Search results for: W. David Wilson

Items from 1 to 20 out of 142 results

article

Physiologic effects of furosemide in combination with water restriction when administered at 4 and 24 hours prior to high‐intensity treadmill training

Heather K. Knych, W. David Wilson, Alina Vale, Philip H. Kass, more

Journal of Veterinary Pharmacology and Therapeutics > 43 > 6 > 565 - 576

Although controversial, due to its reported effectiveness in attenuating bleeding associated with exercise‐induced pulmonary hemorrhage (EIPH), furosemide is currently a permitted race day medication in most North American racing jurisdictions. The objective of this study was to assess the efficacy of furosemide in reducing the presence and severity of EIPH when administered 24 hr prior to strenuous...

article

Small Sequence‐Sensitive Compounds for Specific Recognition of the G⋅C Base Pair in DNA Minor Groove

Abdelbasset A. Farahat, Pu Guo, Hadir Shoeib, Ananya Paul, more

Chemistry – A European Journal > 26 > 20 > 4539 - 4551

A series of small diamidines with thiophene and modified N‐alkylbenzimidazole σ‐hole module represent specific binding to single G⋅C base pair (bp) DNA sequence. The variation of N‐alkyl or aromatic rings were sensitive to microstructures of the DNA minor groove. Thirteen new compounds were synthesized to test their binding affinity and selectivity. The dicyanobenzimidazoles needed to synthesize the...

article

Hierarchical Nanotube Self‐Assembly of DNA Minor Groove‐Binding Ligand DB921 via Alkali Halide Triggering

Ryo Mizuta, Juliette M. Devos, Theyencheri Narayanan, Mizar Oliva, more

Macromolecular Symposia > 386 > 1 > n/a - n/a

A systematic study into a novel self‐assembling system is presented whereby the small molecule DB921 forms nearly monodisperse nanotubes upon addition of a suitable salt. Small‐angle X‐ray scattering and negative stain transmission electron microscopy are employed as the principal characterization methods to study both the fundamental assembly processes and reaction kinetics. The assembly is found...

article

Indole and Benzimidazole Bichalcophenes: Synthesis, DNA Binding and Antiparasitic Activity

Abdelbasset A. Farahat, Mohamed A. Ismail, Arvind Kumar, Tanja Wenzler, more

European Journal of Medicinal Chemistry > 2018 > 143 > C > 1590-1596

A novel series of indole and benzimidazole bichalcophene diamidine derivatives were prepared to study their antimicrobial activity against the tropical parasites causing African sleeping sickness and malaria. The dicyanoindoles needed to synthesize the target diamidines were obtained through Stille coupling reactions while the bis-cyanobenzimidazoles intermediates were made via condensation/cyclization...

article

First Structure of a Designed Minor Groove Binding Heterocyclic Cation that Specifically Recognizes Mixed DNA Base Pair Sequences

Narinder K. Harika, Markus W. Germann, W. David Wilson

Chemistry – A European Journal > 23 > 69 > 17612 - 17620

The high‐resolution NMR structure of the first heterocyclic, non‐amide, organic cation that strongly and selectively recognizes mixed AT/GC bp (bp=base pair) sequences of DNA in a 1:1 complex is described. Compound designs of this type provide essential methods for control of functional, non‐genomic DNA sequences and have broad cell uptake capability, based on studies from animals to humans. The high‐resolution...

article

Inhibition of the myeloid master regulator PU.1 as a therapeutic strategy in acute myeloid leukemia

Ileana Antony-Debre, Joana Leite, Ananya Paul, Kelly Mitchell, more

Experimental Hematology > 2017 > 53 > S > S133

article

Modulation of topoisomerase IIα expression and chemosensitivity through targeted inhibition of NF-Y:DNA binding by a diamino p-anisyl-benzimidazole (Hx) polyamide

Luke Pett, Konstantinos Kiakos, Vijay Satam, Pravin Patil, more

Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms > 2017 > 1860 > 5 > 617-629

Sequence specific polyamide HxIP 1, targeted to the inverted CCAAT Box 2 (ICB2) on the topoisomerase IIα (topo IIα) promoter can inhibit NF-Y binding, re-induce gene expression and increase sensitivity to etoposide. To enhance biological activity, diamino-containing derivatives (HxI*P 2 and HxIP* 3) were synthesised incorporating an alkyl amino group at the N1-heterocyclic position of the imidazole/pyrrole...

article

Exploration of DAPI analogues: Synthesis, antitrypanosomal activity, DNA binding and fluorescence properties

Abdelbasset A. Farahat, Arvind Kumar, Martial Say, Tanja Wenzler, more

European Journal of Medicinal Chemistry > 2017 > 128 > C > 70-78

The DAPI structure has been modified by replacing the phenyl group with substituted phenyl or heteroaryl rings. Twelve amidines were synthesized and their DNA binding, fluorescence properties, in vitro and in vivo activities were evaluated. These compounds are shown to bind in the DNA minor groove with high affinity, and exhibit superior in vitro antitrypanosomal activity to that of DAPI. Six new...

article

Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI

Abdelbasset A. Farahat, Cheree Bennett-Vaughn, Ekaterina M. Mineva, Arvind Kumar, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 24 > 5907-5910

A series of novel benzimidazole diamidines were prepared from the corresponding dicyano analogues either by applying Pinner methodology (5a–c, 10 and 13a) or by making amidoximes intermediates that were reduced to the corresponding amidines (15a–c). The new amidines were evaluated in vitro against the protozoan parasite Trypanosoma brucei rhodesiense (T. b. r.). The thiophene analogue 5b and the N-methyl...

article

The Thiophene “Sigma‐Hole” as a Concept for Preorganized, Specific Recognition of G⋅C Base Pairs in the DNA Minor Groove

Pu Guo, Ananya Paul, Arvind Kumar, Abdelbasset A. Farahat, more

Chemistry – A European Journal > 22 > 43 > 15404 - 15412

In spite of its importance in cell function, targeting DNA is under‐represented in the design of small molecules. A barrier to progress in this area is the lack of a variety of modules that recognize G⋅C base pairs (bp) in DNA sequences. To overcome this barrier, an entirely new design concept for modules that can bind to mixed G⋅C and A⋅T sequences of DNA is reported herein. Because of their successes...

article

Mixed up minor groove binders: Convincing A·T specific compounds to recognize a G·C base pair

Ananya Paul, Rupesh Nanjunda, Arvind Kumar, Sarah Laughlin, more

Bioorganic & Medicinal Chemistry Letters > 2015 > 25 > 21 > 4927-4932

DNA minor-groove-binding compounds have limited biological applications, in part due to problems with sequence specificity that cause off-target effects. A model to enhance specificity has been developed with the goal of preparing compounds that bind to two AT sites separated by G·C base pairs. Compounds of interest were probed using thermal melting, circular dichroism, mass spectrometry, biosensor-SPR,...

article

AzaHx, a novel fluorescent, DNA minor groove and G·C recognition element: Synthesis and DNA binding properties of a p-anisyl-4-aza-benzimidazole-pyrrole-imidazole (azaHx-PI) polyamide

Vijay Satam, Balaji Babu, Pravin Patil, Kimberly A. Brien, more

Bioorganic & Medicinal Chemistry Letters > 2015 > 25 > 17 > 3681-3685

The design, synthesis, and DNA binding properties of azaHx-PI or p-anisyl-4-aza-benzimidazole-pyrrole-imidazole (5) are described. AzaHx, 2-(p-anisyl)-4-aza-benzimidazole-5-carboxamide, is a novel, fluorescent DNA recognition element, derived from Hoechst 33258 to recognize G·C base pairs. Supported by theoretical data, the results from DNase I footprinting, CD, ΔT_M, and SPR studies provided evidence...

article

Resolution of Mixed Site DNA Complexes with Dimer‐Forming Minor‐Groove Binders by Using Electrospray Ionization Mass Spectrometry: Compound Structure and DNA Sequence Effects

Sarah Laughlin, Siming Wang, Arvind Kumar, Abdelbasset A. Farahat, more

Chemistry – A European Journal > 21 > 14 > 5528 - 5539

Small‐molecule targeting of the DNA minor groove is a promising approach to modulate genomic processes necessary for normal cellular function. For instance, dicationic diamindines, a well‐known class of minor groove binding compounds, have been shown to inhibit interactions of transcription factors binding to genomic DNA. The applications of these compounds could be significantly expanded if we understand...

article

Unraveling the Structural, Dynamic, Thermodynamic, and Kinetic Heterogeneity in DNA Site Recognition by Structurally Homologous ETS Transcription Factors

Gregory M.K. Poon, Shuo Wang, Gaofei He, Ana Tolic, more

Biophysical Journal > 2015 > 108 > 2 Supplement 1 > 75a-76a

article

Kinetics and Structures on the Molecular Path to the Quadruplex Form of the Human Telomere

W. David Wilson, Ananya Paul

Journal of Molecular Biology > 2014 > 426 > 8 > 1625-1628

article

Mechanistic Diversity in DNA Site Discrimination by Structurally Homologous ETS-Family Transcription Factors

Miles H. Linde, Ana Tolic, Manoj M. Munde, W. David Wilson, more

Biophysical Journal > 2014 > 106 > 2 Supplement 1 > 497a

article

A novel approach using electrospray ionization mass spectrometry to study competitive binding of small molecules with mixed DNA sequences

Sarah Laughlin, Siming Wang, Arvind Kumar, David W. Boykin, more

Analytical and Bioanalytical Chemistry > 2014 > 406 > 25 > 6441-6445

Minor groove binding compounds have been shown to induce changes in global DNA conformation, allosterically inhibiting DNA-protein interactions necessary for transcriptional processes. Many minor groove binders are specific for AT base pairs but have little preference over alternating AT or A-tract sequences. Few compounds, other than polyamides, show selectivity for mixed sequences with AT and GC...

article

Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues

Laixing Hu, Alpa Patel, Lavanya Bondada, Sihyung Yang, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 21 > 6732-6741

Dicationic 2,6-diphenylpyrazines, aza-analogues and prodrugs were synthesized; evaluated for DNA affinity, activity against Trypanosoma brucei rhodesiense (T. b. r.) and Plasmodium falciparum (P. f.) in vitro, efficacy in T. b. r. STIB900 acute and T. b. brucei GVR35 CNS mouse models. Most diamidines gave poly(dA-dT) ₂ ΔT _m values greater than pentamidine, IC ₅₀ values: T....

article

Design, synthesis, and DNA binding characteristics of a group of orthogonally positioned diamino, N-formamido, pyrrole- and imidazole-containing polyamides

Sameer Chavda, Balaji Babu, Pravin Patil, Adam Plaunt, more

Bioorganic & Medicinal Chemistry > 2013 > 21 > 13 > 3907-3918

Orthogonally positioned diamino/dicationic polyamides (PAs) have good water solubility and enhanced binding affinity, whilst retaining DNA minor groove and sequence specificity compared to their monoamino/monocationic counterparts. The synthesis and DNA binding properties of the following diamino PAs: f-IPI (3a), f-IPP (4), f-PIP (5), and f-PPP (6) are described. P denotes the site where a 1-propylamino...

article

Conformational modulation of DNA by polyamide binding: structural effects of f‐Im‐Py‐Im based derivatives on 5′‐ACGCGT‐3′

Shuo Wang, Yun Chai, Balaji Babu, Vijay Satam, more

Journal of Molecular Recognition > 26 > 8 > 331 - 340

The DNA sequence 5′‐ACGCGT‐3′ is in the core site of the Mlu 1 cell‐cycle box, a transcriptional element in the promoter region of human Dbf4 gene that is highly correlated with a large number of aggressive solid cancers. The polyamide formamido‐imidazole‐pyrrole‐imidazole‐amine⁺ (f‐Im‐Py‐Im‐Am⁺) can target the minor groove of 5′‐ACGCGT‐3′ as an antiparallel stacked dimer and has shown good activity...

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Search results for: W. David Wilson

Physiologic effects of furosemide in combination with water restriction when administered at 4 and 24 hours prior to high‐intensity treadmill training

Small Sequence‐Sensitive Compounds for Specific Recognition of the G⋅C Base Pair in DNA Minor Groove

Hierarchical Nanotube Self‐Assembly of DNA Minor Groove‐Binding Ligand DB921 via Alkali Halide Triggering

Indole and Benzimidazole Bichalcophenes: Synthesis, DNA Binding and Antiparasitic Activity

First Structure of a Designed Minor Groove Binding Heterocyclic Cation that Specifically Recognizes Mixed DNA Base Pair Sequences

Inhibition of the myeloid master regulator PU.1 as a therapeutic strategy in acute myeloid leukemia

Modulation of topoisomerase IIα expression and chemosensitivity through targeted inhibition of NF-Y:DNA binding by a diamino p-anisyl-benzimidazole (Hx) polyamide

Exploration of DAPI analogues: Synthesis, antitrypanosomal activity, DNA binding and fluorescence properties

Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI

The Thiophene “Sigma‐Hole” as a Concept for Preorganized, Specific Recognition of G⋅C Base Pairs in the DNA Minor Groove

Mixed up minor groove binders: Convincing A·T specific compounds to recognize a G·C base pair

AzaHx, a novel fluorescent, DNA minor groove and G·C recognition element: Synthesis and DNA binding properties of a p-anisyl-4-aza-benzimidazole-pyrrole-imidazole (azaHx-PI) polyamide

Resolution of Mixed Site DNA Complexes with Dimer‐Forming Minor‐Groove Binders by Using Electrospray Ionization Mass Spectrometry: Compound Structure and DNA Sequence Effects

Unraveling the Structural, Dynamic, Thermodynamic, and Kinetic Heterogeneity in DNA Site Recognition by Structurally Homologous ETS Transcription Factors

Kinetics and Structures on the Molecular Path to the Quadruplex Form of the Human Telomere

Mechanistic Diversity in DNA Site Discrimination by Structurally Homologous ETS-Family Transcription Factors

A novel approach using electrospray ionization mass spectrometry to study competitive binding of small molecules with mixed DNA sequences

Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues

Design, synthesis, and DNA binding characteristics of a group of orthogonally positioned diamino, N-formamido, pyrrole- and imidazole-containing polyamides

Conformational modulation of DNA by polyamide binding: structural effects of f‐Im‐Py‐Im based derivatives on 5′‐ACGCGT‐3′

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