L
Leonard W. Rozamus
Researcher at ARIAD Pharmaceuticals, Inc.
Publications - 39
Citations - 2016
Leonard W. Rozamus is an academic researcher from ARIAD Pharmaceuticals, Inc.. The author has contributed to research in topics: FKBP & Trifluoromethyl. The author has an hindex of 17, co-authored 39 publications receiving 1930 citations. Previous affiliations of Leonard W. Rozamus include University of Pennsylvania.
Papers
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Journal ArticleDOI
Redesigning an FKBP–ligand interface to generate chemical dimerizers with novel specificity
Tim Clackson,Wu Yang,Leonard W. Rozamus,Marcos Hatada,Jane F. Amara,Carl T. Rollins,Lauren F. Stevenson,Shannon R. Magari,Susan A. Wood,Nancy L. Courage,Xiaode Lu,Franklin Cerasoli,Michael Z. Gilman,Dennis A. Holt +13 more
TL;DR: Ligands that bind specifically to a mutated FKBP over the wild-type protein are designed by remodeling an FK BP-ligand interface to introduce a specificity binding pocket and showed that recognition is surprisingly relaxed, with the modified ligand only partially filling the engineered cavity.
Journal ArticleDOI
Long-term pharmacologically regulated expression of erythropoietin in primates following AAV-mediated gene transfer
Victor M. Rivera,Guangping Gao,Rebecca L. Grant,Michael A. Schnell,Philip W. Zoltick,Leonard W. Rozamus,Tim Clackson,James M. Wilson +7 more
TL;DR: Data indicate that one-time or infrequent gene transfer followed by dimerizer regulation is a promising approach for delivery of therapeutic proteins.
ComponentDOI
Design, synthesis, and kinetic evaluation of high-affinity fkbp ligands and the x-ray crystal-structures of their complexes with fkbp12.
Dennis A. Holt,Juan I. Luengo,Dennis S. Yamashita,Hye-Ja Oh,Arda L. Konialian,H.‐K. Yen,Leonard W. Rozamus,Martin Brandt,Mary J. Bossard,Mark Alan Levy,Drake S. Eggleston,Jun Liang,L.W Schultz,T.J Stout,Jon Clardy +14 more
TL;DR: In this article, the design and synthesis of high affinity FKBP12 ligands is described, which can inhibit the cis-trans-peptidylprolyl isomerase (rotamase) activity with an inhibition constant as low as 1 nM, yet they possess remarkable structural simplicity relative to FK506 and rapamycin.
Patent
Materials and method for treating or preventing pathogenic fungal infection
Dennis A. Holt,Terence P. Keenan,Timothy P. Clackson,Leonard W. Rozamus,Wu Yang,Michael Z. Gilman +5 more
TL;DR: In this paper, the authors discuss derivatives of rapamycin and their antifungal uses and materials and methods relevant to the identification of non-immunosuppressive antIFungal Rapamycin derivatives.
Patent
Phosphorus-containing compounds uses thereof
TL;DR: In this article, a new family of phosphorus-containing compounds containing a moiety JQA- was introduced, in which: A is absent or is -O-, -S- or -NR2-; Q is absent, or Q may be -V-, OVA, SVA or NR2V-, where V is an aliphatic, heteroaliphatic aryl, or heteroaryl moiety.