View
166
Download
0
Category
Preview:
Citation preview
What are theranostics?
MRI PET/SPECT Chemotherapy
Photodynamic
Gene Therapy
Radiation
Therapeutic
HyperthermiaNIR Fluorescence
Diagnostic + Theranostic =
Details published by Sneha S. Kelkar and Theresa M.Reineke1
Theranostics allows design of ‘compound drugs’ with multiple functionalities,
which may aid doctors to diagnose patients more effectively, rapidly and lead to
personalised medicine. Other advantages may include but are not limited to:
Overcoming drug resistance2
Improved relaxivity of imaging agents (hence improved imaging)
Specific targeting to target site (hence reduced toxicity)
Varying linker/spacer groups (unexpected activity? cost?)
Why theranostics?
Ultimate aim of projectSpacer – can use
various functionalities
to link molecules, e.g.
esters via. cyclic
anhydrides
MRI
contrasting
agent
derivative –
DOTA based
(DOTA-GA),
link via. cyclic
anhydride
spacer to
form ester
Therapeutic agent – cisplatin
derivative (oxoplatin). Pt(IV)
based
Targeting group -
RGD tripeptide
(L-Asp-Gly-L-Arg)3
Which molecules did this project aim to
make and why?
12
Retrosynthetic analysis – disconnection approach
What was achieved?
Before I started practical work:
Synthetic routes designed – Combination of research and retrosynthetic
analysis
Verification/changes
Project plan considering realistic time available
COSSH form assessments for all practical work
Ethical form assessments
Chemicals stock check and order forms completed
Background reading
Introduction to lab and cleaning
What was achieved?
After practical work had started:
Extensive review of literature covering state of the art MRI/cisplatin and
derivatives, previous theranostic research and synthetic methods
Continuous synthesis followed by characterisation at most stages – why was
this important? A) Expense B) Time C) Originality
Continuous write up Inc. electronic version and coded experiments
(each attempt)
Oral presentation Inc. Q&A with academics and peers and report
Project VIVA voce
Skills acquired/exercised:
Time management
Organisation
Independent laboratory skills/competency
Communication skills
Knowledge and experience developed in synthetic and analytical chemistry
A much deeper, education appreciation for scientific research
The End
References:
[1]- S. S. Kelkar and T. M. Reineke, Bioconjugate Chem, 2011, 22, 1879.
[2]- Alois Kozubík, Alena Vaculová, Karel Souček, Jan Vondráček, Jaroslav
Turánek, and Jiřina Hofmanová, Metal based drugs, 2008, 15, 2008.
[3]- J. A. Park, J. J. Lee, J. C. Jung, D. Y. Yu, C. Oh, S. Ha,T. J. Kim and Y. Chang,
ChemBioChem, 2008, 9, 2811.
Recommended