D. Mark Bickett

Research Triangle Park Foundation — United States

Biochemistry, Genetics and Molecular Biology · Life Sciences

12h-index757citations23works0.02yr avg
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Research Topics

Protease and Inhibitor Mechanisms(10), Peptidase Inhibition and Analysis(7), Rheumatoid Arthritis Research and Therapies(5), Diabetes Treatment and Management(3), Cell Adhesion Molecules Research(3)

Publications23 total

Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy
Bioorganic & Medicinal Chemistry Letters·2008· 20 citedOpen Access
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups
Bioorganic & Medicinal Chemistry Letters·2008· 7 citedOpen Access
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues
Bioorganic & Medicinal Chemistry Letters·2008· 7 citedOpen Access
Design of Selective and Soluble Inhibitors of Tumor Necrosis Factor-α Converting Enzyme (TACE)
Journal of Medicinal Chemistry·2001· 73 citedOpen Access
Inhibition of Tumor Necrosis Factor-α (TNF-α) Production and Arthritis in the Rat by GW3333, a Dual Inhibitor of TNF-α-Converting Enzyme and Matrix Metalloproteinases
Journal of Pharmacology and Experimental Therapeutics·2001· 39 cited
Screening And Design Of Tumor Necrosis Factor-
2000
Substrate Specificity of Human Collagenase 3 Assessed Using a Phage-displayed Peptide Library
Journal of Biological Chemistry·2000· 130 citedOpen Access
A high throughput assay for the TNF converting enzyme
Birkhäuser Basel eBooks·2000· 2 cited
TNFα converting enzyme
Birkhäuser Basel eBooks·1999· 6 cited
Erratum: Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-α
Nature·1997· 8 citedOpen Access
Structural features and biochemical properties of TNF-α converting enzyme (TACE)
Journal of Neuroimmunology·1997· 113 cited
Rapid synthesis of novel dipeptide inhibitors of human collagenase and gelatinase using solid phase chemistry
Bioorganic & Medicinal Chemistry Letters·1996· 19 cited
Structure-Activity Relationships for Inhibition of Type 1 and 2 Human 5.alpha.-Reductase and Human Adrenal 3.beta.-Hydroxy-.DELTA.5-steroid Dehydrogenase/3-Keto-.DELTA.5-steroid Isomerase by 6-Azaandrost-4-en-3-ones: Optimization of the C17 Substituent
Journal of Medicinal Chemistry·1995· 47 citedOpen Access
[3] Defined substrate mixtures for mapping of proteinase specificities
Methods in enzymology on CD-ROM/Methods in enzymology·1995· 7 cited
ChemInform Abstract: 6‐Azasteroids: Structure‐Activity Relationships for Inhibition of Type 1 and 2 Human 5α‐Reductase and Human Adrenal 3β‐Hydroxy‐. delta.5‐steroid Dehydrogenase/3‐Keto‐δ5‐steroid Isomerase.
ChemInform·1994· 7 cited
Characterization of the peptide substrate specificities of interstitial collagenase and 92-kDa gelatinase. Implications for substrate optimization
Journal of Biological Chemistry·1994· 55 citedOpen Access
A High Throughput Fluorogenic Substrate for Stromelysin (MMP‐3)
Annals of the New York Academy of Sciences·1994· 13 cited
ChemInform Abstract: 6‐Azasteroids: Potent Dual Inhibitors of Human Type 1 and 2 Steroid 5. alpha.‐Reductase.
ChemInform·1994· 5 cited
Matrix metalloproteinase inhibitors containing a [(carboxyalkyl)amino] zinc ligand: Modification of the P1 and P2' residues. [Erratum to document cited in CA120:238898]
Journal of Medicinal Chemistry·1994
Matrix Metalloproteinase Inhibitors Containing a [(Carboxyalkyl)amino]zinc Ligand: Modification of the P1 and P2' Residues
Journal of Medicinal Chemistry·1994· 46 citedOpen Access
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Frequent Co-authors

Marcia L. Moss(11), J. David Becherer(7), Gerard M. McGeehan(6), Judd Berman(5), Robert Andrews(5), Millard H. Lambert(4), Marcos E. Milla(4), Janet Warner(4), James G. Conway(4), M. Anthony Leesnitzer(4), Stephen V. Frye(4), Curt D. Haffner(4), Patrick Maloney(4), Timothy K. Tippin(4), Justin Mitchell(3), Gregory Pahel(3), Theresa Seaton(3), Peter J. Brown(3), Michael H. Rabinowitz(3), David J. Cowan(3)