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1.
PRiMER ; 7: 15, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37465832

RESUMEN

Objectives: This project analyzed the culture of safety quality improvement at the Family Medicine Center (FMC). The Agency for Healthcare Research and Quality (AHRQ) Culture of Safety Survey was used as a benchmark for internal and external comparison. Methods: The AHRQ Culture of Safety Survey was administered to health care staff in 2015, 2017, and 2019, respectively, at the Family Medicine Center. Baseline perceptions of safety and quality were established using the data from the AHRQ Culture of Safety Survey in 2015. We performed multiple large-scope quality improvement projects that focused on identified deficiencies. The changes in perception were monitored over time every 2 years. We analyzed the results using the Kruskal-Wallace test (P=.05). Results: The AHRQ Culture of Safety Survey showed statistically significant improvement in patient centeredness, effectiveness, timeliness, efficiency, equitableness, and overall patient safety from 2015 to 2019. Some inconsistencies were seen between different sections of responses, likely due to wording interpretations by the participants. Conclusion: Overall, the AHRQ Culture of Safety Survey is an effective way to help monitor employee perception of multiple domains that lead to a safe and effective clinical environment as compared to other practices across the country. Clinic-wide implementation of quality and patient care strategies resulted in significant improvements in nearly every category of the survey.

2.
J Pediatr Hematol Oncol ; 44(2): e313-e318, 2022 03 01.
Artículo en Inglés | MEDLINE | ID: mdl-34054051

RESUMEN

Family medicine (FP) residency programs are located throughout Indiana, and most adults with sickle cell disease (SCD) in Indiana have access to a primary care clinic administered by a FP program. Allen County ranks third in SCD incidence in Indiana, but has few providers for adolescents, young adults (AYAs) and adults with SCD. Initiation of a novel partnership between Indianapolis-based adult hematologists (130 miles distant), and the FP program in Allen County aimed to educate FP residents about SCD, hydroxyurea, transition, and SCD complications. To determine the feasibility of utilizing online learning modules to educate FP residents about SCD care in AYA and adults, 3 online learning modules (comprehensive care of AYAs with SCD, hydroxyurea, and best practices in AYA transition) were developed and continuing medical education-accredited. Electronic pretest and posttest were distributed to 32 FP residents to test the retention of content through an Institutional Review Board approved protocol. This pilot study demonstrates that it is feasible to utilize online educational modules to educate providers about SCD care.


Asunto(s)
Anemia de Células Falciformes , Hidroxiurea , Adolescente , Anemia de Células Falciformes/complicaciones , Anemia de Células Falciformes/tratamiento farmacológico , Medicina Familiar y Comunitaria , Estudios de Factibilidad , Humanos , Hidroxiurea/uso terapéutico , Proyectos Piloto , Adulto Joven
3.
Curr Pharm Teach Learn ; 12(12): 1477-1483, 2020 12.
Artículo en Inglés | MEDLINE | ID: mdl-33092778

RESUMEN

BACKGROUND AND PURPOSE: Near-peer teaching is commonly used in experiential learning, residency training, and teaching certificate programs, but data on near-peer teaching in didactic course work are lacking. An innovative, near-peer learning opportunity that encouraged leadership and professionalism is described. EDUCATIONAL ACTIVITY AND SETTING: Thirty-six teams comprised of first-, second-, and third-year pharmacy students presented a 15-min oncology patient case to faculty reviewers. Presentations were focused on calculations, medicinal chemistry, pharmacology, and therapeutic application. Students were evaluated on communication skills, presentation skills, and presentation content. Additionally, students provided feedback about their perceptions of the laboratory experience. A chi-square test was used to determine significance or parity in student responses. FINDINGS: The majority of the students (82%) felt the teams worked well together and 85% indicated that they played an important role on their team, with second- and third-year students rating this item significantly higher than first year students. Additionally, 85% of participating students expressed that this experience provided an opportunity to demonstrate professionalism. SUMMARY: Integration of first-, second-, and third-year pharmacy students into teams was an innovative and effective method to provide opportunity for leadership, professionalism, and near-peer teaching through evaluation and presentation of an oncology patient case.


Asunto(s)
Profesionalismo , Estudiantes de Farmacia , Humanos , Liderazgo , Grupo Paritario , Aprendizaje Basado en Problemas
4.
J Sports Sci ; 38(2): 231-237, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31718476

RESUMEN

Excessive forces and/or loading rates during landing may place ballet dancers at risk for overuse injury. The ability to estimate and monitor the landing forces of ballet dancers could help to improve injury prevention and rehabilitation; however, force platforms are not conducive to testing outside of a laboratory. Fortunately, it may be possible to indirectly assess landing forces via a wearable accelerometer. The purposes of this study were to examine the relationship between impact accelerations, recorded via a pelvis-worn accelerometer, and the peak forces and loading rates during performance of a common ballet manoeuvre, and to examine if a wearable accelerometer is sensitive to fatigue-related changes in landing forces. Fifteen ballet dancers continuously performed a ballet manoeuvre until self-determined exhaustion while impact accelerations and landing forces were simultaneously recorded using an accelerometer and force platforms. We observed very strong, positive relationships between the impact accelerations and the peak forces and loading rates during the landings. In addition, the changes in impact accelerations with fatigue paralleled the changes in the peak forces and loading rates. As a result, it appears that a wearable accelerometer could be used to estimate and monitor landing forces in ballet dancers.


Asunto(s)
Acelerometría/instrumentación , Baile/fisiología , Dispositivos Electrónicos Vestibles , Adolescente , Fenómenos Biomecánicos , Trastornos de Traumas Acumulados/prevención & control , Baile/lesiones , Femenino , Humanos , Fatiga Muscular/fisiología , Estrés Mecánico , Adulto Joven
5.
J Prim Care Community Health ; 10: 2150132719836898, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30900500

RESUMEN

BACKGROUND: Clinical practice guidelines (CPGs) in medicine are recommendations supported by systematic review of evidence to facilitate optimal patient outcomes. Primary care practices are expected to implement more than 200 CPGs, overwhelming many practices. This qualitative study elucidated the perspectives and priorities of family medicine physicians and office managers in grouping CPGs to facilitate implementation. METHODS: A qualitative study was performed using individual, semistructured interviews. During the interviews the participants completed an open card-sort exercise grouping 20 CPGs. Purposive sampling was used to identify family medicine physicians and office managers practicing in medically underserved zip codes listed in the local medical society directory. Seven physicians and 6 office managers were interviewed. The interviews were transcribed and analyzed using thematic analysis and compared with the card-sort results. RESULTS: Thematic content analysis identified priorities and perspectives of office managers and physicians when grouping multiple CPGs for implementation: delegation, personalization, triggers, and change management. The card sort exercise revealed grouping by standardized preventive care visit, standardized rooming and discharge processes, and chronic illness. Chronic illness-based groupings and personalization of guidelines were recognized as presenting barriers to delegation of CPGs to the care team. Development of standardized preventive exams, standard rooming and discharge processes and chronic disease management were identified as promoting CPG adherence through team-based care. Standardized workflows provided opportunities for task delegation through predicable roles. Medicalization of CPG implementation relied heavily on the physician alone to remember to adhere to CPGs and inhibited task sharing by not giving office staff clear disease-based protocols to follow. CONCLUSIONS: This study identified priorities and perspectives of office managers and physicians when grouping multiple CPGs for concomitant implementation: delegation, personalization, triggers, and change management. Successful implementation was perceived to be associated with standardized preventive exams, standard rooming and discharge processes, and chronic disease management.


Asunto(s)
Actitud del Personal de Salud , Administración de Consultorio , Médicos de Familia , Guías de Práctica Clínica como Asunto , Flujo de Trabajo , Adulto , Atención Ambulatoria/organización & administración , Enfermedad Crónica , Femenino , Humanos , Ciencia de la Implementación , Masculino , Persona de Mediana Edad , Enfermeras y Enfermeros , Alta del Paciente , Delegación al Personal , Medicina Preventiva , Rol Profesional , Investigación Cualitativa , Adulto Joven
6.
PRiMER ; 3: 9, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-32537580

RESUMEN

INTRODUCTION: Graduate medical education depends on senior residents to facilitate peer education. Previous studies have described the benefits of resident-as-teacher (RaT) curricula; however, means of assessing these interventions have proven difficult. The purpose of this study was to provide meaningful evaluation of a novel RaT curriculum and scribing activity. METHODS: Didactic sessions on teaching skills were presented in July, 2017. First- and third-year residents then alternated scribing for each other for 4 weeks within the outpatient clinic to allow for near-peer educational exchange. Residents' attitudes toward teaching and perceptions of teaching abilities were assessed using preand postintervention surveys. Independent reviewers reviewed charts completed by PGY-1 residents during the scribing activity, and compared them to charts from the previous academic year. RESULTS: All first-year (n=12; 100%) and third-year (n=10; 100%) residents participated in the study. After participating in the RaT curriculum, residents were more comfortable giving feedback to other residents and felt better prepared to teach and assess the effectiveness of their teaching. Although there was no significant difference in ratings between the 2016 and 2017 charts, reviewers noted that the 2017 charts contained fewer obvious omissions, and third-year residents felt the charts were completed in a timelier manner. First-year residents saw 16% more patients in 2017 than they had in 2016, which expedited integration into the clinic. CONCLUSION: This innovative RaT curriculum with scribing activity improved residents' teaching and communication skills and provided first-year residents with a more efficient and meaningful orientation into the outpatient clinic.

7.
Curr Pharm Teach Learn ; 10(9): 1175-1183, 2018 09.
Artículo en Inglés | MEDLINE | ID: mdl-30497620

RESUMEN

INTRODUCTION: The purpose of this study was to simultaneously assess impact of enhanced training and anonymity on frequency, constructiveness, and professionalism of open-ended comments provided on course and instructor evaluations. METHODS: In a 2 × 2 factorial study, didactic students at one doctor of pharmacy program were randomized to receive enhanced training in providing constructive feedback on student evaluations of teaching or an unrelated control activity at the beginning of the academic year, and to provide or not provide an electronic signature at the time of evaluation completion for two consecutive semesters. After ensuring intercoder reliability and agreement among all investigators, one external investigator coded all open-ended comments based on the following factors: comment provided/comment not provided, constructive/less than constructive, professional/unprofessional, training/no training, and signed/unsigned. RESULTS: Of 836 opportunities to respond to open-ended items, 646 (77.3%) written comments were provided, which was similar by training (76.6% vs. 78.0%, p = 0.631) and signature (76.1% vs. 78.5%, p = 0.401) status. Of the 646 comments, 85.1% (n = 550) were constructive and 98.0% (n = 633) were professional. Students in the untrained/signed group were associated with decreased constructiveness (78.3%, OR 0.43, 95% CI 0.25-0.76, p = 0.003); overall, training was associated with increased constructiveness (88.3%, OR 1.70, 95% CI 1.09-2.65, p = 0.019). No factors were negatively or positively associated with professionalism when accounting for covariates. DISCUSSION: Most students provided comments on course and instructor evaluations; most were constructive and professional. CONCLUSION: Study group assignment did not substantially impact comment frequency or professionalism. Assignment to enhanced training, regardless of signature status, significantly increased constructiveness.


Asunto(s)
Evaluación Educacional/normas , Profesionalismo/normas , Autoinforme , Estudiantes de Farmacia/psicología , Actitud del Personal de Salud , Distribución de Chi-Cuadrado , Curriculum/normas , Curriculum/tendencias , Evaluación Educacional/métodos , Evaluación Educacional/estadística & datos numéricos , Humanos , Indiana , Reproducibilidad de los Resultados , Estudiantes de Farmacia/estadística & datos numéricos
8.
Pharmacogenomics ; 19(5): 393-399, 2018 04.
Artículo en Inglés | MEDLINE | ID: mdl-29517466

RESUMEN

AIM: The aim of this study was to investigate 60 SNPs pertaining to drug metabolism and pharmacodynamics in the Burmese refugee population in the Fort Wayne, Indiana area to better inform patient care. MATERIALS & METHODS: Sixty-two self-identified Burmese refugees were genotyped for 60 common SNPs pertaining to pharmacokinetic and pharmacodynamic pharmacogenes. The resulting allelic frequencies were compared with Ensembl's database for surrounding populations to Myanmar and America. RESULTS: The frequency of OPRM1, CYP2D6, SLCO1B1, MTHFR and VKORC1 were approximately 20% different in the Burmese refugee population as compared with the Ensembl populations. CONCLUSION: Our study demonstrates that genetic differences are expected to affect drug efficacy in patients with a Burmese background.


Asunto(s)
Frecuencia de los Genes/genética , Adulto , Pueblo Asiatico , Bases de Datos Genéticas , Femenino , Predisposición Genética a la Enfermedad , Variación Genética , Genotipo , Humanos , Indiana , Masculino , Mianmar/etnología , Farmacogenética , Polimorfismo de Nucleótido Simple/genética , Refugiados
9.
PRiMER ; 2: 15, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-32818187

RESUMEN

BACKGROUND AND OBJECTIVE: Evaluating the time taken at each step in a patient office visit is important for physicians and clinical staff for clinic workflow improvements. Very little data exists on efficiency that is not self-reported by physicians. Employees often have perceptions of the efficiency of a clinic without supporting data. This study examined whether employee perceptions of the amount of patient time spent at various points in the visit matched observed times. METHODS: Observational cohort study methods and a cross-sectional survey were used in the fall of 2017 in a family practice residency outpatient clinic. Clinical staff (physicians and support staff) were surveyed for their perceptions of patients' time spent at each checkpoint in an office visit. A total of 885 visits were recorded, with 705 being included after review. Time spent at various steps, appointment type, and clinician years of experience were assessed with t-test for statistical significance. RESULTS: The anonymous clinic survey had a 75.5% response rate (37/49) and showed "rooming patients" and "waiting in the exam room to be seen" were the two areas that took longer than expected. The observed data confirmed this perception, showing that rooming and waiting in the exam room each took longer than the staff expected. These values were also greater than available national average times. There was a significant correlation between physician training year and visit length. There was no correlation for nursing experience and patient visit times. CONCLUSIONS: The staff-perceived inefficiencies correlated with observed inefficiencies. Addressing these problems would improve patient care and overall clinic workflow.

10.
Health Serv Res Manag Epidemiol ; 4: 2333392817727424, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28959707

RESUMEN

PURPOSE: To determine the role of opioids in drug overdose deaths in Allen County, Indiana between January 1, 2008, and December 31, 2015. METHODS: File review of 418 overdose deaths was performed using Indiana State Department of Health death certificates available through the Allen County Coroner's Office. Data from autopsy and toxicology reports and coroner-requested prescribing data from Indiana's Prescription Monitoring Program were reviewed. Cause of death and available data were analyzed to identify patterns and trends related to overdose deaths. RESULTS: Four hundred eighteen drug overdose deaths were identified (336 accidental, 66 intentional, and 16 undetermined). Mean age was 42.5 years, 88.5% were Caucasian, and 68.7% were employed. The majority of deaths occurred at a place of residence (71.4%) and with other people present (57.5% of the time). Depression was the most common comorbidity identified. The most common drug classes identified by toxicology were opioids, followed by benzodiazepines. Significant increases in both heroin (35% of deaths in 2015 versus 8.2% in 2013) and fentanyl (30% of deaths in 2015 versus 2.2% in 2011) were observed. CONCLUSIONS: Drug overdose continues to be a significant cause of death in Allen County. The majority of deaths were accidental and in relatively young, employed individuals. Prevention and awareness strategies should be encouraged, given that the majority of overdose deaths occurred at a place of residence with other people frequently present. Additional concerns about patterns of drug use were confirmed with marked increases in both heroin and fentanyl contributing to overdose deaths in the latter part of the study.

11.
Drug Dev Ind Pharm ; 40(12): 1565-75, 2014 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-24766553

RESUMEN

Solid lipid nanoparticles (SLNs) are gaining importance due to numerous advantages they offer as a drug delivery system. SLN incorporate poorly soluble drugs, proteins, biologicals, etc. SLN are prepared by techniques like high-pressure homogenization, sonication and employs a wide range of lipids and surfactants. Physicochemical characterization techniques include particle size analysis, zeta potential and determination of crystallinity/polymorphism. Furthermore, drug loading and drug entrapment efficiency are common parameters used to test the efficiency of SLN. Most importantly, the functionality assay of SLN is essential to predict the activity and performance in vivo. The review presented discusses the importance of SLN in drug delivery with emphasis on principles and limitations associated with their physicochemical characterization.


Asunto(s)
Sistemas de Liberación de Medicamentos/métodos , Lípidos/química , Nanopartículas/química , Tamaño de la Partícula , Animales , Fenómenos Químicos , Química Farmacéutica/métodos , Humanos , Lípidos/administración & dosificación , Nanopartículas/administración & dosificación
12.
J Pharm Sci ; 102(8): 2589-98, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-23761019

RESUMEN

Europium (Eu), dysprosium (Dy), samarium (Sm), and terbium (Tb) complexes were prepared using the neutral tridentate chelator 2,6-bis(1-benzyl-1,2,3-triazol-4-yl)pyridine and one equivalent of each lanthanide salt. The physicochemical, aerodynamic, and in vitro cellular properties of each lanthanide metal complex were studied to determine their viability as cell surface fluorescent probes. Each compound was characterized by electrospray ionization mass spectroscopy (ESI-MS), ultraperformance liquid chromatography (UPLC), differential scanning calorimetry (DSC), and thermogravimetic analysis (TGA). Upon excitation at 320 nm each complex displayed characteristic lanthanide-based fluorescence emission in the visible wavelength range with stokes shifts greater than 200 nm. Each complex was found to be chemically stable when exposed to pH range of 1-11 for 72 h and resistant to photobleaching. To simulate pulmonary administration of these fluorophores, the aerodynamic properties of the Eu and Tb complexes were determined using a next generation impactor (NGI). This measurement confirmed that the complexes retain their fluorescence emission properties after nebulization. Cellular cytotoxicity was determined on A-549 lung cancer cell line using methylthiazol tetrazolium (MTT) cytotoxicity assay at 24, 48, and 72 h postexposure to the complexes. The complexes showed a dose and time-dependent effect on the percent viability of the cells.


Asunto(s)
Quelantes/química , Complejos de Coordinación/química , Colorantes Fluorescentes/química , Elementos de la Serie de los Lantanoides/química , Triazoles/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Quelantes/toxicidad , Complejos de Coordinación/toxicidad , Colorantes Fluorescentes/toxicidad , Humanos , Elementos de la Serie de los Lantanoides/toxicidad , Solubilidad , Triazoles/toxicidad
13.
Hosp Pharm ; 48(6): 479-83, 2013 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-24421509

RESUMEN

BACKGROUND: Patients who undergo Roux-en-Y gastric bypass (RYGB) surgery have self-reported considerable postoperative pain, often requiring opioid administration. OBJECTIVE: To determine whether continuous delivery of local anesthetic via an infusion pump system decreased postoperative opioid usage in post-RYGB patients. METHODS: The electronic health record was used to identify and review 289 patients who underwent RYGB at our institution from January 2009 to October 2011. The treatment group received a continuous infusion of 0.375% bupivacaine administered by intraperitoneal soaker catheter for 48 hours via an infusion pump; the control group did not receive a pump or local anesthetic. Both groups received general anesthesia, nausea prophylaxis, and pain medication. Pain management consisted of opioid-containing patient-controlled analgesia (PCA) for the first 24 hours. Patients transitioned to supplemental intravenous opioid boluses, plus an oral opioid, for the remainder of their stay. Opioid use was measured in terms of morphine equivalents. Secondary outcomes included visual analog scale (VAS) pain scores and length of hospitalization. RESULTS: Morphine equivalents over the postoperative time period studied were significantly lower in the bupivacaine group than the control group (133 vs 106 mg, respectively; P = .001). There was no significant difference in VAS scores between the 2 groups (P = .80). Finally, the length of hospitalization between the 2 groups did not differ (P = .77). CONCLUSIONS: We have shown that continuous infusion of bupivacaine, administered via a pain pump system, may have decreased postoperative opioid utilization. There were no differences in VAS scores or length of hospitalization between groups.

14.
Am J Pharm Educ ; 76(8): 158, 2012 Oct 12.
Artículo en Inglés | MEDLINE | ID: mdl-23129857

RESUMEN

Objectives. To build an integrated medicinal chemistry learning community of campus and distance pharmacy students though the use of innovative technology and interdisciplinary teaching.Design. Mechanisms were implemented to bring distance students into campus-based medicinal chemistry classrooms in real time, stimulate interaction between instructors and various student cohorts, and promote group work during class. Also, pharmacy clinician colleagues were recruited to contribute to the teaching of the 3 medicinal chemistry courses.Assessment. Student perceptions on the value of technology to build community and advance learning were gleaned from course evaluations, in class feedback, and conversations with class officers and student groups. Responses on a survey of second-year students confirmed the benefits of interdisciplinary content integration on engagement and awareness of the connection between drug chemistry and pharmacy practice. A survey of clinician colleagues who contributed to teaching the 3 medicinal chemistry courses found their views were similar to those of students.Conclusions. The purposeful use of technology united learners, fostered communication, and advanced content comprehension in 3 medicinal chemistry courses taught to campus and distance students. Teaching collaboration with pharmacy clinicians enhanced learner interest in course content and provided insight into the integrated nature of the profession of pharmacy.


Asunto(s)
Química Farmacéutica/educación , Educación en Farmacia/métodos , Tecnología Educacional/métodos , Estudiantes de Farmacia , Comunicación , Conducta Cooperativa , Curriculum , Recolección de Datos , Educación a Distancia/métodos , Evaluación Educacional , Docentes , Humanos , Comunicación Interdisciplinaria , Enseñanza/métodos
15.
Am J Health Syst Pharm ; 68(23): 2241-7, 2011 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-22095812

RESUMEN

PURPOSE: Pharmacokinetic considerations in patients who have undergone Roux-en-Y gastric bypass (RYGB) are explored. SUMMARY: The prevalence of obesity, especially morbid obesity, has dramatically increased in recent years. In response, the number of bariatric surgeries performed has risen sharply, as this surgery is the technique demonstrated as being the most effective for sustained treatment of morbid obesity. RYGB, the most popular technique in the United States, combines the principle of restriction (dramatically decreasing stomach size) with malabsorption (bypassing the entire duodenum). It stands to reason that a decrease in gastric and intestinal absorptive surface area may considerably affect oral bioavailability of some drugs. Drugs that require a more acidic environment for absorption, uncoating, or activation and drugs that rely on intestinal transporters located in the duodenum for proper absorption would be most affected. Practitioners looking for guidance in tailoring pharmacotherapy to the RYGB patient will find little help in the primary literature at this time. Until more pharmacokinetic studies are available, practitioners may apply and log P of individual the principles of pK(a) drugs in the attempt to predict the potential impact of the RYGB on a drug's absorption. Likewise, if a drug relies on certain transporters located with highest frequency in the duodenum, alternative therapies can be selected that do not rely on such transport mechanisms for absorption. CONCLUSION: The pK(a), log P, and intestinal transport mechanisms should be considered when determining which drugs may have altered pharmacokinetics in patients who have undergone RYGB.


Asunto(s)
Derivación Gástrica/métodos , Obesidad Mórbida/cirugía , Farmacocinética , Disponibilidad Biológica , Transporte Biológico , Humanos , Absorción Intestinal , Obesidad Mórbida/epidemiología , Preparaciones Farmacéuticas/administración & dosificación , Preparaciones Farmacéuticas/metabolismo , Prevalencia , Estados Unidos
16.
J Org Chem ; 74(8): 2975-81, 2009 Apr 17.
Artículo en Inglés | MEDLINE | ID: mdl-19320430

RESUMEN

Prenylcysteine derivatives are of interest for a variety of different biological reasons, including probing the CaaX protein processing pathway. A solid-phase synthesis protocol for the preparation of prenylcysteines using 2-chlorotrityl chloride resin as a solid support has been developed. A series of novel amide-modified farnesylcysteine analogs were synthesized in both high purity and yield under mild conditions. The farnesylcysteine analogs were evaluated using human isoprenylcysteine carboxyl methyltransferase as a biological target, and several new inhibitors, one with significantly enhanced potency, were identified.


Asunto(s)
Cisteína/análogos & derivados , Proteína Metiltransferasas/química , Compuestos de Tritilo/química , Secuencia de Aminoácidos , Cromatografía Líquida de Alta Presión , Cisteína/síntesis química , Cisteína/química , Humanos , Estructura Molecular , Proteína Metiltransferasas/metabolismo , Extracción en Fase Sólida
17.
Am J Pharm Educ ; 73(8): 150, 2009 Dec 17.
Artículo en Inglés | MEDLINE | ID: mdl-20221343

RESUMEN

OBJECTIVES: To evaluate the effect of electronic integration of embedded prerequisite information (EPI) on student learning. DESIGN: Specific prerequisite information presented in a Chemical Basis of Drug Action course and important to understanding new topics presented in subsequent courses was identified and embedded in online course materials using pop-ups and hyperlinks. Students were encouraged to review the EPI. ASSESSMENT: There was no significant difference (P<0.05) between student performance on examination 3, which covered embedded information, and student performance on examination 1 which did not. Employing the Likert scale, a cumulative average of 75% and 87% of the campus and distance students rated the impact of EPI slightly positive to positive, respectively. CONCLUSION: Although student performance did not improve with the introduction of EPI, both campus and distance students viewed the EPI positively.


Asunto(s)
Química Farmacéutica/educación , Instrucción por Computador , Educación a Distancia , Educación en Farmacia/métodos , Estudiantes de Farmacia , Integración de Sistemas , Adulto , Comprensión , Curriculum , Evaluación Educacional , Femenino , Humanos , Masculino , Recuerdo Mental , Percepción , Desarrollo de Programa , Evaluación de Programas y Proyectos de Salud , Programas Informáticos , Interfaz Usuario-Computador , Adulto Joven
18.
Bioorg Med Chem Lett ; 16(16): 4420-3, 2006 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-16777414

RESUMEN

N-Acetyl-S-farnesyl-L-cysteine (AFC) is the minimal substrate for the enzyme isoprenylcysteine carboxyl methyltransferase (Icmt). A series of amide-modified farnesylcysteine analogs were synthesized and screened against human Icmt. From a 23-membered library of compounds, six inhibitors were identified and evaluated further. The adamantyl derivative 7c was the most potent inhibitor with an IC(50) of 12.4 microM.


Asunto(s)
Cisteína/química , Proteína Metiltransferasas/antagonistas & inhibidores , Amidas/química , Secuencias de Aminoácidos , Membrana Celular/metabolismo , Química Farmacéutica , Diseño de Fármacos , Humanos , Concentración 50 Inhibidora , Modelos Químicos , Proteína Metiltransferasas/química
19.
Bioorg Med Chem Lett ; 15(22): 5080-3, 2005 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-16183278

RESUMEN

N-Acetyl-S-farnesyl cysteine (AFC) is the minimal synthetic substrate for the enzyme Icmt, which methylates prenylated proteins. The desthio-AFC isostere 2 has been synthesized in racemic form. This analog was not an Icmt substrate, but instead a weak inhibitor with an IC50 of approximately 325 microM.


Asunto(s)
Cisteína/análogos & derivados , Cisteína/síntesis química , Sulfuros/síntesis química , Concentración 50 Inhibidora , Metiltransferasas/antagonistas & inhibidores , Metiltransferasas/metabolismo , Estructura Molecular , Sulfuros/química , Terpenos/química , Terpenos/metabolismo
20.
J Chem Inf Model ; 45(4): 1047-52, 2005.
Artículo en Inglés | MEDLINE | ID: mdl-16045300

RESUMEN

Protein farnesyltransferase (FTase) is an important anticancer drug target. In an effort to develop isoprenoid diphosphate-based FTase inhibitors, striking variations have been observed in the ability of conservatively modified analogues to bind to the enzyme. For example, 2Z-GGPP is an alternative substrate with high binding affinity, while GGPP is not an alternative substrate. Using the availability of high-resolution FTase crystal structures, we have used pharmacophore and docking studies to elucidate a new binding pocket for isoprenoid analogues. The unique conformations between the first two isoprene units of 2Z-GGPP, but not GGPP, allows 2Z-GGPP to exploit this new binding pocket. The discovered conformation allows the molecule to adopt a reactive conformation while placing hydrophobic groups within the predominately hydrophobic binding pocket. This computational finding is supported by NMR studies on (13)C-labeled 2Z-farnesol, which confirm that the computationally predicted conformation is also favored in solution. These discoveries suggest that ligand conformational flexibility may be an important design consideration for the development of both inhibitors and alternative substrates of FTase.


Asunto(s)
Simulación por Computador , Farnesiltransferasa/química , Farnesiltransferasa/metabolismo , Fosfatos de Poliisoprenilo/química , Conformación Proteica , Sitios de Unión , Farnesiltransferasa/antagonistas & inhibidores , Estructura Molecular , Fosfatos de Poliisoprenilo/farmacología , Unión Proteica , Sesquiterpenos , Especificidad por Sustrato
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