The Grizzly, March 4, 1983

Zeta Chi Suspended: Fraternity Disciplined for Pledging Violations • Symposium Topics Discussed • New Forum Committee to Revise System • Letters to the Editor: Alumnus Responds to Grizzly Policy • Committee Reviews Appeals Procedure • Meistersingers Tour • Exam Schedule • Woodcuts at Myrin • Stravinsky Program Ends Winterfest • Lantern Deadline Approaches • Lewis on Wall Street • Alpha Sigma Nu Tops GPAs • Roving Reporter: The Administration is Proposing to put a Live-in Dean in 97 of New Men\u27s Dorm • Pre-Legal Society Resurrected • Swimmers Perform Beyond Expectation • Bear Blades Blaze to Victory • Gymnasts Draw No. 2 Ratinghttps://digitalcommons.ursinus.edu/grizzlynews/1096/thumbnail.jp

The Grizzly, February 18, 1983

Rally at Bomberger: Students Protest Criticism • Rushes, Administration Meet Before Pledging • Editorial: Staff Members Defend Grizzly • USGA Notes • Letters to the Editor: Letter to the Editor Receives Support; Constructive Criticism Appreciated; Student Interest Sparked; Irresponsible Groups Cause Anger • Is Reaganomics a Reality? • Admissions Standards at Ursinus • President\u27s Corner • Happy Birthday to U • Talent Show Tonight • Occupational Hazards • Fighting Ursini Head to MACs Optimistically • Inconsistency Still Haunting Women\u27s Basketball • Gymnastics Ranked 13th • Badminton Team Tops Rosemont and Moravian • Lady Swimmers Boast 9-1 Record • Werley\u27s Record Speaks for Itselfhttps://digitalcommons.ursinus.edu/grizzlynews/1094/thumbnail.jp

The Grizzly, February 11, 1983

Bookstore Explains Pricing Policy • Scottish Scholarships Offered to Sophomores • Weekend Alcohol Policy: Campus is Dry • Ursinus Gets Bucks From Sears Roebuck • President\u27s Corner • Visser Fills Exhibits in Corson • Letters to the Editor: Professor Laments Social Conditions at UC; I.F.C. President Irate; President\u27s Response; Bitter About Policy • Varying Viewpoints • Stravinsky to End Winterfest • U.C. Flu Flattens Students • Reaganomics Forum • Key Shooting Aids Lady Hoopsters\u27 Record • Basketball Laments Second Half Loss • Swimmers Glide to Third Straight Victory • Grapplers Deemed Tough • Basketball: End of an Era?? • Swimmers Stroke for Two Wins • Gymnasts Win by 0.75https://digitalcommons.ursinus.edu/grizzlynews/1093/thumbnail.jp

The Grizzly, February 25, 1983

USGA Plans Communication Revision • Foley, D\u27Alesio First Place Winners at Talent Show • College Union Holds Tenth Anniversary • Ritter Production Opens: Skin of Our Teeth • Mass is Popular: Newman Society Links U.C. • Small Heads Alcohol Committee • SPC Seeks Editors • Union Calendar • Grizzly Looks For New Business Manager • Winterfest 1983: International Desserts Festival Tonight • Winterfest Schedule • Letters to the Editor: Admissions Dean Corrects Errors; Hoop Club President Responds; Student Reacts Negatively • Social Life at Ursinus Should be Improved • In the Gates • Registrar Announces Pre-Registration • President\u27s Corner • Roving Reporter: Do You Think the New Alcohol Policy Proposed by the Administration was the Correct Way to Handle the Situations That Occurred on Campus? • Bears Drown Monarchs • Women\u27s Swimming Ends 10-1 • MAC Competition: Wrestlers Take Seventh • Gymnasts Move up a Rank • Lady Hoopsters Finish With Victoryhttps://digitalcommons.ursinus.edu/grizzlynews/1095/thumbnail.jp

Structure–activity relationships of a small-molecule inhibitor of the PDZ domain of PICK1

Recently, we described the first small-molecule inhibitor, (E)-ethyl 2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate (1), of the PDZ domain of protein interacting with Cα-kinase 1 (PICK1), a potential drug target against brain ischemia, pain and cocaine addiction. Herein, we explore structure–activity relationships of 1 by introducing subtle modifications of the acryloylcarbamate scaffold and variations of the substituents on this scaffold. The configuration around the double bond of 1 and analogues was settled by a combination of X-ray crystallography, NMR and density functional theory calculations. Thereby, docking studies were used to correlate biological affinities with structural considerations for ligand–protein interactions. The most potent analogue obtained in this study showed an improvement in affinity compared to 1 and is currently a lead in further studies of PICK1 inhibition