295
Lin HY, Park HY, Radlein S,Mahajan NP, Sellers TS, Zachariah B, Pow-Sang J, Coppola D, Ganapathy V, Park JY. SLC5A8 gene variation and protein levels in prostate cancer risk and aggressiveness.Urology2011. Pubmed ID:20623637
Mahajan K, Challa S, Coppola D, Lawrence H, Luo Y, Zhu W, Chen A, Lawrence NJ andMahajan NP*. Effect of Ack1 Tyrosine Kinase Inhibitor on Ligand-Independent Androgen Receptor Activity.Prostate2010. Pubmed ID:20623637
Mahajan K andMahajan NP*. Shepherding Androgen receptor and AKT by Ack1 in hormonally regulated cancers.Journal of Cellular Physiology224:327-33, 2010. Pubmed ID:20333297
Mahajan NP, Liu Y, Majumder S, Warren MR, Parker CE, Mohler JL, Earp HS, Whang YE. Activated Cdc42-associated kinase Ack1 promotes prostate cancer progression via androgen receptor tyrosine phosphorylation.Proc Natl Acad Sci USA104:8438-8443, 2007. Pubmed ID:17494760
Mahajan NP, Whang YE, Mohler JL, Earp HS. Activated tyrosine kinase Ack1 promotes prostate tumorigenesis: role of Ack1 in polyubiquitination of tumor suppressor Wwox.Cancer Research65:10514-10523, 2005. Pubmed ID:16288044
Li Y,Mahajan NP, Webster-Cyriaque J, Bhende P, Hong GK, Earp HS, Kenney S. The C-mer gene is induced by Epstein-Barr virus immediate-early protein BRLF1.Journal of Virology78:11778-11785, 2004. Pubmed ID:15479819
Mahajan NP, Earp HS. An SH2 domain-dependent, phosphotyrosine-independent interaction between Vav1 and the Mer receptor tyrosine kinase: a mechanism for localizing guanine nucleotide-exchange factor action.J Biol Chem.278:42596-42603, 2003. Pubmed ID:12920122
Guttridge KL, Luft JC, Dawson TL, Kozlowska E,Mahajan NP, Varnum B, Earp HS. Mer receptor tyrosine kinase signaling: prevention of apoptosis and alteration of cytoskeletal architecture without stimulation or proliferation.J Biol Chem.277:24057-24066, 2002. Pubmed ID:11929866
Mahajan K, Gangi-Peterson L, Sorscher D, Wang J, Gathy K,Mahajan NP, Reeves W, Mitchell B. Association of terminal deoxynucleotidyl transferase with Ku.Proc Natl Acad Sci USA.96:13926-13931, 1999. Pubmed ID:10570175
Mahajan NP, Harrison-Shostak D, Michaux J, Herman B. Novel mutant green fluorescent protein protease substrates reveal the activation of specific caspases during apoptosis.Chemistry & Biology6:401-409, 1999. Pubmed ID:10375546
Mahajan NP, Linder K, Berry G, Gordon G, Heim R, Herman B. Bcl-2 and Bax interactions in mitochondria probed with green fluorescent protein and fluorescence resonance energy transfer.Nature Biotechnology16:547-552, 1998. Pubmed ID:9624685
Highlighted in the same issue of Nature Biotechnology
Mahajan NP, Rao C. Nucleotide sequence and expression in E. coli of the complete P4 type VP4 from a G2 serotype human rotavirus.Arch Virol.141:315-329, 1996. Pubmed ID:86340233
Zha H, Fisk H, Yaffe M,Mahajan N, Herman B, Reed J. Structure-function comparisons of proapoptotic protein Bax in yeast and mammalian cells. Mol Cell Biol. 16:6494-08, 1996, Pubmed ID:8887678
BOOK CHAPTERS
Mahajan K,Mahajan N. ACK1/TNK2 tyrosine kinase:An emerging target for cancer therapeuticsIn:AACR Yearbook, 2014
Herman, B, Wang, X, Wodnicki, P, Perisamy A,Mahajan N, Berry G and Gordon G. Fluorescence Lifetime Imaging Microscopy. Applied Fluorescence in Chemistry, Biology and MedicineIn:W. Rettig, B. Strehmel, S. Schrader and H. Seifert (Eds.), Springer Verlag Press, Berlin Heidelberg, 1998.
Herman B,Mahajan N, Casanova E, Michaux J and Gordon G. Two fusion FRET: A new means to observe structural and functional protein dynamics in living cells. 3rd conference on fluorescence microscopy and fluorescent probes, 2000.
Herman B, Gordon G,Mahajan Nand Centonze V. Measurement of fluorescence resonance energy transfer in the optical microscope. Methods in Cellular ImagingIn:Periasamy A (Ed.), Oxford University Press, New York, New York, 2001.
PATENTS
Title: Inhibitors of ACK1/TNK2 Tyrosine Kinase US Patent No. 9,850,216
10,017,478
10,336,734
Title: AKT Tyrosine 176 Phosphorylation as Cancer Biomarker US Patent No. 8,557,516
Title: NXTAR derived oligonucleotides and uses thereof US Patent Application No. 17/554,274
Title: Methods for Diagnosis and Prognosis of Epithelial Tumors US Patent Application No.15/525,787
Title: Methods for treatment of disorders related to phosphorylation of histones US Patent Application No. 14/860,405
Title: Phosphorylated histones and uses thereof U.S. Patent No. 9,594,084
Title: Allosteric inhibitor of WEE1 kinase US Patent Application No. 17/265,649
Title: ACK1 kinase inhibition to treat triple negative breast cancer US Patent Application No. 13/965,034