Probing the opioid receptor complex with (+)-trans-SUPERFIT. II. Evidence that μ ligands are noncompetitive inhibitors of the δcx opioid peptide binding site

Peptides ◽  
1992 ◽  
Vol 13 (6) ◽  
pp. 1137-1143 ◽  
Author(s):  
Richard B. Rothman ◽  
Artin Mahboubi ◽  
Victor Bykov ◽  
Chong-Ho Kim ◽  
Brian R. de Costa ◽  
...  
Keyword(s):  
Binding Site ◽  
Opioid Receptor ◽  
Peptide Binding ◽  
Opioid Peptide ◽  
Receptor Complex ◽  
Peptide Binding Site ◽  
Noncompetitive Inhibitors

Opioid peptide receptor studies. 9. Identification of a novel non-μ- non-δ-like opioid peptide binding site in rat brain

Peptides ◽  
1998 ◽  
Vol 19 (6) ◽  
pp. 1079-1090 ◽  
Author(s):  
Qing Ni ◽  
Heng Xu ◽  
John S Partilla ◽  
Kenner C Rice ◽  
Dorota Matecka ◽  
...  
Keyword(s):  
Binding Site ◽  
Rat Brain ◽  
Peptide Binding ◽  
Opioid Peptide ◽  
Peptide Receptor ◽  
Peptide Binding Site

Rapid Elaboration of Fragments into Leads Applied to Bromodomain-3 Extra Terminal Domain

2020 ◽  
Author(s):  
Luke Adams ◽  
Lorna E. Wilkinson-White ◽  
Menachem J. Gunzburg ◽  
Stephen J. Headey ◽  
Martin J. Scanlon ◽  
...  
Keyword(s):  
Binding Site ◽  
Systematic Approach ◽  
Structural Information ◽  
Peptide Binding ◽  
Chemical Diversity ◽  
Chemical Probes ◽  
Protein Targets ◽  
Structure Activity ◽  
Peptide Binding Site ◽  
Selection Of

The development of low-affinity fragment hits into higher affinity leads is a major hurdle in fragment-based drug design. Here we demonstrate an approach for the Rapid Elaboration of Fragments into Leads (REFiL) applying an integrated workflow that provides a systematic approach to generate higher-affinity binders without the need for structural information. The workflow involves the selection of commercial analogues of fragment hits to generate preliminary structure-activity relationships. This is followed by parallel microscale chemistry using chemoinformatically designed reagent libraries to rapidly explore chemical diversity. Upon completion of a fragment screen against Bromodomain-3 extra terminal (BRD3-ET) domain we applied the REFiL workflow, which allowed us to develop a series of tetrahydrocarbazole ligands that bind to the peptide binding site of BRD3-ET. With REFiL we were able to rapidly improve binding affinity >30-fold. The REFiL workflow can be applied readily to a broad range of protein targets without the need of a structure, allowing the efficient evolution of low-affinity fragments into higher affinity leads and chemical probes.<br>

Solubilization and Characterization of Calcitonin Gene-Related Peptide Binding Site from Porcine Spinal Cord

1988 ◽  
Vol 50 (2) ◽  
pp. 480-485 ◽  
Author(s):  
Osamu Hiroshima ◽  
Yoshihisa Sano ◽  
Teruaki Yuzuriha ◽  
Chiyuki Yamato ◽  
Akira Saito ◽  
...  
Keyword(s):  
Spinal Cord ◽  
Binding Site ◽  
Peptide Binding ◽  
Calcitonin Gene Related Peptide ◽  
Related Peptide ◽  
Calcitonin Gene ◽  
Peptide Binding Site

The Crystal Structures of the SH2 Domain of p56lckComplexed with Two Phosphonopeptides Suggest a Gated Peptide Binding Site

1995 ◽  
Vol 246 (2) ◽  
pp. 344-355 ◽  
Author(s):  
Vincent Mikol ◽  
Götz Baumann ◽  
Thomas H. Keller ◽  
Ute Manning ◽  
Mauro G.M. Zurini
Keyword(s):  
Binding Site ◽  
Crystal Structures ◽  
Peptide Binding ◽  
Sh2 Domain ◽  
Peptide Binding Site

Autoradiographic localization of a novel peptide binding site in rat brain using the substance P analog, eledoisin

Neuropeptides ◽  
1984 ◽  
Vol 4 (4) ◽  
pp. 343-349 ◽  
Author(s):  
Richard B. Rothman ◽  
Janine A. Danks ◽  
Miles Herkenham ◽  
Margaret A. Cascieri ◽  
Gary G. Chicchi ◽  
...  
Keyword(s):  
Substance P ◽  
Binding Site ◽  
Rat Brain ◽  
Peptide Binding ◽  
Peptide Binding Site

scholarly journals Sequence-selective DNA binding with cell-permeable oligoguanidinium–peptide conjugates

2015 ◽  
Vol 51 (23) ◽  
pp. 4811-4814 ◽  
Author(s):  
Jesús Mosquera ◽  
Mateo I. Sánchez ◽  
Julián Valero ◽  
Javier de Mendoza ◽  
M. Eugenio Vázquez ◽  
...  
Keyword(s):  
Dna Binding ◽  
Binding Site ◽  
Peptide Binding ◽  
Peptide Fragment ◽  
Peptide Conjugates ◽  
Bzip Protein ◽  
Short Peptide ◽  
Peptide Binding Site ◽  
Selective Dna Binding

Conjugation of a short peptide fragment from a bZIP protein to an oligoguanidinium tail results in a DNA-binding miniprotein that selectively interacts with composite sequences containing the peptide-binding site next to an A/T-rich tract.

Crystal structure of YrrB: A TPR protein with an unusual peptide-binding site

2007 ◽  
Vol 360 (4) ◽  
pp. 784-790 ◽  
Author(s):  
Dohyun Han ◽  
Jongkil Oh ◽  
Kyunggon Kim ◽  
Hyosun Lim ◽  
Youngsoo Kim
Keyword(s):  
Crystal Structure ◽  
Binding Site ◽  
Peptide Binding ◽  
Peptide Binding Site

Evidence for a μ–δ opioid receptor complex in CHO cells co-expressing μ and δ opioid peptide receptors

Peptides ◽  
2008 ◽  
Vol 29 (8) ◽  
pp. 1424-1431 ◽  
Author(s):  
John M. Rutherford ◽  
Jiabei Wang ◽  
Heng Xu ◽  
Christina M. Dersch ◽  
John S. Partilla ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Cho Cells ◽  
Opioid Peptide ◽  
Receptor Complex ◽  
Peptide Receptors ◽  
Δ Opioid Receptor

scholarly journals Characterization of the Escherichia coli SecA Signal Peptide-Binding Site

2011 ◽  
Vol 194 (2) ◽  
pp. 307-316 ◽  
Author(s):  
L. M. Grady ◽  
J. Michtavy ◽  
D. B. Oliver
Keyword(s):  
Escherichia Coli ◽  
Binding Site ◽  
Signal Peptide ◽  
Peptide Binding ◽  
Peptide Binding Site
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