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Search for New Synthetic Immunosuppressants. Antamanide Analogues Containing the Tetrazole Ring as a cis-Peptide Bond Mimetic

100%

Zubrzak P. , Kaczmarek K. , Kowalski M. L. , Szkudlińska B. , Zabrocki J.

2001

tom Vol. 75, nr 12

1869-1876

Linear and cyclic antamanide (ANT) analogues with dipeptide segments Pro2-Pro3, Pro7-Pro8 and both of them replaced by their tetrazole analogue Pro-psi[CN4]-Ala, respectively, have been synthesized by SPPS method and cyclization with TBTU reagent. The peptides were examined for their immunosuppressive activity in a lymphocyte proliferation test (LPT).

A beta-amino acid pyrokinin analog induces irregular pupariation behavior in larvae of the flesh fly Sarcophaga bullata

100%

Nachman R. J. , Zubrzak P. , Williams H. , Strey A. , Zdarek J.

nr 1-2

95-100

The developmental process of pupariation is accelerated by members of the pyrokinin class of neuropeptides in larvae of the flesh fly Sarcophaga bullata. A pyrokinin analog (Ac-Y[β3Phe]TPRLamide), in which a Phe residue is replaced with a β-amino acid, accelerates pupariation in this fly at a potency (0.2 pmol/larva) that matches that of the native pyrokinin factor. At higher concentrations, this β-amino acid pyrokinin analog induces irregular pupariation behavior patterns that are suggestive of neurotoxic properties. Biostable analogs based on this structure may in future provide analog leads with the potential to disrupt the important pupariation process in flies.

Structure-activity relationships for insect kinins on expressed receptors from a tick [Acari: Ixodidae] and a mosquito [Diptera: Culicidae]

100%

Taneja-Bageshwar S. , Strey A. , Zubrzak P. , Pietrantonio P. V. , Nachman R. J.

2005

nr 3

55-59

Search for new synthetic immunosuppressants II. Tetrazole analogues of hymenistatin I

86%

Zubrzak P. , Kociolek K. , Smoluch M. , Silberring J. , Kowalski M. L. , Szkudlinska B. , Zabrocki J.

Acta Biochimica Polonica

2001

tom 48

nr 4

Linear and cyclic hymenistatin I (HS I) analogues with dipeptide segments Ile2 -Pro3 , Pro3 -Pro4 and Val6 -Pro7 replaced by their tetrazole analogues Ile2-Ψ[CN4]-Ala3 , Pro3 -Ψ[CN4]-Ala4 and Val6 -Ψ[CN4]-Ala7 were synthesized by the solid phase peptide synthesis method and cyclized with the TBTU and/or HATU reagent. The peptides were examined for their immunosuppressive activity in the lymphocyte proliferation test (LPT).