Joshua J Ziarek

Summary

Affiliation: Medical College of Wisconsin
Country: USA

Publications

  1. pmc Sulfotyrosine recognition as marker for druggable sites in the extracellular space
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA E Mails J J Z M S H F C P
    Int J Mol Sci 12:3740-56. 2011
  2. pmc Heparin oligosaccharides inhibit chemokine (CXC motif) ligand 12 (CXCL12) cardioprotection by binding orthogonal to the dimerization interface, promoting oligomerization, and competing with the chemokine (CXC motif) receptor 4 (CXCR4) N terminus
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
    J Biol Chem 288:737-46. 2013
  3. ncbi request reprint Fragment-based optimization of small molecule CXCL12 inhibitors for antagonizing the CXCL12/CXCR4 interaction
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA
    Curr Top Med Chem 12:2727-40. 2012
  4. pmc Binding site identification and structure determination of protein-ligand complexes by NMR a semiautomated approach
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, Milwaukee, Wisconsin, USA
    Methods Enzymol 493:241-75. 2011
  5. pmc Targeting SDF-1/CXCL12 with a ligand that prevents activation of CXCR4 through structure-based drug design
    Christopher T Veldkamp
    Department of Biochemistry, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, Wisconsin 53226, USA
    J Am Chem Soc 132:7242-3. 2010
  6. pmc A locked, dimeric CXCL12 variant effectively inhibits pulmonary metastasis of CXCR4-expressing melanoma cells due to enhanced serum stability
    Tomonori Takekoshi
    Department of Dermatology, Medical College of Wisconsin, FEC 4100, 9200 W Wisconsin Ave, Milwaukee, WI 53226, USA
    Mol Cancer Ther 11:2516-25. 2012
  7. pmc Monomeric structure of the cardioprotective chemokine SDF-1/CXCL12
    Christopher T Veldkamp
    Department of Biochemistry, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
    Protein Sci 18:1359-69. 2009
  8. pmc Monomeric and dimeric CXCL12 inhibit metastasis through distinct CXCR4 interactions and signaling pathways
    Luke J Drury
    Department of Microbiology and Molecular Genetics, Medical College of Wisconsin, 8701 West Watertown Plank Road, Milwaukee, WI 53214, USA
    Proc Natl Acad Sci U S A 108:17655-60. 2011

Collaborators

Detail Information

Publications8

  1. pmc Sulfotyrosine recognition as marker for druggable sites in the extracellular space
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA E Mails J J Z M S H F C P
    Int J Mol Sci 12:3740-56. 2011
    ..Rational drug discovery efforts targeting these sites may be useful in the development of specific as well as broad-spectrum chemokine inhibitors...
  2. pmc Heparin oligosaccharides inhibit chemokine (CXC motif) ligand 12 (CXCL12) cardioprotection by binding orthogonal to the dimerization interface, promoting oligomerization, and competing with the chemokine (CXC motif) receptor 4 (CXCR4) N terminus
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
    J Biol Chem 288:737-46. 2013
    ..These results clarify the structural basis for GAG recognition by CXCL12 and lend insight into the development of CXCL12-based therapeutics...
  3. ncbi request reprint Fragment-based optimization of small molecule CXCL12 inhibitors for antagonizing the CXCL12/CXCR4 interaction
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA
    Curr Top Med Chem 12:2727-40. 2012
    ..The fragment from this library that exhibited the highest affinity and ligand efficiency (11: K(d) = 13 μM, LE = 0.33) may serve as a starting point for development of inhibitors targeting the sY12 site...
  4. pmc Binding site identification and structure determination of protein-ligand complexes by NMR a semiautomated approach
    Joshua J Ziarek
    Department of Biochemistry, Medical College of Wisconsin, Milwaukee, Wisconsin, USA
    Methods Enzymol 493:241-75. 2011
    ....
  5. pmc Targeting SDF-1/CXCL12 with a ligand that prevents activation of CXCR4 through structure-based drug design
    Christopher T Veldkamp
    Department of Biochemistry, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, Wisconsin 53226, USA
    J Am Chem Soc 132:7242-3. 2010
    ..This compound selectively inhibits SDF1-induced CXCR4 signaling in THP1 cells. Our results suggest that sulfotyrosine recognition sites can be targeted for the development of novel chemokine inhibitors...
  6. pmc A locked, dimeric CXCL12 variant effectively inhibits pulmonary metastasis of CXCR4-expressing melanoma cells due to enhanced serum stability
    Tomonori Takekoshi
    Department of Dermatology, Medical College of Wisconsin, FEC 4100, 9200 W Wisconsin Ave, Milwaukee, WI 53226, USA
    Mol Cancer Ther 11:2516-25. 2012
    ..In summary, our results suggest CXCL122 possesses greater potential as an antimetastatic drug as compared with AMD3100 or wtCXCL12, potentially due to enhanced serum stability in the presence of N-terminal degrading enzymes...
  7. pmc Monomeric structure of the cardioprotective chemokine SDF-1/CXCL12
    Christopher T Veldkamp
    Department of Biochemistry, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
    Protein Sci 18:1359-69. 2009
    ..We conclude that interactions with the alignment medium biased the previous structure, masking flexibility in the helix position that may be essential for the distinct functional properties of the SDF-1 monomer...
  8. pmc Monomeric and dimeric CXCL12 inhibit metastasis through distinct CXCR4 interactions and signaling pathways
    Luke J Drury
    Department of Microbiology and Molecular Genetics, Medical College of Wisconsin, 8701 West Watertown Plank Road, Milwaukee, WI 53214, USA
    Proc Natl Acad Sci U S A 108:17655-60. 2011
    ..We conclude that cellular migration is tightly regulated by selective CXCR4 signaling evoked by unique interactions with distinct ligand quaternary structures...