Staff Profile: Ganesha Rai

Ganesha Rai, Ph.D.

Research Scientist/Chemist

Division of Preclinical Innovation
Chemistry Technologies

National Center for Advancing Translational Sciences

National Institutes of Health

Email Ganesha Rai


Ganesha Rai is a research scientist/chemist in the Chemistry Technology program within NCATS’ Division of Preclinical Innovation, where — on a team led by Juan Marugan, Ph.D. — he develops small molecule tools for many disease-relevant biological targets.

Prior to joining NIH in 2006 as a postdoctoral fellow, Rai conducted postdoctoral research at Seoul National University, where he designed small molecules capable of detecting beta-amyloid plaques in the early stages of Alzheimer's disease.

Rai earned his Master of Science and doctorate in organic chemistry from Mangalore University in India.

Research Topics

Rai’s research focuses on developing small molecule tools to modulate biological targets and validating these targets as potential therapeutic opportunities for various diseases, including rare and neglected illnesses. Rai advances validated hits into attractive chemical leads and, when possible, eventually into therapeutics. Rai has optimized first-in-class small molecule inhibitors for disease-relevant enzymes, such as 12-lipoxygenase, 15-lipoxygenase, Ape1, the epigenetic target JMJD2 and the novel antibacterial target PPTase. Discovery of these well-characterized drug-like molecules has enabled Rai to interrogate these enzymes as novel therapeutic targets. Rai has developed probes in the following areas:

  • Cancer (LDHA, Ape1, FOXM1, NOX2)
  • Epigenetics ( JMJD2A-E, JARID)
  • Diabetes and stroke (12-LO, 15-LO)
  • Infectious diseases/agents (schistosomiasis, malaria, hookworm and antibacterials)

Selected Publications

  1. Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies
  2. 4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth
  3. Targeting the JMJD2 histone demethylases to epigenetically control herpesvirus infection and reactivation from latency
  4. Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors
  5. Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase