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Nanomolar Inhibitors for Two Distinct Biological Target Families from a Single Synthetic Sequence: A Next Step in Combinatorial Library Design?
Author(s) -
Burns Christopher J.,
Groneberg Robert D.,
Salvino Joseph M.,
McGeehan Gerard,
Condon Stephen M.,
Morris Robert,
Morrissette Matthew,
Mathew Rose,
Darnbrough Shelley,
Neuenschwander Kent,
Scotese Anthony,
Djuric Stevan W.,
Ullrich John,
Labaudiniere Richard
Publication year - 1998
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/(sici)1521-3773(19981102)37:20<2848::aid-anie2848>3.0.co;2-c
Subject(s) - pharmacophore , computational biology , matrix metalloproteinase , sequence (biology) , combinatorial chemistry , drug discovery , computer science , biology , chemistry , bioinformatics , genetics
One common synthetic route creates small‐molecule libraries directed toward two functionally distinct target families. The novel structural template 1 can independently display the necessary pharmacophore patterns for inhibition of members of two different biomolecular target families, the matrix metalloproteinases (MMPs) or the phosphodiesterases (PDEs). The incorporation of multiple target family directed design elements into combinatorial library design could help expedite the pharmaceutical lead discovery process. Z=OR′ (PDE4), H (MMPs).