ORCID Profile
0000-0002-2446-1376
Current Organisation
The University of Auckland
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Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/D0SC01814G
Abstract: We herein report the synthesis and biological and computational evaluation of 12 linear analogues of the cyclic lipopeptide battacin, enabled by Cysteine Lipidation on a Peptide or Amino Acid (CLipPA) technology.
Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/D0SM01071E
Abstract: Increased water solubility and long-range intermolecular ordering have been introduced into the fluorescent organic molecule thiophene-diketopyrrolopyrrole via its conjugation to the octapeptide HEFISTAH, derived from a protein–protein β-interface.
Publisher: Elsevier BV
Date: 06-2020
Publisher: Royal Society of Chemistry (RSC)
Date: 2021
DOI: 10.1039/D0CS00354A
Abstract: Thiol–ene chemistry, a tailored approach to access novel peptide-based drugs.
Publisher: Elsevier BV
Date: 12-2019
Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/D0OB00203H
Abstract: Cyclic lipopeptides are often challenging synthetic targets. A synthetic approach is presented that employs cyclisation by intramolecular native chemical ligation (NCL) and a thiol–ene “CLipPA” reaction to afford S -lipidated analogues of iturin A.
Publisher: Royal Society of Chemistry (RSC)
Date: 2020
DOI: 10.1039/D0OB00950D
Abstract: Thiol–ene CLipPA reaction of a vinyl ester and thiolated peptide for generation of an S -lipidated paenipeptin C′ analogue with broad spectrum antibacterial activity.
Publisher: Royal Society of Chemistry (RSC)
Date: 2018
DOI: 10.1039/C8OB02929F
Abstract: The amyloidogenic Aβ42 peptide was efficiently prepared using a double linker system, markedly improving solubility and chromatographic peak resolution, thus enabling full characterisation using standard techniques. The tag was readily cleaved with sodium hydroxide and removed by aqueous extraction, affording Aβ42 in high purity and yield for biophysical characterisation studies.
Publisher: Elsevier BV
Date: 08-2020
Publisher: MDPI AG
Date: 27-09-2021
DOI: 10.3390/MOLECULES26195847
Abstract: The large number of emerging antibody-drug conjugates (ADCs) for cancer therapy has resulted in a significant market ‘boom’, garnering worldwide attention. Despite ADCs presenting huge challenges to researchers, particularly regarding the identification of a suitable combination of antibody, linker, and payload, as of September 2021, 11 ADCs have been granted FDA approval, with eight of these approved since 2017 alone. Optimism for this therapeutic approach is clear, despite the COVID-19 pandemic, 2020 was a landmark year for deals and partnerships in the ADC arena, suggesting that there remains significant interest from Big Pharma. Herein we review the enthusiasm for ADCs by focusing on the features of those approved by the FDA, and offer some thoughts as to where the field is headed.
Publisher: Royal Society of Chemistry (RSC)
Date: 2023
DOI: 10.1039/D3OB01469J
Publisher: MDPI AG
Date: 14-01-2023
DOI: 10.3390/PHARMACEUTICS15010287
Abstract: Pancreatic ductal adenocarcinoma remains a highly debilitating condition with no effective disease-modifying interventions. In our search for natural products with promising anticancer activity, we identified the aminolipopeptide trichoderin A as a potential candidate. While it was initially isolated as an antitubercular peptide, we provide evidence that it is also selectively toxic against BxPC-3 and PANC-1 human pancreatic ductal adenocarcinoma cells cultured under glucose deprivation. This has critical implications for the pancreatic ductal adenocarcinoma, which is characterized by nutrient deprivation due to its hypovascularized network. We have also successfully simplified the trichoderin A peptide backbone, allowing greater accessibility to the peptide for further biological testing. In addition, we also conducted a preliminary investigation into the role of peptide lipidation at the N-terminus. This showed that analogues with longer fatty acyl chains exhibited superior cytotoxicity than those with shorter acyl chains. Further structural optimization of trichoderin A is anticipated to improve its biological activity, whilst ongoing mechanistic studies to elucidate its intracellular mechanism of action are conducted in parallel.
Publisher: Royal Society of Chemistry (RSC)
Date: 2021
DOI: 10.1039/D1OB00355K
Abstract: In this work, the synthesis of reactive oxygen species responsive mono S -lipidated peptide hydrogels via a photoinitiated thiol–ene reaction is reported.
Publisher: Royal Society of Chemistry (RSC)
Date: 2017
DOI: 10.1039/C7CC05025A
Abstract: Advanced lipid peroxidation end-products (ALEs) accumulate with ageing and oxidative stress-related diseases.
Publisher: Royal Society of Chemistry (RSC)
Date: 2023
DOI: 10.1039/D2OB02262A
Abstract: Cysteine-selective thia-Michael addition provides opportunities in chemistry, biology, and medicine.
No related grants have been discovered for Iman Kavianinia.