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Adventures in drug discovery: Potent agents based on ligands for cell-surface receptors

Article Abstract:

Different approaches are presented for the identification of high-affinity ligands for cell-surface receptors, en route to drug candidates. The protease-activated receptor-I (PAR-I) project has resulted in a pharmacological tool compound that has facilitated in vivo proof-of-principle studies, whereas the vasopressin and fibrinogen receptor projects have resulted in many preclinical development compounds, three of which have advanced into human clinical trials.

Author: Maryanoff, Bruce E.
Publisher: American Chemical Society
Publication Name: Accounts of Chemical Research
Subject: Science and technology
ISSN: 0001-4842
Year: 2006
Cell receptors

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Applications of one-bead one-compound combinatorial libraries and chemical microarrays in signal transduction research

Article Abstract:

Beads synthesized by the "one-bead-one-compound" (OBOC) combinational library are screened and positive beads are isolated for structure analysis. Developing a novel encoding strategy for OBOC libraries, Peptidomimetic and small-molecule ligands specifically interacting with cellular proteins are identified.

Author: Lam, Kit S., Liu, Ruiwu, Miyamoto, Suzanne, Lehman, Alan L., Tuscano, Joseph M.
Publisher: American Chemical Society
Publication Name: Accounts of Chemical Research
Subject: Science and technology
ISSN: 0001-4842
Year: 2003
Protein microarrays

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Phosphotyrosyl mimetics in the development of signal transduction inhibitors

Article Abstract:

Phosphotyrosyl (pTyr) residues roles in cellular signal transduction and pTyr mimetic development and utilization are reported. pTyr motifs act as signal antagonists in facilitating recognition and binding necessary for critical protein interactions.

Author: Burke, Terrence R., Jr, Lee, Kyeong
Publisher: American Chemical Society
Publication Name: Accounts of Chemical Research
Subject: Science and technology
ISSN: 0001-4842
Year: 2003
Influence, Phosphotransferases

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Subjects list: Research, Ligands (Biochemistry), Cellular signal transduction
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