Richard B Hochberg PhD

Professor of Obstetrics, Gynecology, and Reproductive Sciences

Research Interests

Steroid biochemistry; Steroid receptors; Synthesis of estrogens; locally active estrogens; SERMs; Radiochemistry; Estrogens and Androgens labeled with high energy isotopes

Current Projects

1. SPECT imaging the estrogen and androgen responsive regions of the primate brain
2. Developing SERMs that do not act on the brain and cause hot flashes.
3. Develop locally active antiandrogens for the treatment of skin

Research Summary

Studies of hormone action, detection of tumors with steroid hormones labeled with radioactive tags, imaging the hormone responsive regions of the brain, and synthesis of unique estrogens for treatment of menopausal symptoms. Studies of an unusual family of the fatty acid esters of steroids.

Extensive Research Description

Dr Hochberg was trained in the field of steroid chemistry and biochemistry in the laboratory of the renowned Dr Seymour Lieberman where he investigated the unique biosynthetic pathways involving steroid sulfates as intermediates, as well as the mechanisms in steroid biosynthetic pathway.

Subsequently, he discovered the previously unknown “lipoidal derivatives”, fatty acid esters of the steroids which included the estrogens and androgens, the most potent of the naturally occurring steroid hormones. He designed and synthesized the first steroid hormones labeled with high energy isotopes: the estrogen, 16a-iodoestradiol (and the 11ß-methoxy analog) which when labeled with 123I was used for detecting breast cancer metastases and with 125I for unique neuroendocrine studies of the estrogen responsive regions of the brain; an androgen, 7a-fluoro-DHT designed to detect prostate metastases by androgen receptor mediated uptake when labeled with 18F.

He developed the first in vitro bioassay for estrogens a procedure that is still currently used for the accurate determinations of estrogenic potency applicable to humans. He has also synthesized “local estrogens” for the treatment of menopausal dyspareunia, compounds that are devoid of systemic action and unique SERMs

Selected Publications

  • Zhang J, Labaree DC, Mor G, Hochberg RB 2004 Estrogen to Antiestrogen with a Single Methylene Group Resulting in an Unusual Steroidal SERM. J Clin Endocrinol Metab 89:3527-3535
  • Labaree DC, Zhang J, Harris HA, O'Connor C, Reynolds TY, Hochberg RB 2003 The Synthesis and Evaluation of B-, C-, and D-ring Substituted Estradiol Carboxylic Acid Esters as Locally Active Estrogens. J Med Chem 46:1886-1904
  • Labaree DC, Hoyte RM, Nazareth LV, Weigel NL, Hochberg RB 1999 7a-iodo and fluoro steroids as androgen receptor mediated imaging agents. J Med Chem 42:2021-2034
  • Toran-Allerand CD, Miranda RC, Bentham WDL, Sohrabji F, Brown TJ, Hochberg RB, MacLusky NJ 1992 Estrogen receptors colocalize with low-affinity nerve growth factor receptors in cholinergic neurons of the basal forebrain. Proc Natl Acad Sci USA 89:4668-4672
  • Mellon-Nussbaum S, Ponticorvo L, Schatz F, Hochberg RB 1982 Estradiol fatty acid esters: The isolation and identification of the lipoidal derivative of estradiol synthesized in the bovine uterus. J Biol Chem 257:5678-5684
  • Borg W, Shackleton CHL, Pahuja SL, Hochberg RB 1995 Endogenous Long-Lived Esters of Testosterone in the Rat. Proc Natl Acad Sci USA 92:1545-1549
  • Littlefield BA, Gurpide E, Markiewicz L, McKinley B, Hochberg RB 1990 A simple and sensitive microtiter plate estrogen bioassay based on stimulation of alkaline phosphatase in Ishikawa cells: Estrogenic action of D5 adrenal steroids. Endocrinology 127:2757-2762
  • Zielinski JE, Larner JM, Hoffer PB, Hochberg RB 1989 The synthesis of 11b-methoxy-[16a-123I]iodoestradiol and its interaction with the estrogen receptor in vivo and in vitro. J Nucl Med 30:209-215

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