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Joel Desharnais

Explore the profile of Joel Desharnais including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 14
Citations 345
Followers 0
Related Specialties
Biochemistry
Chemistry
Science
Top 10 Co-Authors
Dale L Boger
Yan Zhang
Ian A Wilson
Stephen J Benkovic
Ali Tavassoli
Michael P Hedrick
Thomas H Marsilje
Kevin Capps
Gary Woodnutt
Angelo J Castellino
Published In
Bioorg Med Chem
Biochemistry
Proc Natl Acad Sci U S A
Bioorg Med Chem Lett
J Am Chem Soc
Affiliations
Soon will be listed here.
Recent Articles
1.
Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide
Liu S, Desharnais J, Sahasrabudhe P, Jin P, Li W, Oates B, et al.
Sci Rep . 2016 May; 6:26071. PMID: 27184415
IL-17A is a pro-inflammatory cytokine that has been implicated in autoimmune and inflammatory diseases. Monoclonal antibodies inhibiting IL-17A signaling have demonstrated remarkable efficacy, but an oral therapy is still lacking....
2.
Pyroglutamate and O-linked glycan determine functional production of anti-IL17A and anti-IL22 peptide-antibody bispecific genetic fusions
Zhong X, Kieras E, Sousa E, DAntona A, Baber J, He T, et al.
J Biol Chem . 2012 Nov; 288(2):1409-19. PMID: 23184956
Protein biosynthesis and extracellular secretion are essential biological processes for therapeutic protein production in mammalian cells, which offer the capacity for correct folding and proper post-translational modifications. In this study,...
3.
Chemical generation of bispecific antibodies
Doppalapudi V, Huang J, Liu D, Jin P, Liu B, Li L, et al.
Proc Natl Acad Sci U S A . 2010 Dec; 107(52):22611-6. PMID: 21149738
Bispecific antibodies (BsAbs) are regarded as promising therapeutic agents due to their ability to simultaneously bind two different antigens. Several bispecific modalities have been developed, but their utility is limited...
4.
Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells
Aspland S, Ballatore C, Castillo R, Desharnais J, Eustaquio T, Goelet P, et al.
Bioorg Med Chem Lett . 2006 Jul; 16(19):5194-8. PMID: 16870428
In the present work, we explore the possibility of introducing selectivity to existing chemotherapeutics via the design of non-pro-drug, bi-functional molecules comprising a microtubule-binding agent and a substrate for a...
5.
A facile route to paclitaxel C-10 carbamates
Ballatore C, Aspland S, Castillo R, Desharnais J, Eustaquio T, Sun C, et al.
Bioorg Med Chem Lett . 2005 May; 15(10):2477-80. PMID: 15863300
A general protocol for the synthesis of paclitaxel C-10 carbamates is described. The method entails MeI-mediated activation of 2'-O-TBS-7-O-TES-10-O-deacetyl-paclitaxel-10-O-carbonylimidazole prior to reaction with amines. This method is effective for the...
6.
Solution-phase combinatorial libraries: modulating cellular signaling by targeting protein-protein or protein-DNA interactions
Boger D, Desharnais J, Capps K
Angew Chem Int Ed Engl . 2003 Sep; 42(35):4138-76. PMID: 14502729
The high-throughput synthesis and screening of compound libraries hold tremendous promise for drug discovery and powerful methods for both solid-phase and solution-phase library preparation have been introduced. The question of...
7.
Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway
Desharnais J, Hwang I, Zhang Y, Tavassoli A, Baboval J, Benkovic S, et al.
Bioorg Med Chem . 2003 Sep; 11(20):4511-21. PMID: 13129587
The synthesis and evaluation of analogues and key derivatives of 10-CF3CO-DDACTHF as inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Polyglutamate analogues of...
8.
10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase
Marsilje T, Hedrick M, Desharnais J, Capps K, Tavassoli A, Zhang Y, et al.
Bioorg Med Chem . 2003 Sep; 11(20):4503-9. PMID: 13129586
The design and synthesis of 10-(2-benzoxazolcarbonyl)-DDACTHF (1) as an inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Ketone 1 and the corresponding alcohol...
9.
Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase
Marsilje T, Hedrick M, Desharnais J, Tavassoli A, Zhang Y, Wilson I, et al.
Bioorg Med Chem . 2003 Sep; 11(20):4487-501. PMID: 13129585
A series of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues lacking the benzoylglutamate subunit were prepared and examined as potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase)...
10.
Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
Zhang Y, Desharnais J, Marsilje T, Li C, Hedrick M, Gooljarsingh L, et al.
Biochemistry . 2003 May; 42(20):6043-56. PMID: 12755606
Glycinamide ribonucleotide transformylase (GAR Tfase) has been the target of anti-neoplastic intervention for almost two decades. Here, we use a structure-based approach to design a novel folate analogue, 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid...