Bibliography


  1. Croston GE. The utility of target-based discovery. Expert Opin Drug Discov. 2017 May;12(5):427-429. doi: 10.1080/17460441.2017.1308351. Epub 2017 Mar 23. PubMed PMID: 28306350.
  2. Wiśniewski K, Sueiras-Diaz J, Jiang G, Galyean R, Lu M, Thompson D, Wang YC, Croston G, Posch A, Hargrove DM, Wiśniewska H, Laporte R, Dwyer JJ, Qi S, Srinivasan K, Hartwig J, Ferdyan N, Mares M, Kraus J, Alagarsamy S, Rivière PJ, Schteingart CD. Synthesis and Pharmacological Characterization of Novel Glucagon-like Peptide-2 (GLP-2) Analogues with Low Systemic Clearance. J Med Chem. 2016 Apr 14;59(7):3129-39. doi: 10.1021/acs.jmedchem.5b01909. Epub 2016 Mar 25. PubMed PMID: 26986178.
  3. Wiśniewski K, Alagarsamy S, Galyean R, Tariga H, Thompson D, Ly B, Wiśniewska H, Qi S, Croston G, Laporte R, Rivière PJ, Schteingart CD. New, potent, and selective peptidic oxytocin receptor agonists. J Med Chem. 2014 Jun 26;57(12):5306-17. doi: 10.1021/jm500365s. Epub 2014 Jun 12. PubMed PMID: 24874785.
  4. Wisniewski K, Galyean R, Tariga H, Alagarsamy S, Croston G, Heitzmann J, Kohan A, Wisniewska H, Laporte R, Rivière PJ, Schteingart CD. New, potent, selective, and short-acting peptidic V1a receptor agonists. J Med Chem. 2011 Jul 14;54(13):4388-98. doi: 10.1021/jm200278m. Epub 2011 Jun 20. PubMed PMID: 21688787.
  5. Laporte R, Kohan A, Heitzmann J, Wisniewska H, Toy J, La E, Tariga H, Alagarsamy S, Ly B, Dykert J, Qi S, Wisniewski K, Galyean R, Croston G, Schteingart CD, Rivière PJ. Pharmacological characterization of FE 202158, a novel, potent, selective, and short-acting peptidic vasopressin V1a receptor full agonist for the treatment of vasodilatory hypotension. J Pharmacol Exp Ther. 2011 Jun;337(3):786-96. doi: 10.1124/jpet.111.178848. Epub 2011 Mar 16. PubMed PMID: 21411496.
  6. Wisniewski K, Galyean R, Taki H, Alagarsamy S, Croston G, Laporte R, Schteingart CD, Rivière PJ. Synthesis and in vitro pharmacological profile of potent and selective peptidic V1a receptor agonists. Adv Exp Med Biol. 2009;611:507-8. PubMed PMID: 19400287.
  7. Samant MP, White R, Hong DJ, Croston G, Conn PM, Janovick JA, Rivier J. Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives. J Med Chem. 2007 May 3;50(9):2067-77. Epub 2007 Apr 3. PubMed PMID: 17402723; PubMed Central PMCID: PMC2536683.
  8. Samant MP, Hong DJ, Croston G, Rivier C, Rivier J. Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III. J Med Chem. 2006 Jun 15;49(12):3536-43. PubMed PMID: 16759096; PubMed Central PMCID: PMC2536684.
  9. Piu F, Gauthier NK, Olsson R, Currier EA, Lund BW, Croston GE, Hacksell U, Brann MR. Identification of novel subtype selective RAR agonists. Biochem Pharmacol. 2005 Dec 19;71(1-2):156-62. Epub 2005 Nov 21. PubMed PMID: 16303118.
  10. Samant MP, Gulyas J, Hong DJ, Croston G, Rivier C, Rivier J. Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II. J Med Chem. 2005 Jul 28;48(15):4851-60. PubMed PMID: 16033265; PubMed Central PMCID: PMC2593149.
  11. Samant MP, Gulyas J, Hong DJ, Croston G, Rivier C, Rivier J. Synthesis, in vivo and in vitro biological activity of novel azaline B analogs. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2894-7. PubMed PMID: 15911275.
  12. Samant MP, Miller C, Hong DJ, Koerber SC, Croston G, Rivier CL, Rivier JE. Synthesis and biological activity of GnRH antagonists modified at position 3 with 3-(2-methoxy-5-pyridyl)-alanine. J Pept Res. 2005 Feb;65(2):284-91. PubMed PMID: 15705170.
  13. Samant MP, Hong DJ, Croston G, Rivier C, Rivier J. Novel gonadotropin-releasing hormone antagonists with substitutions at position 5. Biopolymers. 2005;80(2-3):386-91. PubMed PMID: 15614806.
  14. Farmer LJ, Zhi L, Jeong S, Lamph WW, Osburn DL, Croston G, Flatten KS, Heyman RA, Nadzan AM. Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid. Bioorg Med Chem Lett. 2003 Jan 20;13(2):261-4. PubMed PMID: 12482435.
  15. Croston GE, Olsson R, Currier EA, Burstein ES, Weiner D, Nash N, Severance D, Allenmark SG, Thunberg L, Ma JN, Mohell N, O'Dowd B, Brann MR, Hacksell U. Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954). J Med Chem. 2002 Nov 7;45(23):4950-3. PubMed PMID: 12408704.
  16. Croston GE. Functional cell-based uHTS in chemical genomic drug discovery. Trends Biotechnol. 2002 Mar;20(3):110-5. Review. PubMed PMID: 11841862.
  17. Hacksell U, Nash N, Burstein ES, Piu F, Croston G, Brann MR. Chemical genomics: massively parallel technologies for rapid lead identification and target validation. Cytotechnology. 2002 Jan;38(1-3):3-10. doi: 10.1023/A:1021169023731. PubMed PMID: 19003080; PubMed Central PMCID: PMC3449916.
  18. Weiner DM, Burstein ES, Nash N, Croston GE, Currier EA, Vanover KE, Harvey SC, Donohue E, Hansen HC, Andersson CM, Spalding TA, Gibson DF, Krebs-Thomson K, Powell SB, Geyer MA, Hacksell U, Brann MR. 5-hydroxytryptamine2A receptor inverse agonists as antipsychotics. J Pharmacol Exp Ther. 2001 Oct;299(1):268-76. PubMed PMID: 11561089.
  19. Hansen HC, Olsson R, Croston G, Andersson CM. Multistep solution-phase parallel synthesis of spiperone analogues. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2435-9. PubMed PMID: 11078195.
  20. Mukherjee R, Hoener PA, Jow L, Bilakovics J, Klausing K, Mais DE, Faulkner A, Croston GE, Paterniti JR Jr. A selective peroxisome proliferator-activated receptor-gamma (PPARgamma) modulator blocks adipocyte differentiation but stimulates glucose uptake in 3T3-L1 adipocytes. Mol Endocrinol. 2000 Sep;14(9):1425-33. PubMed PMID: 10976920.
  21. Canan Koch SS, Dardashti LJ, Cesario RM, Croston GE, Boehm MF, Heyman RA, Nadzan AM. Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells. J Med Chem. 1999 Feb 25;42(4):742-50. PubMed PMID: 10052980.
  22. Croston GE, Milan LB, Marschke KB, Reichman M, Briggs MR. Androgen receptor-mediated antagonism of estrogen-dependent low density lipoprotein receptor transcription in cultured hepatocytes. Endocrinology. 1997 Sep;138(9):3779-86. PubMed PMID: 9275065.
  23. Mukherjee R, Jow L, Croston GE, Paterniti JR Jr. Identification, characterization, and tissue distribution of human peroxisome proliferator-activated receptor (PPAR) isoforms PPARgamma2 versus PPARgamma1 and activation with retinoid X receptor agonists and antagonists. J Biol Chem. 1997 Mar 21;272(12):8071-6. PubMed PMID: 9065481.
  24. Lala DS, Mukherjee R, Schulman IG, Koch SS, Dardashti LJ, Nadzan AM, Croston GE, Evans RM, Heyman RA. Activation of specific RXR heterodimers by an antagonist of RXR homodimers. Nature. 1996 Oct 3;383(6599):450-3. PubMed PMID: 8837780.
  25. Canan Koch SS, Dardashti LJ, Hebert JJ, White SK, Croston GE, Flatten KS, Heyman RA, Nadzan AM. Identification of the first retinoid X, receptor homodimer antagonist. J Med Chem. 1996 Aug 16;39(17):3229-34. PubMed PMID: 8765503.
  26. Zhang L, Nadzan AM, Heyman RA, Love DL, Mais DE, Croston G, Lamph WW, Boehm MF. Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells. J Med Chem. 1996 Jul 5;39(14):2659-63. PubMed PMID: 8709094.
  27. Croston GE, Cao Z, Goeddel DV. NF-kappa B activation by interleukin-1 (IL-1) requires an IL-1 receptor-associated protein kinase activity. J Biol Chem. 1995 Jul 14;270(28):16514-7. PubMed PMID: 7622454.
  28. Croston GE, Kadonaga JT. Role of chromatin structure in the regulation of transcription by RNA polymerase II. Curr Opin Cell Biol. 1993 Jun;5(3):417-23. Review. PubMed PMID: 8352958.
  29. Croston GE, Laybourn PJ, Paranjape SM, Kadonaga JT. Mechanism of transcriptional antirepression by GAL4-VP16. Genes Dev. 1992 Dec;6(12A):2270-81. PubMed PMID: 1459451.
  30. Croston GE, Lira LM, Kadonaga JT. A general method for purification of H1 histones that are active for repression of basal RNA polymerase II transcription. Protein Expr Purif. 1991 Apr-Jun;2(2-3):162-9. PubMed PMID: 1821786.
  31. Croston GE, Kerrigan LA, Lira LM, Marshak DR, Kadonaga JT. Sequence-specific antirepression of histone H1-mediated inhibition of basal RNA polymerase II transcription. Science. 1991 Feb 8;251(4994):643-9. PubMed PMID: 1899487.


 

Glenn Croston - Principal Consultant


Summary of Qualifications

  • Track record of drug discovery success at startup, small and mid-sized pharma companies
  • Advanced eight clinical candidates in ten years
  • Proven scientific innovator (published in Science, Nature, Genes and Development)
  • Strong network of collaborators throughout biotech and pharma
  • Broad skill set spanning the full range of preclinical drug discovery

Croston Consulting

Excellence in Drug Discovery

Professional Experience


CROSTON CONSULTING, San Diego CA

Principal Consultant

Pharmaceutical research and development consulting across a broad range of therapeutic areas, including gastroenterology, urology, oncology, CNS, reproductive health, endocrinology, cardiovascular, metabolic disease, sepsis, pain, liver disease, and more.  Services provided include therapeutic area strategy, business development, due diligence, grant writing, literature preparation, literature review, and startup consulting.  


FERRING RESEARCH INSTITUTE, San Diego, CA                                                
Director/Senior Director of Drug Discovery Pharmacology
Built and led pharmacology team delivering lead optimization, target validation, biomarkers, and translational pharmacology using in vitro, ex vivo, and in vivo models. Therapeutic areas included gastroenterology, inflammatory bowel disease, prostate cancer, bladder cancer, reproductive health, urology, sepsis, pain, and novel molecular targets, from hypothesis to clinical candidate, with a focus on peptide and protein-based therapeutics. Developed strategic research plans as a member of senior management team.  Delivered translational pharmacology to advance eight clinical candidates in ten years, including ground breaking work in pain (now in Phase 3), sepsis (now in Phase 3), and hepatology (Phase 1).

ACADIA PHARMACEUTICALS, San Diego, CA                                                      
Group Leader
Developed all systems for chemical genomics to identify target-selective hits and leads, validate targets and perform lead optimization.  Optimized capabilities with cell-based functional assays for GPCRs, cytokine receptors, nuclear receptors, and protein kinases. Therapeutic areas included schizophrenia, cardiovascular disease, glaucoma, pain, cancer, and obesity.  Contributed to Pimavanserin discovery, NDA filed 2015.

LIGAND PHARMACEUTICALS, San Diego, CA

Senior Research Scientist                                                      
Delivered lead discovery, lead optimization, and molecular pharmacology in oncology, metabolic disease and cardiovascular disease.  Research with Rich Heymans' group published in Nature.

TULARIK, INCORPORATED, South San Francisco, CA                                        
Postdoctoral Researcher
Research with biotech pioneer Dr. Dave Goeddel (first non-academic scientist at Genentech) identified a novel IL-1 receptor associated kinase (IRAK) coupled to NF-kB activation as a potential target in the development of anti-inflammatory drugs.

UC SAN DIEGO, San Diego, CA                                                                                  
Ph.D. Graduate Research
Working with Dr. Jim Kadonaga, discovered role of histone H1 as a key component in the regulation of gene expression in cell free systems.  My graduate thesis was awarded the Kamen prize as outstanding thesis in the UCSD Department of Biology.  Thesis research included first author publication in Science, Genes and Development