Modern NMR spectroscopy of proteins and peptides in solution and its relevance to drug designPerspectives in Drug Discovery and Design - Tập 1 Số 2 - Trang 391-417 - 1993
Zuiderweg, E. R. P., van Doren, S. R., Kurochkin, A. V., Neubig, R. R., Majumdar, A.
The knowledge of the three-dimensional (3D) structures and conformational
dynamics of proteins and peptides is important for the understanding of
biochemical and genetic data derived for these molecules. This understanding can
ultimately be of help in drug design. We describe here the role of Nuclear
Magnetic Resonance (NMR) spectroscopy in this process for three distinct
situations: for small pro... hiện toàn bộ
GOLPE-guided region selectionPerspectives in Drug Discovery and Design - Tập 12 - Trang 71-86 - 1998
Gabriele Cruciani, Sergio Clementi, Manuel Pastor
The medicinal chemistry of FK-506Perspectives in Drug Discovery and Design - Tập 2 - Trang 145-162 - 1994
Mark T. Goulet, Kathleen M. Rupprecht, Peter J. Sinclair, Matthew J. Wyvratt, William H. Parsons
Substantial strides have been made in the past decade in the discovery of potent
immunosuppressants that are effective in the prevention of rejection in organ
transplantation and in the treatment of autoimmune diseases. The past three
years have witnessed stunning breakthroughs in the elucidation of the common
mechanism of immunosuppressive action of FK-506 and cyclosporin A (CsA). FK-506
is 50- t... hiện toàn bộ
Seeing our way to drug designPerspectives in Drug Discovery and Design - Tập 1 - Trang 329-344 - 1993
Arthur J. Olson, Garrett M. Morris
Interactive molecular graphics plays an important role in every stage of the
drug design process. The technology of molecular graphics has advanced
considerably over the past 30 years, both in terms of hardware features for
advanced rendering and computation, and in terms of software environments for
rapid, flexible and extensible program development. This paper discusses the
role of interactive c... hiện toàn bộ
The cysteine protease cathepsin B in cancerPerspectives in Drug Discovery and Design - Tập 6 - Trang 12-32 - 1996
Edith Elliott, Bonnie F. Sloane
Of the cysteine proteases, cathepsin B has been most often implicated in tumor
progression. Accumulating evidence indicates that the regulation of cathepsin B
and other cysteine proteases is under both transcriptional and
posttranscriptional control. The elucidation of such control mechanisms may be
important for therapeutic strategies aimed at reducing cathepsin B
overexpression in tumors and oth... hiện toàn bộ
ACD/Log P method descriptionPerspectives in Drug Discovery and Design - - 2000
Alanas A. Petrauskas, Eduard A. Kolovanov
This study describes the development of the ACD/Log P calculation method.
Analysis of 14 calculation methods revealed that the most accurate calculations
are obtained when correction factors are used. We evaluated the correction
factors used by Hansch and Leo in CLOGP in order to simplify their method. Most
of the CLOGP structural factors are included in our fragmental increments.
Aliphatic and ar... hiện toàn bộ
Non-nucleoside inhibitors of HIV-1 reverse transcriptasePerspectives in Drug Discovery and Design - Tập 1 - Trang 181-192 - 1993
Steven D. Young
Four years ago it became apparent that an allosteric site on HIV-1 reverse
transcriptase was responsible for the enzyme inhibitory activity of a number of
structurally diverse organic compounds. These molecules bear little resemblance
to the endogenous substrate, deoxynucleotide triphosphates, and through kinetic
measurements they were found to be noncompetitive inhibitors. When examined in
cell c... hiện toàn bộ
Estimating log P with atom/fragments and water solubility with log PPerspectives in Drug Discovery and Design - Tập 19 Số 1 - Trang 67-84 - 2000
Meylan, William M., Howard, Philip H.
An atom/fragment contribution method that predicts log P is described.
Coefficient values for 150 atom/fragments and 250 correction factors have been
derived from a training set of 2473 compounds. When applied to an independent
validation set of 10589 compounds, the method estimates log P with excellent
accuracy (correlation coefficient r 2 of 0.943, standard deviation of 0.473, and
absolute mean ... hiện toàn bộ