Medicinal Chemistry/Formulations and Manufacturing

Synthesis and Biophysical Characterization of R-6'-Me-α-l-LNA Modified Oligonucleotides

Seth PP, Yu J, Allerson CR, Berdeja A, Swayze EE

Bioorg Med Chem Lett. 2010 Dec 31. [Epub ahead of print]

An Exocyclic Methylene Group Acts As a Bioisostere of the 2'-Oxygen Atom in LNA

Seth PP, Allerson CR, Berdeja A, Siwkowski A, Pallan PS, Gaus H, Prakash TP, Watt AT, Egli M, Swayze EE

J Am Chem Soc. 2010 Oct 27;132(42):14942-50

Synthesis and Biophysical Evaluation of 2',4'-Constrained 2'O-Methoxyethyl and 2',4'-Constrained 2'O-Ethyl Nucleic Acid Analogues

Seth PP, Vasquez G, Allerson CA, Berdeja A, Gaus H, Kinberger GA, Prakash TP, Migawa MT, Bhat B, Swayze EE

J Org Chem. 2010 Mar 5;75(5):1569-81

Antisense Oligonucleotides Containing Conformationally Constrained 2',4'-(N-Methoxy)aminomethylene and 2',4'-Aminooxymethylene and 2'-O,4'-C-Aminomethylene Bridged Nucleoside Analogues Show Improved Potency in Animal Models

Prakash TP, Siwkowski A, Allerson CR, Migawa MT, Lee S, Gaus HJ, Black C, Seth PP, Swayze EE, Bhat B

J Med Chem. 2010 Jan 28;53:1636–1650

Activity of siRNAs with 2-Thio-2'-O-Methyluridine Modification in Mammalian Cells

Prakash TP, Naik N, Sioufi N, Bhat B, Swayze EE

Nucleosides, Nucleotides and Nucleic Acids. 2009 Oct 10;28:902-910

Short Antisense Oligonucleotides with Novel 2'-4' Conformationaly Restricted Nucleoside Analogues Show Improved Potency Without Increased Toxicity in Animals.

Seth PP, Siwkowski A, Allerson CR, Vasquez G, Lee S, Prakash TP, Wancewicz EV, Witchell D, Swayze EE.

Journal of Medicinal Chemistry. 2008 December [Epub ahead of print].

Oral delivery of antisense oligonucleotides in man.

Tillman LG, Geary RS, Hardee GE.

J Pharm Sci. 2008 Jan;97(1):225-236.

Systematic Studies on the Paracellular Permeation of Model Permeants and Oligonucleotides in the Rat Small Intestine With Chenodeoxycholate as Enhancer

Tsutsumi K, Li SK, Hymas RV, Teng CL, Tillman LG, Hardee GE, Higuchi WI, Ho NF

J Pharm Sci. 2008 Jan;97(1):350-67

The Positional Influence of the Helical Geometry of the Heteroduplex Substrate on Human RNase H1 Catalysis

Lima WF, Rose JB, Nichols JG, Wu H, Migawa MT, Wyrzykiewicz TK, Vasquez G, Swayze EE, Crooke ST

Mol Pharmacol. 2007 Jan;71(1):73-82

A Novel Universal Linker for Efficient Synthesis of Phosphorothioate Oligonucleotides.

Wang Z, Olsen P, Ravikumar VT.

Nucleosides Nucleotides Nucleic Acids. 2007;26(3):259-69.

Dermal Delivery of Topically Applied Oligonucleotides via Follicular Transport in Mouse Skin

Dokka S, Cooper SR, Kelly S, Hardee GE, Karras JG

J Invest Dermatol. 2005 May;124(5):971-5

Synthesis of antisense oligonucleotides with minimum depurination.

Krotz, A. H., Cole, D.L. , Ravikumar, V. T.

Nucleosides Nucleotides Nucleic Acids. 22(2):129-34, 2003.

Applications of green chemistry in the manufacture of oligonucleotide drugs.

Sanghvi, Y.S., Ravikumar, VT., Scozzari, A.N., Cole, D.L.

Pure App Chem. 73(1):175-180, 2001.

Intercellular adhesion molecule-1 suppression in skin by topical delivery of anti-sense oligonucleotides.

Mehta, R.C., Stecker, K.K., Cooper, S.R., Templin, M.V., Tsai, Y.J., Condon, T.P., Bennett, C.F., Hardee, G.E.

J Invest Dermatol.115(5):805-812, 2000.

Pharmacokinetic and toxicity profile of a phosphorothioate oligonucleotide following inhalation delivery to lung in mice.

Templin, M. V., Levin, A. A., Graham, M. J., Aberg, P. M., Axelsson, B. I., Butler, M., Geary, R. S., and Bennett, C. F.

Antisense Nucleic Acid Drug Dev. 10(5):359-368, 2000.