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  1. Article ; Online: Designing Novel Compounds for the Treatment and Management of RET-Positive Non-Small Cell Lung Cancer—Fragment Based Drug Design Strategy

    Priyanka Ramesh / Shanthi Veerappapillai

    Molecules, Vol 27, Iss 1590, p

    2022  Volume 1590

    Abstract: Rearranged during transfection (RET) is an oncogenic driver receptor that is overexpressed in several cancer types, including non-small cell lung cancer. To date, only multiple kinase inhibitors are widely used to treat RET-positive cancer patients. ... ...

    Abstract Rearranged during transfection (RET) is an oncogenic driver receptor that is overexpressed in several cancer types, including non-small cell lung cancer. To date, only multiple kinase inhibitors are widely used to treat RET-positive cancer patients. These inhibitors exhibit high toxicity, less efficacy, and specificity against RET. The development of drug-resistant mutations in RET protein further deteriorates this situation. Hence, in the present study, we aimed to design novel drug-like compounds using a fragment-based drug designing strategy to overcome these issues. About 18 known inhibitors from diverse chemical classes were fragmented and bred to form novel compounds against RET proteins. The inhibitory activity of the resultant 115 hybrid molecules was evaluated using molecular docking and RF-Score analysis. The binding free energy and chemical reactivity of the compounds were computed using MM-GBSA and density functional theory analysis, respectively. The results from our study revealed that the developed hybrid molecules except for LF21 and LF27 showed higher reactivity and stability than Pralsetinib. Ultimately, the process resulted in three hybrid molecules namely LF1, LF2, and LF88 having potent inhibitory activity against RET proteins. The scrutinized molecules were then subjected to molecular dynamics simulation for 200 ns and MM-PBSA analysis to eliminate a false positive design. The results from our analysis hypothesized that the designed compounds exhibited significant inhibitory activity against multiple RET variants. Thus, these could be considered as potential leads for further experimental studies.
    Keywords RET protein ; docking ; RF-Score ; molecular dynamics ; DFT calculations ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2022-02-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: A retrospective study on the clinico-demographic profile of multiple sclerosis patients in various tertiary care hospitals in Mangalore city of South India

    Nitin Joseph / Rachel Melissa Salins / Priyanka Ramesh / Narayana Venkatesh Krishna

    Romanian Journal of Neurology, Vol 20, Iss 3, Pp 349-

    2021  Volume 355

    Abstract: Objectives. To study the risk factors, clinical presentations, course of the disease, investigations and management practices in MS. Materials and methods. Records of 23 patients diagnosed with MS using the McDonald diagnostic criteria were analysed. ... ...

    Abstract Objectives. To study the risk factors, clinical presentations, course of the disease, investigations and management practices in MS. Materials and methods. Records of 23 patients diagnosed with MS using the McDonald diagnostic criteria were analysed. Outcomes. The mean age at diagnosis was 34.6±17.1 years. 17 (73.9%) patients were females. Early and late onset MS were present among 2 (8.7%) and 4 (17.4%) patients respectively. The most common symptom at diagnosis was paraesthesia [9 (39.1%)]. Motor symptoms and sensory symptoms at the time of diagnosis were present among 9(39.1%) patients each. 20 (87%) patients had motor system involvement, 9 (39.1%) had sensory system involvement, 12 (52.2%) had cranial nerve involvement, 4 (17.4%) had sphincter dysfunction and 2 (8.7%) had cerebellar involvement. Relapsing and remitting MS (RRMS) were present among 18 (78.3%) patients. Oligoclonal bands were present among 17 (73.9%) patients. Vitamin D levels in the blood were found deficient among 4 (80%) out of 5 patients with available reports of the same. Juxtacortical region was the most common [9 (39.1%)] site of involvement. Steroids were used for management among majority [12 (52.2%)] of the patients. Non-pharmacological methods for management constituted only physiotherapy which was advised among 13 (56.5%) patients. Improvement in treatment outcome were seen among 19 (82.6%) patients. Conclusions. Almost three fourth of the patients were females. RRMS was the most common course of the disease. Juxtacortical region was the most common site involved. Steroids were most commonly used for management. More non-pharmacological methods need to be introduced for MS management.
    Keywords multiple sclerosis ; risk factors ; clinical features ; investigations ; management ; hospital based study ; Medicine ; R ; Neurology. Diseases of the nervous system ; RC346-429
    Subject code 610 ; 616
    Language English
    Publishing date 2021-09-01T00:00:00Z
    Publisher Amaltea Medical Publishing House
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article: Cone Beam Computed Tomography- An Effective Tool in Detecting Caries Under Fixed Dental Prostheses.

    Vedpathak, Priyanka Ramesh / Gondivkar, Shailesh Madhukar / Bhoosreddy, Ajay Ramesh / Shah, Karan Rajendra / Verma, Gaurav Ravishankar / Mehrotra, Gayatri Praveen / Nerkar, Ashwini Chandrakant

    Journal of clinical and diagnostic research : JCDR

    2016  Volume 10, Issue 8, Page(s) ZC10–3

    Abstract: Introduction: Caries under restorations is the most common reason for re-treatment and replacement in restorative failures. To avoid failures of fixed dental prostheses, it is important to diagnose caries under it earlier. Without image degradation and ... ...

    Abstract Introduction: Caries under restorations is the most common reason for re-treatment and replacement in restorative failures. To avoid failures of fixed dental prostheses, it is important to diagnose caries under it earlier. Without image degradation and metal artifacts, Cone Beam Computed Tomography (CBCT) can be the solution to detect caries without removing fixed dental prostheses.
    Aim: The aim of this study was to determine the efficacy of CBCT in detecting caries under fixed dental prostheses.
    Materials and methods: Each specimen was scanned with CBCT for evaluation of secondary caries under fixed prostheses. Exposure parameters were 60 kVp and 3mA. Field of View (FOV) used was 8cm X 8cm. According to International Caries Detection and Assessment System (ICDAS) criteria, six Grade 6 carious extracted teeth were selected. All teeth were prepared with four different specimens - full metal, metal-ceramic, full ceramic and metal-acrylic crowns for each tooth. Each specimen was scanned by CBCT. T-test was performed for mean gray value differences between caries and noncaries regions of each material. Gray values were recorded and evaluated for different parameters using two-way analysis of variance.
    Results: Significant differences were found with respect to material (full metal, metal-ceramic, full ceramic and metal-acrylic) and situation (caries/noncaries) (p<0.001). There were no significant differences with respect to location (anterior or posterior). Mean gray values of caries and noncaries regions were found to be different for each material.
    Conclusion: CBCT can be used as a post-treatment diagnostic technique for detecting caries under fixed prostheses without removing it.
    Language English
    Publishing date 2016-08-01
    Publishing country India
    Document type Journal Article
    ZDB-ID 2775283-5
    ISSN 0973-709X ; 2249-782X
    ISSN (online) 0973-709X
    ISSN 2249-782X
    DOI 10.7860/JCDR/2016/18589.8228
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Cone Beam Computed Tomography-An Effective Tool in Detecting Caries Under Fixed Dental Prostheses

    Priyanka Ramesh Vedpathak / Shailesh Madhukar Gondivkar / Ajay Ramesh Bhoosreddy / Karan Rajendra Shah / Gaurav Ravishankar Verma / Gayatri Praveen Mehrotra / Ashwini Chandrakant Nerkar

    Journal of Clinical and Diagnostic Research, Vol 10, Iss 8, Pp ZC10-ZC

    2016  Volume 13

    Abstract: Introduction: Caries under restorations is the most common reason for re-treatment and replacement in restorative failures. To avoid failures of fixed dental prostheses, it is important to diagnose caries under it earlier. Without image degradation and ... ...

    Abstract Introduction: Caries under restorations is the most common reason for re-treatment and replacement in restorative failures. To avoid failures of fixed dental prostheses, it is important to diagnose caries under it earlier. Without image degradation and metal artifacts, Cone Beam Computed Tomography (CBCT) can be the solution to detect caries without removing fixed dental prostheses. Aim: The aim of this study was to determine the efficacy of CBCT in detecting caries under fixed dental prostheses. Materials and Methods: Each specimen was scanned with CBCT for evaluation of secondary caries under fixed prostheses. Exposure parameters were 60 kVp and 3mA. Field of View (FOV) used was 8cm X 8cm. According to International Caries Detection and Assessment System (ICDAS) criteria, six Grade 6 carious extracted teeth were selected. All teeth were prepared with four different specimens - full metal, metal-ceramic, full ceramic and metal-acrylic crowns for each tooth. Each specimen was scanned by CBCT. T-test was performed for mean gray value differences between caries and noncaries regions of each material. Gray values were recorded and evaluated for different parameters using two-way analysis of variance. Results: Significant differences were found with respect to material (full metal, metal-ceramic, full ceramic and metalacrylic) and situation (caries/noncaries) (p<0.001). There were no significant differences with respect to location (anterior or posterior). Mean gray values of caries and noncaries regions were found to be different for each material. Conclusion: CBCT can be used as a post-treatment diagnostic technique for detecting caries under fixed prostheses without removing it.
    Keywords dentin ; diagnosis ; mean gray value ; Medicine ; R
    Subject code 670
    Language English
    Publishing date 2016-08-01T00:00:00Z
    Publisher JCDR Research and Publications Private Limited
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: Generation and characterization of a bivalent protein boost for future clinical trials

    Yingxia Wen / Hung V Trinh / Christine E Linton / Chiara Tani / Nathalie Norais / DeeAnn Martinez-Guzman / Priyanka Ramesh / Yide Sun / Frank Situ / Selen Karaca-Griffin / Christopher Hamlin / Sayali Onkar / Sai Tian / Susan Hilt / Padma Malyala / Rushit Lodaya / Ning Li / Gillis Otten / Giuseppe Palladino /
    Kristian Friedrich / Yukti Aggarwal / Celia LaBranche / Ryan Duffy / Xiaoying Shen / Georgia D Tomaras / David C Montefiori / William Fulp / Raphael Gottardo / Brian Burke / Jeffrey B Ulmer / Susan Zolla-Pazner / Hua-Xin Liao / Barton F Haynes / Nelson L Michael / Jerome H Kim / Mangala Rao / Robert J O'Connell / Andrea Carfi / Susan W Barnett

    PLoS ONE, Vol 13, Iss 4, p e

    HIV-1 subtypes CR01_AE and B gp120 antigens with a potent adjuvant.

    2018  Volume 0194266

    Abstract: The RV144 Phase III clinical trial with ALVAC-HIV prime and AIDSVAX B/E subtypes CRF01_AE (A244) and B (MN) gp120 boost vaccine regime in Thailand provided a foundation for the future development of improved vaccine strategies that may afford protection ... ...

    Abstract The RV144 Phase III clinical trial with ALVAC-HIV prime and AIDSVAX B/E subtypes CRF01_AE (A244) and B (MN) gp120 boost vaccine regime in Thailand provided a foundation for the future development of improved vaccine strategies that may afford protection against the human immunodeficiency virus type 1 (HIV-1). Results from this trial showed that immune responses directed against specific regions V1V2 of the viral envelope (Env) glycoprotein gp120 of HIV-1, were inversely correlated to the risk of HIV-1 infection. Due to the low production of gp120 proteins in CHO cells (2-20 mg/L), cleavage sites in V1V2 loops (A244) and V3 loop (MN) causing heterogeneous antigen products, it was an urgent need to generate CHO cells harboring A244 gp120 with high production yields and an additional, homogenous and uncleaved subtype B gp120 protein to replace MN used in RV144 for the future clinical trials. Here we describe the generation of Chinese Hamster Ovary (CHO) cell lines stably expressing vaccine HIV-1 Env antigens for these purposes: one expressing an HIV-1 subtype CRF01_AE A244 Env gp120 protein (A244.AE) and one expressing an HIV-1 subtype B 6240 Env gp120 protein (6240.B) suitable for possible future manufacturing of Phase I clinical trial materials with cell culture expression levels of over 100 mg/L. The antigenic profiles of the molecules were elucidated by comprehensive approaches including analysis with a panel of well-characterized monoclonal antibodies recognizing critical epitopes using Biacore and ELISA, and glycosylation analysis by mass spectrometry, which confirmed previously identified glycosylation sites and revealed unknown sites of O-linked and N-linked glycosylations at non-consensus motifs. Overall, the vaccines given with MF59 adjuvant induced higher and more rapid antibody (Ab) responses as well as higher Ab avidity than groups given with aluminum hydroxide. Also, bivalent proteins (A244.AE and 6240.B) formulated with MF59 elicited distinct V2-specific Abs to the epitope previously shown to ...
    Keywords Medicine ; R ; Science ; Q
    Subject code 570
    Language English
    Publishing date 2018-01-01T00:00:00Z
    Publisher Public Library of Science (PLoS)
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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