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3.
J Mol Graph Model ; 108: 107999, 2021 11.
Article in English | MEDLINE | ID: mdl-34352727

ABSTRACT

Bioactive peptides derived from food proteins are becoming increasingly popular due to the growing awareness of their health-promoting properties. The structure and mechanism of anti-cancer action of pentapeptide Glu-Gln-Arg-Pro-Arg (EQRPR) derived from a rice bran protein are not known. Theoretical and experimental methods were employed to fill this gap. The conformation analysis of the EQRPR pentapeptide was performed first and the obtained lowest energy conformer was optimized. The experimental structural data obtained by FTIR and CD spectroscopies agree well with the theoretical results. d-isomer introduced one-by-one to each position and all D-isomers of the peptide were also examined for its possible anti-proteolytic and activity enhancement properties. The molecular docking revealed avid binding of the pentapeptide to the integrins α5ß1 and αIIbß3, with Kd values of 90 nM and 180 nM, respectively. Moreover, the EQRPR and its D-isomers showed strong binding affinities to apo- and holo-forms of Mpro, spike glycoprotein, ACE2, and dACE2. The predicted results indicate that the pentapeptide may significantly inhibit SARS-CoV-2 infection. Thus, the peptide has the potential to be the leading molecule in the drug discovery process as having multifunctional with diverse biological activities.


Subject(s)
COVID-19 , Oryza , Humans , Molecular Docking Simulation , Oligopeptides , SARS-CoV-2
4.
Clin Nucl Med ; 44(6): e415-e417, 2019 Jun.
Article in English | MEDLINE | ID: mdl-30789400

ABSTRACT

A 54-year-old man with multiple endocrine neoplasia type 1 had previous history of parathyroid surgery and left thyroid lobectomy 5 years earlier, and was referred for recurrent hypoglycemic episodes. Ga-DOTATATE PET/CT had showed multiple lesions in the right lung, liver, and pancreas. Biopsy from pancreas revealed low-grade neuroendocrine neoplasia. After 2 fractions of Lu-DOTATATE therapy, the size of lesions and its activity reduced on the Ga-DOTATATE scan and the hypoglycemic episodes manifested every day have scaled down to 1 time over 1-year follow-up. Herein, we report a case of malignant insulinoma successfully treated with radiolabeled somatostatin receptor therapy using Lu-DOTATATE.


Subject(s)
Antineoplastic Agents, Hormonal/therapeutic use , Insulinoma/secondary , Multiple Endocrine Neoplasia Type 1/pathology , Octreotide/analogs & derivatives , Organometallic Compounds/therapeutic use , Pancreas/pathology , Pancreatic Neoplasms/secondary , Positron Emission Tomography Computed Tomography , Biopsy , Humans , Insulinoma/diagnostic imaging , Insulinoma/drug therapy , Male , Middle Aged , Octreotide/therapeutic use , Pancreatic Neoplasms/diagnostic imaging , Pancreatic Neoplasms/drug therapy , Radiopharmaceuticals , Receptors, Somatostatin/therapeutic use , Solitary Kidney
5.
J Contemp Brachytherapy ; 9(2): 106-111, 2017 Apr.
Article in English | MEDLINE | ID: mdl-28533797

ABSTRACT

PURPOSE: To describe early results of two cohorts of patients with low and intermediate risk of early breast cancer treated with accelerated partial breast irradiation (APBI) using different schedules of multicatheter brachytherapy. MATERIAL AND METHODS: Patients with early stage breast cancer after breast conserving surgery were enrolled for a prospective analysis. The APBI, using multicatheter brachytherapy, was delivered either eight times 4 Gy in five days with a planned total dose of 32 Gy, or seven times 5 Gy in four days with a planned total dose of 35 Gy. Primary endpoints were side effects. RESULTS: Forty-eight patients were enrolled between 2012 and 2014. Patients characteristics were as follow: median age of patients was 55 years, early breast cancer was defined according GEC-ESTRO recommendations. With a median follow-up period of 37 months, no significant differences regarding late side effects and cosmesis between two cohorts of patients were documented. In total, cosmesis was excellent in 13/48 (27.1%) patients, good in 34/48 (70.8%) patients, and moderate in 1/48 patient (2.1%). CONCLUSIONS: Accelerated partial breast irradiation using multicatheter brachytherapy with 32 Gy/8 fractions and 35 Gy/7 fractions for early breast cancer seems to be similar in terms of late side effects. According to our findings, APBI was also feasible for intermediate-risk of early breast cancer patients.

6.
Clin Nucl Med ; 40(1): 47-9, 2015 Jan.
Article in English | MEDLINE | ID: mdl-25275413

ABSTRACT

A 68-year-old man, with a history of pituitary surgery and radiation therapy for pituitary macroadenoma 20 years earlier, presented with a pituitary mass and enlarging lesions within the posterior fossa and spinal canal. Biopsy revealed low-grade pituitary carcinoma. PET/CT scan showed multiple foci of increased Ga DOTATATE activity including pituitary and posterior fossa lesions. After 3 fractions of Lu DOTATATE therapy, the tumor remained stable over 4 years on MRI and Ga DOTATATE scans. This case illustrates the benefit of Ga DOTATATE PET/CT in malignant pituitary disease to assess potential for somatostatin receptor therapy with Lu DOTATATE and monitor treatment.


Subject(s)
Carcinoma/diagnostic imaging , Octreotide/analogs & derivatives , Organometallic Compounds/therapeutic use , Pituitary Neoplasms/diagnostic imaging , Radiopharmaceuticals , Aged , Carcinoma/radiotherapy , Humans , Male , Multimodal Imaging , Octreotide/therapeutic use , Pituitary Neoplasms/radiotherapy , Positron-Emission Tomography , Radiopharmaceuticals/therapeutic use , Tomography, X-Ray Computed
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