Drug Discovery and Development Lab

 

Focus

Conduct research to identify new drug candidates that are safe and effective for people with cancer or who are at high risk of developing cancer. The Cancer Drug Discovery and Development Center is developing novel compounds that are especially effective for colon, lung, breast and pancreatic tumors having abnormal levels of the Ras oncogene (shown at right).

 


piazza lab 847 2016.jpgFaculty and staff

Gary A. Piazza, Ph.D.: Lab chief and Professor of Oncologic Sciences and Pharmacology
Adam B. Keeton, Ph.D.: Research Assistant Professor, screening, assay development, signal transduction, cell biology, Ras project and colon cancer
Xi Chen, Ph.D.: Research Assistant Professor, medicinal chemist
Jacob Vallyaveettil, Ph.D.: Research Assistant Professor, medicinal chemist
Bing Zhu, Ph.D.: Research Assistant Professor, biochemistry, lung cancer, Ras project
Verónica Ramirez-Alcántara, Ph.D.: Research Assistant Professor, pharmacology, toxicology, mouse model development, drug formulation
Bernard Gary: Staff, cell culture and in vitro evaluation of experimental compounds
Kristy Berry: Staff, in vivo evaluation of experimental compounds in mouse tumor models
Kevin Lee, Ph.D.: Postdoc, phosphodiesterase 10A, colon cancer
Ashley Lindsey, Ph.D.: Postdoc, lung cancer, mouse model tumors
Mary Kate Saville: Graduate student
Tyler Maddox: Graduate student

 

Ras oncoprotein resized.jpgAccomplishments

Identification of a clinical candidate, Ras inhibitor (DC070-547)

  • Highly potent and selective compound that inhibits the growth tumor cells with activated Ras relative to cells lacking activated Ras
  • Strong anti-tumor activity in a mutant K-Ras  tumor mouse xenograft model
  • Appears to non-covalently  bind Ras to inhibit Raf/Mek/Erk signaling
  • Low probability of off-target binding
  • Non-peptidic, stable, small molecule comprising an indene core structure
  • Favorable physicochemical properties meeting “Lipinski” criteria for drug-like properties
  • Readily synthesized, modified, and scaled

 

Core Labs

High Throughput Screening Lab

 

Funding

Current:

  • NCI,R01CA131378-07 (Piazza) Novel sulindac derivatives for colon cancer chemoprevention
  • NCI,R01CA148817-05 (Piazza) Development of a novel sulindac amide for colorectal cancer
  • NCI,R01CA155638-04 (Piazza) PDE5, a novel target and inhibitor for breast cancer
  • NCI,R01CA155638-04W1 (Piazza) Diversity supplement for Luciana Barnes -- ovarian cancer
  • NCI,R21CA182941-01 (Piazza and Zhu) PDE inhibition by sulindac derivatives for lung cancer
  • NCI,R43CA189613-01 (Piazza and Canzoneri) Novel PDE target and inhibitors for lung cancer
  • Austin Lacey Family (Piazza) lung cancer-related research

To be funded:

  • NCIR01CA197147A1 (Piazza) PDE10A, a novel target for lung cancer chemoprevention
  • NCIR43CA206807-01A1 (Piazza and Canzoneri) Novel Ras inhibitor pro-drug for colorectal cancer

Completed:

  • NCI,R01CA131378-01-06 (Piazza) Novel sulindac derivatives for colon cancer chemoprevention, subcontract
  • NCI,R01CA155638-04 (Piazza) PDE5, a novel target and inhibitor for breast cancer, supplement
  • NCI,R01CA148817-05 (Piazza) Development of a novel sulindac amide for colorectal cancer, supplement
  • UAB (Sorscher) CF Foundation
  • HTS Service facility

Pending:

  • Diversity career development supplement for Verónica Ramirez-Alcántara

 

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