Dr. Sevgi B. Rodan

Throughout their productive careers, Dr. Sevgi B. Rodan and her
late husband and frequent collaboator, Dr. Gideon A. Rodan, have made
outstanding contributions to the field of bone biology, including: the
isolation and characterization of the first transformed osteoblastic
cell line (ROS 17/2.8), the unraveling of the PTH signal transduction
mechanisms, the development of the concept of osteoblast-osteoclast
interaction, the identification and characterization of integrin
antagonists as osteoclast inhibitors, the development of the
blockbuster drug Alendronate (Fosamax), and the cloning of alkaline
phosphatase. Both scientists worked for many years in the Department of
Bone Biology and Osteoporosis Research at Merck & Company, and both
have been leaders in several bone-related organizations. (adapted
from The International Bone & Mineral Society announcement of The
Gideon and Sevgi Rodan IBMS Fellowship)
Recent Publications
- Zartman AE, Duong le T, Fernandez-Metzler C,
Hartman GD, Leu CT, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME, Meissner RS
2005 Nonpeptide alpha(v)beta3 antagonists: identification of potent,
chain-shortened 7-oxo RGD mimetics. Bioorg Med Chem Lett 15(6):1647-50.
- Whitman DB, Askew BC, Duong le T, Fernandez-Metzler C,
Halczenko W, Hartman GD, Hutchinson JH, Leu CT, Prueksaritanont T,
Rodan GA, Rodan SB, Duggan ME
2004 Nonpeptide alpha V beta 3 antagonists. Part 9: Improved
pharmacokinetic profile through the use of an aliphatic, des-amide
backbone. Bioorg Med Chem Lett 14(17):4411-5.
- Wang J, Breslin MJ, Coleman PJ, Duggan ME, Hunt CA,
Hutchinson JH, Leu CT, Rodan SB,
Rodan GA, Duong le T, Hartman GD 2004 Non-peptide alpha v beta 3
antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine
derivatives. Bioorg Med Chem Lett 14(4):1049-52.
- Robichaud J, Bayly C, Oballa R, Prasit P, Mellon C,
Falgueyret JP, Percival MD, Wesolowski G, Rodan SB 2004 Rational design of
potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.
Bioorg Med Chem Lett 14(16):4291-5.
- Prueksaritanont T, Fernandez-Metzler C, Meng Y, Barrish A,
Halczenko W, Rodan SB,
Hutchinson JH, Duggan ME, Lin JH 2004 Disposition of a novel and potent
alpha(v)beta3 antagonist in animals, and extrapolation to man.
Xenobiotica 34(1):103-15.
- Falgueyret JP, Black WC, Cromlish W, Desmarais S, Lamontagne
S, Mellon C, Riendeau D, Rodan S,
Tawa P, Wesolowski G, Bass KE, Venkatraman S, Percival MD 2004 An
activity-based probe for the determination of cysteine cathepsin
protease activities in whole cells. Anal Biochem 335(2):218-27.
- Coleman PJ, Brashear KM, Askew BC, Hutchinson JH, McVean CA,
Duong le T, Feuston BP, Fernandez-Metzler C, Gentile MA, Hartman GD,
Kimmel DB, Leu CT, Lipfert L, Merkle K, Pennypacker B, Prueksaritanont
T, Rodan GA, Wesolowski GA, Rodan SB,
Duggan ME 2004 Nonpeptide alphavbeta3 antagonists. Part 11: discovery
and preclinical evaluation of potent alphavbeta3 antagonists for the
prevention and treatment of osteoporosis. J Med Chem 47(20):4829-37.
- Breslin MJ, Duggan ME, Halczenko W, Hartman GD, Duong le T,
Fernandez-Metzler C, Gentile MA, Kimmel DB, Leu CT, Merkle K,
Prueksaritanont T, Rodan GA, Rodan SB,
Hutchinson JH 2004 Nonpeptide alpha V beta 3 antagonists. Part 10: In
vitro and in vivo evaluation of a potent 7-methyl substituted
tetrahydro-[1,8]naphthyridine derivative. Bioorg Med Chem Lett
14(17):4515-8.
- Robichaud J, Oballa R, Prasit P, Falgueyret JP, Percival MD,
Wesolowski G, Rodan SB, Kimmel
D, Johnson C, Bryant C, Venkatraman S, Setti E, Mendonca R, Palmer JT
2003 A novel class of nonpeptidic biaryl inhibitors of human cathepsin
K. J Med Chem 46(17):3709-27.
- Perkins JJ, Duong LT, Fernandez-Metzler C, Hartman GD,
Kimmel DB, Leu CT, Lynch JJ, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME, Meissner RS
2003 Non-peptide alpha(v)beta(3) antagonists: identification of potent,
chain-shortened RGD mimetics that incorporate a central pyrrolidinone
constraint. Bioorg Med Chem Lett 13(24):4285-8.
- Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman
PJ, Duong le T, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD,
Huff JR, Kimmel DB, Leu CT, Meissner RS, Merkle K, Nagy R, Pennypacker
B, Perkins JJ, Prueksaritanont T, Rodan GA, Varga SL, Wesolowski GA,
Zartman AE, Rodan SB, Duggan
ME 2003 Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo
evaluation of a potent alphavbeta3 antagonist for the prevention and
treatment of osteoporosis. J Med Chem 46(22):4790-8.
- Breslin MJ, Duggan ME, Halczenko W, Fernandez-Metzler C,
Hunt CA, Leu CT, Merkle KM, Naylor-Olsen AM, Prueksaritanont T, Stump
G, Wallace A, Rodan SB,
Hutchinson JH 2003 Non-peptide alphavbeta3 antagonists. Part 6: design
and synthesis of alphavbeta3 antagonists containing a pyridone or
pyrazinone central scaffold. Bioorg Med Chem Lett 13(10):1809-12.
- Rydzewski RM, Bryant C, Oballa R, Wesolowski G, Rodan SB, Bass KE, Wong DH 2002
Peptidic 1-cyanopyrrolidines: synthesis and SAR of a series of potent,
selective cathepsin inhibitors. Bioorg Med Chem 10(10):3277-84.
- Meissner RS, Perkins JJ, Duong le T, Hartman GD, Hoffman WF,
Huff JR, Ihle NC, Leu CT, Nagy RM, Naylor-Olsen A, Rodan GA, Rodan SB, Whitman DB, Wesolowski GA,
Duggan ME 2002 Nonpeptide alpha(v)beta(3) antagonists. Part 2:
constrained glycyl amides derived from the RGD tripeptide. Bioorg Med
Chem Lett 12(1):25-9.
- Feuston BP, Culberson JC, Duggan ME, Hartman GD, Leu CT, Rodan SB 2002 Binding model for
nonpeptide antagonists of alpha(v)beta(3) integrin. J Med Chem
45(26):5640-8.
- Coleman PJ, Brashear KM, Hunt CA, Hoffman WF, Hutchinson JH,
Breslin MJ, McVean CA, Askew BC, Hartman GD, Rodan SB, Rodan GA, Leu CT,
Prueksaritanont T, Fernandez-Metzler C, Ma B, Libby LA, Merkle KM,
Stump GL, Wallace AA, Lynch JJ, Lynch R, Duggan ME 2002 Non-peptide
alpha(v)beta(3) antagonists. Part 3: identification of potent RGD
mimetics incorporating novel beta-amino acids as aspartic acid
replacements. Bioorg Med Chem Lett 12(1):31-4.
- Coleman PJ, Askew BC, Hutchinson JH, Whitman DB, Perkins JJ,
Hartman GD, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C,
Merkle KM, Lynch R, Lynch JJ, Rodan SB,
Duggan ME 2002 Non-peptide alpha(v)beta(3) antagonists. Part 4: potent
and orally bioavailable chain-shortened RGD mimetics. Bioorg Med Chem
Lett 12(17):2463-5.
- Brashear KM, Hunt CA, Kucer BT, Duggan ME, Hartman GD, Rodan
GA, Rodan SB, Leu CT,
Prueksaritanont T, Fernandez-Metzler C, Barrish A, Homnick CF,
Hutchinson JH, Coleman PJ 2002 Non-peptide alpha(v)beta(3) antagonists.
Part 5: identification of potent RGD mimetics incorporating 2-aryl
beta-amino acids as aspartic acid replacements. Bioorg Med Chem Lett
12(23):3483-6.
- Machwate M, Harada S, Leu CT, Seedor G, Labelle M, Gallant
M, Hutchins S, Lachance N, Sawyer N, Slipetz D, Metters KM, Rodan SB, Young R, Rodan GA 2001
Prostaglandin receptor EP(4) mediates the bone anabolic effects of
PGE(2). Mol Pharmacol 60(1):36-41.
- Falgueyret JP, Oballa RM, Okamoto O, Wesolowski G, Aubin Y,
Rydzewski RM, Prasit P, Riendeau D, Rodan
SB, Percival MD 2001 Novel, nonpeptidic cyanamides as potent and
reversible inhibitors of human cathepsins K and L. J Med Chem
44(1):94-104.
- Duggan ME, Duong LT, Fisher JE, Hamill TG, Hoffman WF, Huff
JR, Ihle NC, Leu CT, Nagy RM, Perkins JJ, Rodan SB, Wesolowski G, Whitman DB,
Zartman AE, Rodan GA, Hartman GD 2000 Nonpeptide alpha(v)beta(3)
antagonists. 1. Transformation of a potent, integrin-selective
alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.
J Med Chem 43(20):3736-45.