Synthesis and preclinical evaluation of a selective MET kinase positron emission tomography tracer.

The tyrosine kinase MET (hepatocyte growth factor receptor) is activated or mutated in a wide range of cancers and is often correlated with a poor prognosis. Precision medicine with positron emission tomography (PET) can potentially aid in the assessment of tumor biochemistry and heterogeneity, which can prompt the selection of the most effective therapeutic regimes. The selective MET inhibitor PF04217903 (1) formed the basis for a bioisosteric replacement, leading to the deoxyfluorinated analog [ F]2.

Four new subspecies of butterflies (Lepidoptera, Papilionoidea) from Phu Quoc Island, southern Vietnam.

We describe and illustrate four new subspecies of Papilionoidea butterflies which were collected from Phu Quoc Island, Kien Giang province, southern Vietnam between 2006 and 2017. These are papilionid Graphium antiphates matsui T. Saito & Vu subspec.

Thirty years of nutrients and biogeochemistry in the Norwegian, Greenland and Iceland Seas, 1990-2019.

This dataset contains biogeochemical samples analyzed by the Plankton Chemistry Laboratory at the Institute of Marine Research (IMR), from the Norwegian, Greenland and Iceland Seas. Number of surveys and stations have varied greatly over the last 3 decades. IMR is conducting one annual Ecosystem Survey in April-May each year, with multiple trawl surveys and net tows, but only CTD water collections are reported here.

Thirty Years of Nutrient Biogeochemistry in the Barents Sea and the adjoining Arctic Ocean, 1990-2019.

This dataset contains biogeochemical samples from the Barents Sea and Arctic region analyzed by the Plankton Chemistry Laboratory at the Institute of Marine Research (IMR). Number of surveys and stations visited in the Barents Sea and Arctic has varied over the last 30 years. One major effort is the annual Ecosystem Survey in the fall, with multiple trawl surveys, net tows and CTD water sampling.

A new species related to Ypthima praenubila Leech, 1891 in Vietnam and China (Lepidoptera, Nymphalidae, Satyrinae).

We describe a new species of satyrine butterfly, Ypthima thao Monastyrskii Lang sp. nov., recently discovered in northern Vietnam and southwestern China.

New taxa and new records of butterflies from Vietnam (Lepidoptera, Papilionoidea)nbsp.

A new species and eight new subspecies of Papilionoidea discovered in Vietnam between 2002 and 2020 are described and illustrated. The status of two taxa are revised. New taxa include Pieridae: Delias sanaca bidoupa Monastyrskii Vu subspec.

Preclinical evaluation of [F]cabozantinib as a PET imaging agent in a prostate cancer mouse model.

Introduction: Cabozantinib is a tyrosine kinase inhibitor (TKI) approved for the treatment of medullary thyroid cancer, renal cell carcinoma and hepatocellular carcinoma, and is currently in clinical trials for the treatment of prostate cancer and others. It exerts its therapeutic effect mainly through inhibition of the tyrosine kinases MET (hepatocyte growth factor receptor) and VEGFR2 (vascular endothelial growth factor receptor 2), in addition to several other kinases involved in cancer. PET imaging with TKIs such as [F]cabozantinib could potentially aid in cancer diagnosis and guide treatment.

Correction: Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation.

[This corrects the article DOI: 10.1039/C9RA08954C.].

Towards dual inhibitors of the MET kinase and WNT signaling pathway; design, synthesis and biological evaluation.

Both the kinase MET and the WNT signaling pathway are attractive targets in cancer therapy, and synergistic effects have previously been observed in animal models upon simultaneous inhibition. A strategy towards a designed multiple ligand of MET and WNT signaling is pursued based on the two hetero biaryl systems present in both the MET inhibitor tepotinib and WNT signaling inhibitor TC-E 5001. Initial screening was conducted to find the most suitable ring systems for further optimization, whereas a second screen explored modifications towards pyridazinones and triazolo pyridazines.

Analysis of the 56-kDa type specific antigen gene of Orientia tsutsugamushi from northern Vietnam.

Scrub typhus has been documented since 1932 in Vietnam, however, the disease burden of scrub typhus remains poorly understood in the country. We conducted this study to describe the phylogenetic analysis of the 56-kDa type-specific antigen (TSA) gene of Orientia tsutsugamushi associated with PCR positive cases of scrub typhus. Of 116 positive samples, 65 type-specific antigen gene sequences were obtained and classified into 3 genogroups: Karp, Kato and Gilliam.

Design, synthesis and biological evaluation of 6-substituted quinolines derived from cabozantinib as c-Met inhibitors.

Based on the cabozantinib scaffold, novel c-Met inhibitors were rationalized from the limited knowledge of structure-activity relationships for the quinoline 6-position. Emphasis was given to modifications capable of engaging in additional polar interactions with the c-Met active site. In addition, ortho-fluorinations of the terminal benzene ring were explored.

Clinical Manifestations and Molecular Diagnosis of Scrub Typhus and Murine Typhus, Vietnam, 2015-2017.

Rickettsioses are endemic to Vietnam; however, only a limited number of clinical studies have been performed on these vectorborne bacteria. We conducted a prospective hospital-based study at 2 national referral hospitals in Hanoi to describe the clinical characteristics of scrub typhus and murine typhus in northern Vietnam and to assess the diagnostic applicability of quantitative real-time PCR assays to diagnose rickettsial diseases. We enrolled 302 patients with acute undifferentiated fever and clinically suspected rickettsiosis during March 2015-March 2017.

Description of a new species of Cephalaeschna (Odonata: Anisoptera: Aeshnidae) from northern Vietnam.

A new aeshnid species, Cephalaeschna yanagisawai sp. nov. from northern Vietnam (Hoang Lien National Park, Lai Chau Province, 103°45'E, 22°20'N, 1900~2000 m a.

One-step synthesis of [ F]cabozantinib for use in positron emission tomography imaging of c-Met.

Cabozantinib is an FDA-approved kinase inhibitor for the treatment of medullary thyroid cancer and advanced renal cell carcinoma, which exerts its therapeutic effect by inhibiting, among others, the tyrosine kinase c-Met. Noninvasive imaging techniques are becoming increasingly important clinically to ensure drug efficacy, staging, monitoring, and patient stratification. PET isotope labelled tyrosine kinase inhibitors have, for the same reason, potential as PET tracers for imaging of various cancers.

Protocol for a single-centre, randomised controlled study of a preoperative rehabilitation bundle in the frail and elderly undergoing abdominal surgery.

Introduction: Frail patients have decreased physiological reserves and consequently, they are unable to recover as quickly from surgery. Frailty, as an entity, is a risk factor of increased morbidity and mortality. It is also associated with a longer time to discharge.

Crystal structure of 6,7-dimeth-oxy-1-(4-nitro-phen-yl)quinolin-4(1)-one: a mol-ecular scaffold for potential tubulin polymerization inhibitors.

The protein tubulin is central for maintaining normal cellular processes, and mol-ecules inter-fering with the tubulin dynamics have potential in the treatment of cancerous diseases. The title compound, CHNO, was prepared as a lead compound in a project dedicated to the development of therapeutic agents binding to the colchicine binding site on tubulin, thereby inter-fering with the cell division in cancer cells. It holds many of the main structural characteristics for colchicine binding and has the potential for further modification and functionalization.

Tunable luminescent emission characterization of type-I and type-II systems in CdS-ZnSe core-shell nanoparticles: Raman and photoluminescence study.

We used wet chemical methods to synthesize core-shell nanocrystalline samples CdS(d)/ZnSe N , where d = 3-6 nm and N = 1-5 are the size of CdS cores and the number of monolayers grown on the cores, respectively. By annealing typical CdS(d)/ZnSe N samples (with d = 3 and 6 nm and N = 2) at 300 °C for various times t an = 10-600 min, we created an intermediate layer composed of Zn1-x Cd x Se and Cd1-x Zn x S alloys with various thicknesses. The formation of core-shell structures and intermediate layers was monitored by Raman scattering and UV-vis absorption spectrometers.

Use of Scleral Lenses and Miniscleral Lenses After Penetrating Keratoplasty.

Purpose: To examine the clinical outcomes of scleral lenses for visual rehabilitation after penetrating keratoplasty (PK).

Methods: A retrospective review was conducted for 34 patients (48 eyes) who had a history of prior PK and were fit with scleral lenses between October 2009 and December 2013 at the UC Davis Eye Center.

Results: The most common initial indication for PK was keratoconus in 27 eyes (56%).

Dispersants have limited effects on exposure rates of oil spills on fish eggs and larvae in shelf seas.

Early life stages of fish are particularly vulnerable to oil spills. Simulations of overlap of fish eggs and larvae with oil from different oil-spill scenarios, both without and with the dispersant Corexit 9500, enable quantitative comparisons of dispersants as a mitigation alternative. We have used model simulations of a blow out of 4500 m(3) of crude oil per day (Statfjord light crude) for 30 days at three locations along the Norwegian coast.

Radiosynthesis of [18)F]trifluoroalkyl groups: scope and limitations.

The present paper is concerned with radiochemical methodology to furnish the trifluoromethyl motif labelled with (18)F. Literature spanning the last four decades is comprehensively reviewed and radiochemical yields and specific activities are discussed.

Cu(I)-mediated (18)F-trifluoromethylation of arenes: rapid synthesis of (18)F-labeled trifluoromethyl arenes.

This report is concerned with an efficient, Cu(I)-mediated method for the radiosynthesis of [(18)F]trifluoromethyl arenes, abundant motifs in small molecule drug candidates and potential radiotracers for positron emission tomography. Three (18)F-labelled radiotracer candidates were synthesised from [(18)F]fluoride ions as proof of principle. The new protocol is widely applicable for the synthesis of novel radiotracers in high radiochemical yields.

Universally applicable three-dimensional hydrodynamic microfluidic flow focusing.

We have demonstrated a microfluidic device that can not only achieve three-dimensional flow focusing but also confine particles to the center stream along the channel. The device has a sample channel of smaller height and two sheath flow channels of greater height, merged into the downstream main channel where 3D focusing effects occur. We have demonstrated that both beads and cells in our device display significantly lower CVs in velocity and position distributions as well as reduced probability of coincidental events than they do in conventional 2D-confined microfluidic channels.

One mechanism contributing to co-variability of the Atlantic inflow branches to the Arctic.

The two-branched inflow of warm and saline Atlantic Water to the Arctic is the major contributor of oceanic heat to the Arctic climate system. However, while the Atlantic Water entering the Arctic through the Fram Strait retains a large part of its heat as it flows along the Arctic continental slope, the branch flowing through the shallow Barents Sea releases a substantial amount of heat to the atmosphere. Hence, the pathway of the Atlantic Water into the Arctic to a large degree determines the short term fate of its heat.