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Revealing an Internal Stabilization Deficiency in the DNA Polymerase β K289M Cancer Variant through the Combined Use of Chemical Biology and X-ray Crystallography.

Batra VK, Alnajjar KS, Sweasy JB, McKenna CE, Goodman MF, Wilson SH.

Biochemistry. 2020 Feb 12. doi: 10.1021/acs.biochem.9b01072. [Epub ahead of print]


A pre-catalytic non-covalent step governs DNA polymerase β fidelity.

Alnajjar KS, Krylov IS, Negahbani A, Haratipour P, Kashemirov BA, Huang J, Mahmoud M, McKenna CE, Goodman MF, Sweasy JB.

Nucleic Acids Res. 2019 Dec 16;47(22):11839-11849. doi: 10.1093/nar/gkz1076.


Synthesis of ortho-Formylphenylphosphonic Acids as Covalent Probes of Active Site Lysines.

Duro MVV, Alnajjar KS, Sweasy JB, Kashemirov BA, McKenna CE.

Phosphorus Sulfur Silicon Relat Elem. 2019;194(4-6):313-314. doi: 10.1080/10426507.2018.1539996. Epub 2019 Feb 13.


Rescue bisphosphonate treatment of alveolar bone improves extraction socket healing and reduces osteonecrosis in zoledronate-treated mice.

Hokugo A, Kanayama K, Sun S, Morinaga K, Sun Y, Wu Q, Sasaki H, Okawa H, Evans C, Ebetino FH, Lundy MW, Sadrerafi K, McKenna CE, Nishimura I.

Bone. 2019 Jun;123:115-128. doi: 10.1016/j.bone.2019.03.027. Epub 2019 Mar 26.


A Transition-State Perspective on Y-Family DNA Polymerase η Fidelity in Comparison with X-Family DNA Polymerases λ and β.

Oertell K, Florián J, Haratipour P, Crans DC, Kashemirov BA, Wilson SH, McKenna CE, Goodman MF.

Biochemistry. 2019 Apr 2;58(13):1764-1773. doi: 10.1021/acs.biochem.9b00087. Epub 2019 Mar 14.


Diketopyrrolopyrrole Bis-Phosphonate Conjugate: A New Fluorescent Probe for In Vitro Bone Imaging.

Chiminazzo A, Borsato G, Favero A, Fabbro C, McKenna CE, Dalle Carbonare LG, Valenti MT, Fabris F, Scarso A.

Chemistry. 2019 Mar 7;25(14):3617-3626. doi: 10.1002/chem.201805436. Epub 2019 Feb 12.


Probing DNA Base-Dependent Leaving Group Kinetic Effects on the DNA Polymerase Transition State.

Oertell K, Kashemirov BA, Negahbani A, Minard C, Haratipour P, Alnajjar KS, Sweasy JB, Batra VK, Beard WA, Wilson SH, McKenna CE, Goodman MF.

Biochemistry. 2018 Jul 3;57(26):3925-3933. doi: 10.1021/acs.biochem.8b00417. Epub 2018 Jun 19.


Mapping Functional Substrate-Enzyme Interactions in the pol β Active Site through Chemical Biology: Structural Responses to Acidity Modification of Incoming dNTPs.

Batra VK, Oertell K, Beard WA, Kashemirov BA, McKenna CE, Goodman MF, Wilson SH.

Biochemistry. 2018 Jul 3;57(26):3934-3944. doi: 10.1021/acs.biochem.8b00418. Epub 2018 Jun 21.


USC-087 protects Syrian hamsters against lethal challenge with human species C adenoviruses.

Toth K, Spencer JF, Ying B, Tollefson AE, Hartline CB, Richard ET, Fan J, Lyu J, Kashemirov BA, Harteg C, Reyna D, Lipka E, Prichard MN, McKenna CE, Wold WSM.

Antiviral Res. 2018 May;153:1-9. doi: 10.1016/j.antiviral.2018.03.001. Epub 2018 Mar 3.


Bisphosphonate-Linked TrkB Agonist: Cochlea-Targeted Delivery of a Neurotrophic Agent as a Strategy for the Treatment of Hearing Loss.

Kempfle JS, Nguyen K, Hamadani C, Koen N, Edge AS, Kashemirov BA, Jung DH, McKenna CE.

Bioconjug Chem. 2018 Apr 18;29(4):1240-1250. doi: 10.1021/acs.bioconjchem.8b00022. Epub 2018 Feb 27.


Removal of matrix-bound zoledronate prevents post-extraction osteonecrosis of the jaw by rescuing osteoclast function.

Elsayed R, Abraham P, Awad ME, Kurago Z, Baladhandayutham B, Whitford GM, Pashley DH, McKenna CE, Elsalanty ME.

Bone. 2018 May;110:141-149. doi: 10.1016/j.bone.2018.01.030. Epub 2018 Feb 9.


DNA Polymerase β Cancer-Associated Variant I260M Exhibits Nonspecific Selectivity toward the β-γ Bridging Group of the Incoming dNTP.

Alnajjar KS, Negahbani A, Nakhjiri M, Krylov IS, Kashemirov BA, McKenna CE, Goodman MF, Sweasy JB.

Biochemistry. 2017 Oct 10;56(40):5449-5456. doi: 10.1021/acs.biochem.7b00713. Epub 2017 Sep 20.


Remarkably Stereospecific Utilization of ATP α,β-Halomethylene Analogues by Protein Kinases.

Ni F, Kung A, Duan Y, Shah V, Amador CD, Guo M, Fan X, Chen L, Chen Y, McKenna CE, Zhang C.

J Am Chem Soc. 2017 Jun 14;139(23):7701-7704. doi: 10.1021/jacs.7b03266. Epub 2017 Jun 2.


Selective BET bromodomain inhibition as an antifungal therapeutic strategy.

Mietton F, Ferri E, Champleboux M, Zala N, Maubon D, Zhou Y, Harbut M, Spittler D, Garnaud C, Courçon M, Chauvel M, d'Enfert C, Kashemirov BA, Hull M, Cornet M, McKenna CE, Govin J, Petosa C.

Nat Commun. 2017 May 18;8:15482. doi: 10.1038/ncomms15482.


Design, Synthesis, and Antimicrobial Evaluation of a Novel Bone-Targeting Bisphosphonate-Ciprofloxacin Conjugate for the Treatment of Osteomyelitis Biofilms.

Sedghizadeh PP, Sun S, Junka AF, Richard E, Sadrerafi K, Mahabady S, Bakhshalian N, Tjokro N, Bartoszewicz M, Oleksy M, Szymczyk P, Lundy MW, Neighbors JD, Russell RG, McKenna CE, Ebetino FH.

J Med Chem. 2017 Mar 23;60(6):2326-2343. doi: 10.1021/acs.jmedchem.6b01615. Epub 2017 Feb 13.


Teriparatide attenuates scarring around murine cranial bone allograft via modulation of angiogenesis.

Cohn Yakubovich D, Eliav U, Yalon E, Schary Y, Sheyn D, Cook-Wiens G, Sun S, McKenna CE, Lev S, Binshtok AM, Pelled G, Navon G, Gazit D, Gazit Z.

Bone. 2017 Apr;97:192-200. doi: 10.1016/j.bone.2017.01.020. Epub 2017 Jan 21.


Recent advances in therapeutics and drug delivery for the treatment of inner ear diseases: a patent review (2011-2015).

Nguyen K, Kempfle JS, Jung DH, McKenna CE.

Expert Opin Ther Pat. 2017 Feb;27(2):191-202. doi: 10.1080/13543776.2017.1252751. Epub 2016 Nov 18. Review.


Response to "Drug Diffusion to the Apex of the Human Cochlea?".

Jung DH, Kang WS, McKenna MJ, Sewell WF, Nguyen K, McKenna CE.

Otol Neurotol. 2016 Oct;37(9):1463-4. doi: 10.1097/MAO.0000000000001159. No abstract available.


Measurement of Ototoxicity Following Intracochlear Bisphosphonate Delivery.

Kang WS, Nguyen K, McKenna CE, Sewell WF, McKenna MJ, Jung DH.

Otol Neurotol. 2016 Jul;37(6):621-6. doi: 10.1097/MAO.0000000000001042.


Functional interplay between NTP leaving group and base pair recognition during RNA polymerase II nucleotide incorporation revealed by methylene substitution.

Hwang CS, Xu L, Wang W, Ulrich S, Zhang L, Chong J, Shin JH, Huang X, Kool ET, McKenna CE, Wang D.

Nucleic Acids Res. 2016 May 5;44(8):3820-8. doi: 10.1093/nar/gkw220. Epub 2016 Apr 7.


Intracochlear Drug Delivery Through the Oval Window in Fresh Cadaveric Human Temporal Bones.

Kang WS, Nguyen K, McKenna CE, Sewell WF, McKenna MJ, Jung DH.

Otol Neurotol. 2016 Mar;37(3):218-22. doi: 10.1097/MAO.0000000000000964.


Bromodomains: Structure, function and pharmacology of inhibition.

Ferri E, Petosa C, McKenna CE.

Biochem Pharmacol. 2016 Apr 15;106:1-18. doi: 10.1016/j.bcp.2015.12.005. Epub 2015 Dec 18. Review.


Erratum: Bisphosphonate-induced differential modulation of immune cell function in gingiva and bone marrow in vivo: Role in osteoclast-mediated NK cell activation.

Tseng HC, Kanayama K, Kaur K, Park SH, Park S, Kozlowska A, Sun S, McKenna CE, Nishimura I, Jewett A.

Oncotarget. 2015 Dec 1;6(38):41398. doi: 10.18632/oncotarget.6431. No abstract available.


Fluorescent Bisphosphonate and Carboxyphosphonate Probes: A Versatile Imaging Toolkit for Applications in Bone Biology and Biomedicine.

Sun S, Błażewska KM, Kadina AP, Kashemirov BA, Duan X, Triffitt JT, Dunford JE, Russell RG, Ebetino FH, Roelofs AJ, Coxon FP, Lundy MW, McKenna CE.

Bioconjug Chem. 2016 Feb 17;27(2):329-40. doi: 10.1021/acs.bioconjchem.5b00369. Epub 2015 Dec 8.


Bisphosphonate-induced differential modulation of immune cell function in gingiva and bone marrow in vivo: role in osteoclast-mediated NK cell activation.

Tseng HC, Kanayama K, Kaur K, Park SH, Park S, Kozlowska A, Sun S, McKenna CE, Nishimura I, Jewett A.

Oncotarget. 2015 Aug 21;6(24):20002-25. Erratum in: Oncotarget. 2015 Dec 1;6(38):41398.


Non-Ototoxic Local Delivery of Bisphosphonate to the Mammalian Cochlea.

Kang WS, Sun S, Nguyen K, Kashemirov B, McKenna CE, Hacking SA, Quesnel AM, Sewell WF, McKenna MJ, Jung DH.

Otol Neurotol. 2015 Jul;36(6):953-60. doi: 10.1097/MAO.0000000000000786.


Two Scaffolds from Two Flips: (α,β)/(β,γ) CH2/NH "Met-Im" Analogues of dTTP.

Kadina AP, Kashemirov BA, Oertell K, Batra VK, Wilson SH, Goodman MF, McKenna CE.

Org Lett. 2015 Jun 5;17(11):2586-9. doi: 10.1021/acs.orglett.5b00799. Epub 2015 May 13.


5'-β,γ-CHF-ATP diastereomers: synthesis and fluorine-mediated selective binding by c-Src protein kinase.

Hwang CS, Kung A, Kashemirov BA, Zhang C, McKenna CE.

Org Lett. 2015 Apr 3;17(7):1624-7. doi: 10.1021/ol503765n. Epub 2015 Mar 17.


Endocytotic uptake of zoledronic acid by tubular cells may explain its renal effects in cancer patients receiving high doses of the compound.

Verhulst A, Sun S, McKenna CE, D'Haese PC.

PLoS One. 2015 Mar 10;10(3):e0121861. doi: 10.1371/journal.pone.0121861. eCollection 2015.


Real-time intravital imaging establishes tumor-associated macrophages as the extraskeletal target of bisphosphonate action in cancer.

Junankar S, Shay G, Jurczyluk J, Ali N, Down J, Pocock N, Parker A, Nguyen A, Sun S, Kashemirov B, McKenna CE, Croucher PI, Swarbrick A, Weilbaecher K, Phan TG, Rogers MJ.

Cancer Discov. 2015 Jan;5(1):35-42. doi: 10.1158/2159-8290.CD-14-0621. Epub 2014 Oct 13.


Bisphosphonate uptake in areas of tooth extraction or periapical disease.

Cheong S, Sun S, Kang B, Bezouglaia O, Elashoff D, McKenna CE, Aghaloo TL, Tetradis S.

J Oral Maxillofac Surg. 2014 Dec;72(12):2461-8. doi: 10.1016/j.joms.2014.07.004. Epub 2014 Jul 12.


Small molecule inhibition of SAMHD1 dNTPase by tetramer destabilization.

Seamon KJ, Hansen EC, Kadina AP, Kashemirov BA, McKenna CE, Bumpus NN, Stivers JT.

J Am Chem Soc. 2014 Jul 16;136(28):9822-5. doi: 10.1021/ja5035717. Epub 2014 Jul 8.


Development of oral osteomucosal tissue constructs in vitro and localization of fluorescently-labeled bisphosphonates to hard and soft tissue.

Bae S, Sun S, Aghaloo T, Oh JE, McKenna CE, Kang MK, Shin KH, Tetradis S, Park NH, Kim RH.

Int J Mol Med. 2014 Aug;34(2):559-63. doi: 10.3892/ijmm.2014.1802. Epub 2014 Jun 11.


On the observation of discrete fluorine NMR spectra for uridine 5'-β,γ-fluoromethylenetriphosphate diastereomers at basic pH.

Hwang CS, Kashemirov BA, McKenna CE.

J Org Chem. 2014 Jun 6;79(11):5315-9. doi: 10.1021/jo500452b. Epub 2014 May 12.


Transition state in DNA polymerase β catalysis: rate-limiting chemistry altered by base-pair configuration.

Oertell K, Chamberlain BT, Wu Y, Ferri E, Kashemirov BA, Beard WA, Wilson SH, McKenna CE, Goodman MF.

Biochemistry. 2014 Mar 25;53(11):1842-8. doi: 10.1021/bi500101z. Epub 2014 Mar 12.


Jaw bone marrow-derived osteoclast precursors internalize more bisphosphonate than long-bone marrow precursors.

Vermeer JA, Jansen ID, Marthi M, Coxon FP, McKenna CE, Sun S, de Vries TJ, Everts V.

Bone. 2013 Nov;57(1):242-51. doi: 10.1016/j.bone.2013.08.007. Epub 2013 Aug 17.


Reduction of fluorinated cyclopropene by nitrogenase.

Ni F, Lee CC, Hwang CS, Hu Y, Ribbe MW, McKenna CE.

J Am Chem Soc. 2013 Jul 17;135(28):10346-52. doi: 10.1021/ja3121058. Epub 2013 Jul 8.


Identification of a novel BET bromodomain inhibitor-sensitive, gene regulatory circuit that controls Rituximab response and tumour growth in aggressive lymphoid cancers.

Emadali A, Rousseaux S, Bruder-Costa J, Rome C, Duley S, Hamaidia S, Betton P, Debernardi A, Leroux D, Bernay B, Kieffer-Jaquinod S, Combes F, Ferri E, McKenna CE, Petosa C, Bruley C, Garin J, Ferro M, Gressin R, Callanan MB, Khochbin S.

EMBO Mol Med. 2013 Aug;5(8):1180-95. doi: 10.1002/emmm.201202034. Epub 2013 Jul 4.


Evolution of an amino acid based prodrug approach: stay tuned.

Krylov IS, Kashemirov BA, Hilfinger JM, McKenna CE.

Mol Pharm. 2013 Feb 4;10(2):445-58. doi: 10.1021/mp300663j. Epub 2013 Jan 22.


Equilibrium-dependent bisphosphonate interaction with crystalline bone mineral explains anti-resorptive pharmacokinetics and prevalence of osteonecrosis of the jaw in rats.

Hokugo A, Sun S, Park S, McKenna CE, Nishimura I.

Bone. 2013 Mar;53(1):59-68. doi: 10.1016/j.bone.2012.11.030. Epub 2012 Dec 4.


Rab-geranylgeranyl transferase regulates glucose-stimulated insulin secretion from pancreatic β cells.

Arora DK, Syed I, Machhadieh B, McKenna CE, Kowluru A.

Islets. 2012 Sep-Oct;4(5):354-8. doi: 10.4161/isl.22538. Epub 2012 Sep 1.


Effect of β,γ-CHF- and β,γ-CHCl-dGTP halogen atom stereochemistry on the transition state of DNA polymerase β.

Oertell K, Wu Y, Zakharova VM, Kashemirov BA, Shock DD, Beard WA, Wilson SH, McKenna CE, Goodman MF.

Biochemistry. 2012 Oct 30;51(43):8491-501. doi: 10.1021/bi3010335. Epub 2012 Oct 19.


Host modulators of H1N1 cytopathogenicity.

Ward SE, Kim HS, Komurov K, Mendiratta S, Tsai PL, Schmolke M, Satterly N, Manicassamy B, Forst CV, Roth MG, García-Sastre A, Blazewska KM, McKenna CE, Fontoura BM, White MA.

PLoS One. 2012;7(8):e39284. doi: 10.1371/journal.pone.0039284. Epub 2012 Aug 2.


β,γ-CHF- and β,γ-CHCl-dGTP diastereomers: synthesis, discrete 31P NMR signatures, and absolute configurations of new stereochemical probes for DNA polymerases.

Wu Y, Zakharova VM, Kashemirov BA, Goodman MF, Batra VK, Wilson SH, McKenna CE.

J Am Chem Soc. 2012 May 30;134(21):8734-7. doi: 10.1021/ja300218x. Epub 2012 May 18.


Stereospecific formation of a ternary complex of (S)-α,β-fluoromethylene-dATP with DNA pol β.

Chamberlain BT, Batra VK, Beard WA, Kadina AP, Shock DD, Kashemirov BA, McKenna CE, Goodman MF, Wilson SH.

Chembiochem. 2012 Mar 5;13(4):528-30. doi: 10.1002/cbic.201100738. Epub 2012 Feb 7.


Bisphosphonate binding affinity affects drug distribution in both intracortical and trabecular bone of rabbits.

Turek J, Ebetino FH, Lundy MW, Sun S, Kashemirov BA, McKenna CE, Gallant MA, Plotkin LI, Bellido T, Duan X, Triffitt JT, Russell RG, Burr DB, Allen MR.

Calcif Tissue Int. 2012 Mar;90(3):202-10. doi: 10.1007/s00223-012-9570-0. Epub 2012 Jan 17.


Influence of bone affinity on the skeletal distribution of fluorescently labeled bisphosphonates in vivo.

Roelofs AJ, Stewart CA, Sun S, Błażewska KM, Kashemirov BA, McKenna CE, Russell RG, Rogers MJ, Lundy MW, Ebetino FH, Coxon FP.

J Bone Miner Res. 2012 Apr;27(4):835-47. doi: 10.1002/jbmr.1543.


Binary complex crystal structure of DNA polymerase β reveals multiple conformations of the templating 8-oxoguanine lesion.

Batra VK, Shock DD, Beard WA, McKenna CE, Wilson SH.

Proc Natl Acad Sci U S A. 2012 Jan 3;109(1):113-8. doi: 10.1073/pnas.1112235108. Epub 2011 Dec 16.


Structure of cyclic nucleoside phosphonate ester prodrugs: an inquiry.

Krylov IS, Zakharova VM, Serpi M, Haiges R, Kashemirov BA, McKenna CE.

J Org Chem. 2012 Jan 6;77(1):684-9. doi: 10.1021/jo201735f. Epub 2011 Nov 30.


Synthesis and characterization of novel fluorescent nitrogen-containing bisphosphonate imaging probes for bone active drugs.

Sun S, Błażewska KM, Kashemirov BA, Roelofs AJ, Coxon FP, Rogers MJ, Ebetino FH, McKenna MJ, McKenna CE.

Phosphorus Sulfur Silicon Relat Elem. 2011 Apr;186(4):970-971.

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