| 000 | 03784nlm1a2200589 4500 | ||
|---|---|---|---|
| 001 | 664012 | ||
| 005 | 20231030041915.0 | ||
| 035 | _a(RuTPU)RU\TPU\network\35182 | ||
| 035 | _aRU\TPU\network\35144 | ||
| 090 | _a664012 | ||
| 100 | _a20210323a2019 k y0engy50 ba | ||
| 101 | 0 | _aeng | |
| 135 | _adrcn ---uucaa | ||
| 181 | 0 | _ai | |
| 182 | 0 | _ab | |
| 200 | 1 |
_aComparative Evaluation of Two DARPin Variants: Effect of Affinity, Size, and Label on Tumor Targeting Properties _fS. M. Deev, A. Vorobjeva, A. A. Schulga [et al.] |
|
| 203 |
_aText _celectronic |
||
| 300 | _aTitle screen | ||
| 330 | _aDesigned ankyrin repeat proteins (DARPins) are small engineered scaffold proteins that can be selected for binding to desirable molecular targets. High affinity and small size of DARPins render them promising probes for radionuclide molecular imaging. However, detailed knowledge on many factors influencing their imaging properties is still lacking. We have evaluated two human epidermal growth factor 2 (HER2)-specific DARPins with different size and binding properties. DARPins 9_29-H6 and G3-H6 were radiolabeled with iodine-125 and tricarbonyl technetium-99m and evaluated in vitro. A side-by-side comparison of biodistribution and tumor targeting was performed. HER2-specific tumor accumulation of G3-H6 was demonstrated. A combination of smaller size and higher affinity resulted in a higher tumor uptake of G3-H6 in comparison to 9_29-H6. Technetium-99m labeled G3-H6 demonstrated a better biodistribution profile than 9_29-H6, with several-fold lower uptake in liver. Radioiodinated G3-H6 showed the best tumor-to-organ ratios. The combined effect of affinity, molecular weight, scaffold composition, and nonresidualizing properties of iodine label provided radioiodinated G3-H6 with high clinical potential for imaging of HER2. | ||
| 333 | _aРежим доступа: по договору с организацией-держателем ресурса | ||
| 338 |
_bРоссийский научный фонд _d14-24-00106 |
||
| 461 | _tACS Molecular Pharmaceutics | ||
| 463 |
_tVol. 16, No. 3 _v[P. 995–1008] _d2019 |
||
| 610 | 1 | _aтруды учёных ТПУ | |
| 610 | 1 | _aэлектронный ресурс | |
| 610 | 1 | _aDARPin | |
| 610 | 1 | _atargeting | |
| 610 | 1 | _aradionuclide | |
| 610 | 1 | _aimaging | |
| 610 | 1 | _aI-125 | |
| 610 | 1 | _aTc-99m | |
| 610 | 1 | _aрадионуклиды | |
| 610 | 1 | _aвизуализация | |
| 610 | 1 | _aопухоли | |
| 610 | 1 | _aтехнеций-99м | |
| 701 | 1 |
_aDeev _bS. M. _cbiologist _cLeading Researcher, Tomsk Polytechnic University, Doctor of Biological Sciences _f1951- _gSergey Mikhaylovich _2stltpush _3(RuTPU)RU\TPU\pers\39299 |
|
| 701 | 1 |
_aVorobjeva _bA. _gAnzhelika |
|
| 701 | 1 |
_aSchulga _bA. A. _gAleksey Anatoljevich |
|
| 701 | 1 |
_aProshkina _bG. M. _gGalina Mikhaylovna |
|
| 701 | 1 |
_aGuler _bR. _gRezan |
|
| 701 | 1 |
_aLofblom _bJ. _gJohn |
|
| 701 | 1 |
_aMitran _bB. _gBogdan |
|
| 701 | 1 |
_aGarousi _bJ. _gJavad |
|
| 701 | 1 |
_aAltai _bM. _gMohamed |
|
| 701 | 1 |
_aBuijs _bJ. _gJos |
|
| 701 | 1 |
_aChernov _bV. I. _cspecialist in the field of medical technology _clead engineer of Tomsk Polytechnic University, doctor of medical sciences _f1962- _gVladimir Ivanovich _2stltpush _3(RuTPU)RU\TPU\pers\34191 |
|
| 701 | 1 |
_aOrlova _bA. _gAnna |
|
| 701 | 1 |
_aTolmachev _bV. M. _gVladimir Mikhaylovich |
|
| 712 | 0 | 2 |
_aНациональный исследовательский Томский политехнический университет _bФизико-технический институт _bЛаборатория № 31 ядерного реактора _h6471 _2stltpush _3(RuTPU)RU\TPU\col\20054 |
| 801 | 2 |
_aRU _b63413507 _c20210323 _gRCR |
|
| 856 | 4 | _uhttps://doi.org/10.1021/acs.molpharmaceut.8b00922 | |
| 942 | _cCF | ||